PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 16000699-11 2005 Maximum amplitudes of ATP-evoked P2X-mediated currents (I(ATP)) were significantly increased for P2X2, P2X(2/6), and P2X5 receptor subtypes after coexpression of ENaC. PP242 33-36 purinergic receptor P2X, ligand gated ion channel, 2 L homeolog Xenopus laevis 97-101 18404518-4 2005 Caspase-3 activation and DNA fragmentation in rPCNs induced by the P2X(7)R agonist BzATP were inhibited by the P2X(7)R antagonist oxidized ATP (oATP) or by pre-treatment of cells with P2X(7)R antisense oligonucleotide indicating a direct involvement of the P2X(7)R in nucleotide-induced neuronal cell death. PP242 67-70 caspase 3 Rattus norvegicus 0-9 12122056-5 2002 Extracellular and whole-cell voltage-clamp recordings in CA3 revealed that bath application of the potent P2X(7) agonist 2",3"-O-(4-benzoylbenzoyl)-ATP (Bz-ATP) caused a long-lasting inhibition of neurotransmission at mossy fiber-CA3 synapses. PP242 106-109 carbonic anhydrase 3 Rattus norvegicus 57-60 12122056-5 2002 Extracellular and whole-cell voltage-clamp recordings in CA3 revealed that bath application of the potent P2X(7) agonist 2",3"-O-(4-benzoylbenzoyl)-ATP (Bz-ATP) caused a long-lasting inhibition of neurotransmission at mossy fiber-CA3 synapses. PP242 106-109 carbonic anhydrase 3 Rattus norvegicus 230-233 34731371-0 2022 mTOR inhibitor PP242 increases antitumor activity of sulforaphane by blocking Akt/mTOR pathway in esophageal squamous cell carcinoma. PP242 15-20 mechanistic target of rapamycin kinase Homo sapiens 0-4 33801030-4 2021 A structure-based pharmacophore (SBP) model exploiting the key features of a selective mTOR inhibitor, Torkinib directed at the ATP-binding pocket was generated. PP242 103-111 mechanistic target of rapamycin kinase Homo sapiens 87-91 34731371-0 2022 mTOR inhibitor PP242 increases antitumor activity of sulforaphane by blocking Akt/mTOR pathway in esophageal squamous cell carcinoma. PP242 15-20 AKT serine/threonine kinase 1 Homo sapiens 78-81 34731371-0 2022 mTOR inhibitor PP242 increases antitumor activity of sulforaphane by blocking Akt/mTOR pathway in esophageal squamous cell carcinoma. PP242 15-20 mechanistic target of rapamycin kinase Homo sapiens 82-86 34731371-9 2022 The mechanism was that PP242 abrogated the promoting effects of SFN on p-p70S6K (Thr389) and p-Akt (Ser473) in ESCC. PP242 23-28 ribosomal protein S6 kinase B1 Homo sapiens 73-79 34731371-9 2022 The mechanism was that PP242 abrogated the promoting effects of SFN on p-p70S6K (Thr389) and p-Akt (Ser473) in ESCC. PP242 23-28 AKT serine/threonine kinase 1 Homo sapiens 95-98 34731371-10 2022 CONCLUSIONS: Our findings demonstrate that PP242 enhances the anti-tumor activity of SFN by blocking SFN-induced activation of Akt/mTOR pathway in ESCC, which provides a rationale for treating ESCC using SFN combined with Akt/mTOR pathway inhibitors. PP242 43-48 AKT serine/threonine kinase 1 Homo sapiens 127-130 34731371-10 2022 CONCLUSIONS: Our findings demonstrate that PP242 enhances the anti-tumor activity of SFN by blocking SFN-induced activation of Akt/mTOR pathway in ESCC, which provides a rationale for treating ESCC using SFN combined with Akt/mTOR pathway inhibitors. PP242 43-48 mechanistic target of rapamycin kinase Homo sapiens 131-135 35439535-7 2022 Our results also confirmed that mTOR inhibitor sensitized senolytic cell death is apoptotic and pan-mTOR inhibitors PP242 and AZD8055 works more effectively than mTORC1 inhibitor Rapamycin. PP242 116-121 Megator Drosophila melanogaster 32-36 34911836-7 2021 After treatment with mTOR inhibitor PP242, the expression of LC3-II was detected by Western blotting. PP242 36-41 mechanistic target of rapamycin kinase Homo sapiens 21-25 34911836-7 2021 After treatment with mTOR inhibitor PP242, the expression of LC3-II was detected by Western blotting. PP242 36-41 microtubule associated protein 1 light chain 3 alpha Homo sapiens 61-64 34911836-8 2021 Total RNAs of 3 cases of RA-FLSs before and after treatment with mTOR inhibitor PP242 were extracted by TRIzol and screened by Agilent Human ceRNA Microarray 2019 (4x180 K, design ID: 086188) chip. PP242 80-85 mechanistic target of rapamycin kinase Homo sapiens 65-69 34911836-13 2021 After 6 RA-FLSs were treated with PP242, the expression level of autophagy marker protein LC3-II was increased (P<0.05). PP242 34-39 microtubule associated protein 1 light chain 3 alpha Homo sapiens 90-93 34532116-0 2021 A dual-targeted molecular therapy of PP242 and cetuximab plays an anti-tumor effect through EGFR downstream signaling pathways in colorectal cancer. PP242 37-42 epidermal growth factor receptor Homo sapiens 92-96 34532116-3 2021 Methods: Here we combined the anti-EGFR monoclonal antibody cetuximab (CTX) with the mTOR inhibitor PP242 in CRC cell lines and mouse xenograft models and discussed the changes of EGFR downstream signaling pathways of CRC cell lines. PP242 100-105 epidermal growth factor receptor Mus musculus 35-39 34532116-3 2021 Methods: Here we combined the anti-EGFR monoclonal antibody cetuximab (CTX) with the mTOR inhibitor PP242 in CRC cell lines and mouse xenograft models and discussed the changes of EGFR downstream signaling pathways of CRC cell lines. PP242 100-105 mechanistic target of rapamycin kinase Mus musculus 85-89 34532116-5 2021 In BRAF wild-type Caco-2 cells, combined application of CTX and PP242 inhibited the activation of the EGFR and its downstream signaling pathways. PP242 64-69 B-Raf proto-oncogene, serine/threonine kinase Homo sapiens 3-7 34532116-5 2021 In BRAF wild-type Caco-2 cells, combined application of CTX and PP242 inhibited the activation of the EGFR and its downstream signaling pathways. PP242 64-69 epidermal growth factor receptor Homo sapiens 102-106 34532116-7 2021 We revealed that the combined application of CTX and PP242 can inhibit tumor growth and proliferation by inhibiting the phosphorylation of key molecules in EGFR downstream MEK-ERK and MEK 4/7 (MKK)-c-Jun N-terminal kinase (JNK) signaling pathways in BRAF wild-type CRC cells. PP242 53-58 epidermal growth factor receptor Mus musculus 156-160 34532116-7 2021 We revealed that the combined application of CTX and PP242 can inhibit tumor growth and proliferation by inhibiting the phosphorylation of key molecules in EGFR downstream MEK-ERK and MEK 4/7 (MKK)-c-Jun N-terminal kinase (JNK) signaling pathways in BRAF wild-type CRC cells. PP242 53-58 midkine Mus musculus 172-175 34532116-7 2021 We revealed that the combined application of CTX and PP242 can inhibit tumor growth and proliferation by inhibiting the phosphorylation of key molecules in EGFR downstream MEK-ERK and MEK 4/7 (MKK)-c-Jun N-terminal kinase (JNK) signaling pathways in BRAF wild-type CRC cells. PP242 53-58 mitogen-activated protein kinase 1 Mus musculus 176-179 34532116-7 2021 We revealed that the combined application of CTX and PP242 can inhibit tumor growth and proliferation by inhibiting the phosphorylation of key molecules in EGFR downstream MEK-ERK and MEK 4/7 (MKK)-c-Jun N-terminal kinase (JNK) signaling pathways in BRAF wild-type CRC cells. PP242 53-58 mitogen-activated protein kinase kinase 4 Homo sapiens 184-191 34532116-7 2021 We revealed that the combined application of CTX and PP242 can inhibit tumor growth and proliferation by inhibiting the phosphorylation of key molecules in EGFR downstream MEK-ERK and MEK 4/7 (MKK)-c-Jun N-terminal kinase (JNK) signaling pathways in BRAF wild-type CRC cells. PP242 53-58 mitogen-activated protein kinase 8 Homo sapiens 223-226 34532116-7 2021 We revealed that the combined application of CTX and PP242 can inhibit tumor growth and proliferation by inhibiting the phosphorylation of key molecules in EGFR downstream MEK-ERK and MEK 4/7 (MKK)-c-Jun N-terminal kinase (JNK) signaling pathways in BRAF wild-type CRC cells. PP242 53-58 Braf transforming gene Mus musculus 250-254 34532116-8 2021 In addition, we found that in BRAF mutant CRC cells, the monotherapy of PP242 resulted in negative feedback increased EGFR phosphorylation rates, accompanied by significant up-regulation of downstream MEK and ERK phosphorylation. PP242 72-77 Braf transforming gene Mus musculus 30-34 34532116-8 2021 In addition, we found that in BRAF mutant CRC cells, the monotherapy of PP242 resulted in negative feedback increased EGFR phosphorylation rates, accompanied by significant up-regulation of downstream MEK and ERK phosphorylation. PP242 72-77 epidermal growth factor receptor Mus musculus 118-122 34532116-8 2021 In addition, we found that in BRAF mutant CRC cells, the monotherapy of PP242 resulted in negative feedback increased EGFR phosphorylation rates, accompanied by significant up-regulation of downstream MEK and ERK phosphorylation. PP242 72-77 midkine Mus musculus 201-204 34532116-8 2021 In addition, we found that in BRAF mutant CRC cells, the monotherapy of PP242 resulted in negative feedback increased EGFR phosphorylation rates, accompanied by significant up-regulation of downstream MEK and ERK phosphorylation. PP242 72-77 mitogen-activated protein kinase 1 Mus musculus 209-212 34073791-4 2021 Second-generation inhibitor, pp242, inhibits both mTORC1 and mtORC2, which led us to explore its therapeutic potential after SCI and compare it to RAPA treatment. PP242 29-34 CREB regulated transcription coactivator 1 Mus musculus 50-56 34073791-4 2021 Second-generation inhibitor, pp242, inhibits both mTORC1 and mtORC2, which led us to explore its therapeutic potential after SCI and compare it to RAPA treatment. PP242 29-34 CREB regulated transcription coactivator 2 Mus musculus 61-67 34073791-9 2021 These results suggest that dual mTOR inhibition by pp242 after SCI induces distinct mechanisms and leads to recovery somewhat inferior to that following RAPA treatment. PP242 51-56 mechanistic target of rapamycin kinase Rattus norvegicus 32-36 35439535-7 2022 Our results also confirmed that mTOR inhibitor sensitized senolytic cell death is apoptotic and pan-mTOR inhibitors PP242 and AZD8055 works more effectively than mTORC1 inhibitor Rapamycin. PP242 116-121 Megator Drosophila melanogaster 100-104 32861759-13 2020 Meanwhile, PFOS-mediated lysosomal function and the inhibitory effect of autophagic flux could be reversed by PP242 at 40 nM concentration, an mTOR inhibitor. PP242 110-115 mechanistic target of rapamycin kinase Homo sapiens 143-147 35472745-6 2022 Thus, the bromodomain inhibitor RVX-208 significantly augmented the therapeutic effects of the dual mTORC1/2 inhibitors, OSI-027 and PP242, both in vitro and in a human xenograft murine model. PP242 133-138 CREB regulated transcription coactivator 2 Mus musculus 100-108 33790341-4 2021 PP242, an inhibitor of mTORC1/2 pathways exhibits potent natriuretic actions and completely prevented salt-induced hypertension in SS rats. PP242 0-5 CREB regulated transcription coactivator 2 Mus musculus 23-31 33790341-8 2021 These responses were almost completely abolished by pretreatment of mTAL with 10 microM PP242, indicating that mTORC1/2 pathways were involved in the H2O2 induced increase of [Na+]i. mTAL cell volume remained unchanged (+- 1%) by H2O2 as determined by 3D reconstruction confocal laser scanning microscopy techniques. PP242 88-93 CREB regulated transcription coactivator 2 Mus musculus 111-119 33790341-9 2021 Consistent with the microscopy data, Western Blot analysis of proteins obtained from freshly isolated mTAL treated with 100 microM H2O2 exhibited increased activity/phosphorylation of AKT (pAKTSer473/AKT) that was inhibited by PP242. PP242 227-232 AKT serine/threonine kinase 1 Rattus norvegicus 184-187 33790341-9 2021 Consistent with the microscopy data, Western Blot analysis of proteins obtained from freshly isolated mTAL treated with 100 microM H2O2 exhibited increased activity/phosphorylation of AKT (pAKTSer473/AKT) that was inhibited by PP242. PP242 227-232 AKT serine/threonine kinase 1 Rattus norvegicus 190-193 32990653-7 2020 Results: V-ATPase activity in PTs was markedly enhanced by insulin, and its activation was completely inhibited by bafilomycin (a V-ATPase-specific inhibitor), Akt inhibitor VIII, and PP242 (an mTORC1/2 inhibitor), but not by rapamycin (an mTORC1 inhibitor). PP242 184-189 ATPase, H+ transporting, lysosomal V0 subunit D2 Mus musculus 9-17 33067464-1 2020 PP242, an inhibitor of mechanistic target of rapamycin (mTOR), displays potent anticancer effects against various cancer types. PP242 0-5 mechanistic target of rapamycin kinase Mus musculus 23-54 33067464-1 2020 PP242, an inhibitor of mechanistic target of rapamycin (mTOR), displays potent anticancer effects against various cancer types. PP242 0-5 mechanistic target of rapamycin kinase Mus musculus 56-60 33067464-8 2020 This study reveals new insights into the underlying anticancer mechanism of the dual mTOR inhibitor PP242, and could help further to facilitate the understanding of PP242 effects in the clinical application. PP242 100-105 mechanistic target of rapamycin kinase Mus musculus 85-89 33067464-8 2020 This study reveals new insights into the underlying anticancer mechanism of the dual mTOR inhibitor PP242, and could help further to facilitate the understanding of PP242 effects in the clinical application. PP242 165-170 mechanistic target of rapamycin kinase Mus musculus 85-89 32990653-7 2020 Results: V-ATPase activity in PTs was markedly enhanced by insulin, and its activation was completely inhibited by bafilomycin (a V-ATPase-specific inhibitor), Akt inhibitor VIII, and PP242 (an mTORC1/2 inhibitor), but not by rapamycin (an mTORC1 inhibitor). PP242 184-189 ATPase, H+ transporting, lysosomal V0 subunit D2 Mus musculus 130-138 32990653-7 2020 Results: V-ATPase activity in PTs was markedly enhanced by insulin, and its activation was completely inhibited by bafilomycin (a V-ATPase-specific inhibitor), Akt inhibitor VIII, and PP242 (an mTORC1/2 inhibitor), but not by rapamycin (an mTORC1 inhibitor). PP242 184-189 CREB regulated transcription coactivator 2 Mus musculus 194-202 32990653-7 2020 Results: V-ATPase activity in PTs was markedly enhanced by insulin, and its activation was completely inhibited by bafilomycin (a V-ATPase-specific inhibitor), Akt inhibitor VIII, and PP242 (an mTORC1/2 inhibitor), but not by rapamycin (an mTORC1 inhibitor). PP242 184-189 CREB regulated transcription coactivator 1 Mus musculus 194-200 32990653-9 2020 PP242 completely suppressed the insulin-mediated V-ATPase stimulation in mouse PTs, whereas rapamycin failed to influence the effect of insulin. PP242 0-5 ATPase, H+ transporting, lysosomal V0 subunit D2 Mus musculus 49-57 32990653-10 2020 Insulin-induced Akt phosphorylation in the mouse renal cortex was completely suppressed by Akt1/2 inhibitor VIII and PP242, but not by rapamycin. PP242 117-122 thymoma viral proto-oncogene 1 Mus musculus 16-19 32642408-4 2020 Furthermore, we found that mTORC1/ mTORC2 inhibitor PP242 exhibited more efficacious anti-proliferative effect on ESCC cells than mTORC1 inhibitor RAD001 due to RAD001-triggered feedback activation of AKT signal. PP242 52-57 CREB regulated transcription coactivator 1 Mus musculus 27-33 32512069-11 2020 The mTOR inhibitor PP242 ameliorated Cu(II)-impaired TFEB expression, lysosomal biogenesis, autophagic flux, and Abetao clearance in microglia. PP242 19-24 mechanistic target of rapamycin kinase Homo sapiens 4-8 32512069-11 2020 The mTOR inhibitor PP242 ameliorated Cu(II)-impaired TFEB expression, lysosomal biogenesis, autophagic flux, and Abetao clearance in microglia. PP242 19-24 transcription factor EB Homo sapiens 53-57 32642408-4 2020 Furthermore, we found that mTORC1/ mTORC2 inhibitor PP242 exhibited more efficacious anti-proliferative effect on ESCC cells than mTORC1 inhibitor RAD001 due to RAD001-triggered feedback activation of AKT signal. PP242 52-57 CREB regulated transcription coactivator 2 Mus musculus 35-41 32642408-4 2020 Furthermore, we found that mTORC1/ mTORC2 inhibitor PP242 exhibited more efficacious anti-proliferative effect on ESCC cells than mTORC1 inhibitor RAD001 due to RAD001-triggered feedback activation of AKT signal. PP242 52-57 AKT serine/threonine kinase 1 Homo sapiens 201-204 32642408-6 2020 Noteworthy, knocking-down stably RICTOR significantly suppresses RAD001-induced feedback activation of AKT/PRAS40 signaling, and enhances inhibition efficacy of PP242 on the phosphorylation of AKT and PRAS40, thus potentiates the antitumor effect of RAD001 and PP242 both in vitro and in vivo. PP242 161-166 RPTOR independent companion of MTOR complex 2 Homo sapiens 33-39 32642408-6 2020 Noteworthy, knocking-down stably RICTOR significantly suppresses RAD001-induced feedback activation of AKT/PRAS40 signaling, and enhances inhibition efficacy of PP242 on the phosphorylation of AKT and PRAS40, thus potentiates the antitumor effect of RAD001 and PP242 both in vitro and in vivo. PP242 161-166 AKT serine/threonine kinase 1 Homo sapiens 193-196 32642408-6 2020 Noteworthy, knocking-down stably RICTOR significantly suppresses RAD001-induced feedback activation of AKT/PRAS40 signaling, and enhances inhibition efficacy of PP242 on the phosphorylation of AKT and PRAS40, thus potentiates the antitumor effect of RAD001 and PP242 both in vitro and in vivo. PP242 161-166 AKT1 substrate 1 Homo sapiens 201-207 32642408-6 2020 Noteworthy, knocking-down stably RICTOR significantly suppresses RAD001-induced feedback activation of AKT/PRAS40 signaling, and enhances inhibition efficacy of PP242 on the phosphorylation of AKT and PRAS40, thus potentiates the antitumor effect of RAD001 and PP242 both in vitro and in vivo. PP242 261-266 RPTOR independent companion of MTOR complex 2 Homo sapiens 33-39 31732667-2 2019 Here we demonstrate that dual mTORC1/mTORC2 inhibitors OSI-027 and PP242 cause catastrophic macropinocytosis in rhabdomyosarcoma (RMS) cells and cancers of the skin, breast, lung, and cervix, whereas the effects are much less pronounced in immortalized human keratinocytes. PP242 67-72 CREB regulated transcription coactivator 1 Mus musculus 30-36 32062191-7 2020 Interestingly, PP242 (mTORC1/2 inhibitor) or Akt inhibitor X, like rapamycin (mTORC1 inhibitor), reduced the basal or hsBAFF-induced [Ca2+]i elevations. PP242 15-20 CREB regulated transcription coactivator 1 Mus musculus 22-28 31806641-3 2020 Here, we tested three distinct mTOR kinase inhibitors (TORKi) PP242, KU-0063794, and sapanisertib against glioblastoma cells. PP242 62-67 mechanistic target of rapamycin kinase Homo sapiens 31-35 31806641-5 2020 Apoptosis induced by PP242 resulted from off-target cooperative inhibition of JAK2 and protein kinase C alpha (PKCalpha). PP242 21-26 Janus kinase 2 Homo sapiens 78-82 31806641-5 2020 Apoptosis induced by PP242 resulted from off-target cooperative inhibition of JAK2 and protein kinase C alpha (PKCalpha). PP242 21-26 protein kinase C alpha Homo sapiens 87-109 31806641-5 2020 Apoptosis induced by PP242 resulted from off-target cooperative inhibition of JAK2 and protein kinase C alpha (PKCalpha). PP242 21-26 protein kinase C alpha Homo sapiens 111-119 31732667-2 2019 Here we demonstrate that dual mTORC1/mTORC2 inhibitors OSI-027 and PP242 cause catastrophic macropinocytosis in rhabdomyosarcoma (RMS) cells and cancers of the skin, breast, lung, and cervix, whereas the effects are much less pronounced in immortalized human keratinocytes. PP242 67-72 CREB regulated transcription coactivator 2 Mus musculus 37-43 30993706-10 2019 In addition, PP242, an mTOR inhibitor, induced mRNA expression of Muc1, miRNA200a, and miRNa223-3p whereas it declined the expression of LIF. PP242 13-18 mechanistic target of rapamycin kinase Homo sapiens 23-27 31771139-8 2019 Treatment with pan-mTOR inhibitor PP242 diminishes DNA damage-induced gammaH2AX and BRCA1 foci formation. PP242 34-39 mechanistic target of rapamycin kinase Homo sapiens 19-23 31771139-8 2019 Treatment with pan-mTOR inhibitor PP242 diminishes DNA damage-induced gammaH2AX and BRCA1 foci formation. PP242 34-39 BRCA1 DNA repair associated Homo sapiens 84-89 30968418-11 2019 The PP242-treated group demonstrated a significant rise in the expression of MUC1, miRNA 223-3p and a remarkable decline in ERK1/2 and p-4E-BP1 levels in comparison with the control group. PP242 4-9 mucin 1, transmembrane Mus musculus 77-81 30968418-11 2019 The PP242-treated group demonstrated a significant rise in the expression of MUC1, miRNA 223-3p and a remarkable decline in ERK1/2 and p-4E-BP1 levels in comparison with the control group. PP242 4-9 mitogen-activated protein kinase 3 Mus musculus 124-130 30993706-10 2019 In addition, PP242, an mTOR inhibitor, induced mRNA expression of Muc1, miRNA200a, and miRNa223-3p whereas it declined the expression of LIF. PP242 13-18 mucin 1, transmembrane Mus musculus 66-70 30968418-11 2019 The PP242-treated group demonstrated a significant rise in the expression of MUC1, miRNA 223-3p and a remarkable decline in ERK1/2 and p-4E-BP1 levels in comparison with the control group. PP242 4-9 eukaryotic translation initiation factor 4E binding protein 1 Homo sapiens 137-143 30993706-10 2019 In addition, PP242, an mTOR inhibitor, induced mRNA expression of Muc1, miRNA200a, and miRNa223-3p whereas it declined the expression of LIF. PP242 13-18 leukemia inhibitory factor Mus musculus 137-140 30968418-12 2019 Combination therapy of (FCA+PP242) resulted in a remarkable rise in LIF, Msx-1, HB-EGF, ERK1/2, and mTOR levels, in comparison with the PP242 group. PP242 28-33 leukemia inhibitory factor Mus musculus 68-71 30993706-11 2019 Moreover, activity of the ERK1/2-mTOR pathway in the endometrial cells was deterred by dexamethasone and PP242. PP242 105-110 mitogen-activated protein kinase 3 Homo sapiens 26-32 30993706-11 2019 Moreover, activity of the ERK1/2-mTOR pathway in the endometrial cells was deterred by dexamethasone and PP242. PP242 105-110 mechanistic target of rapamycin kinase Homo sapiens 33-37 30968418-12 2019 Combination therapy of (FCA+PP242) resulted in a remarkable rise in LIF, Msx-1, HB-EGF, ERK1/2, and mTOR levels, in comparison with the PP242 group. PP242 28-33 msh homeobox 1 Mus musculus 73-78 31065010-5 2019 Torin, PP242, and a PKCzeta inhibitory peptide, but not rapamycin, prevented these biliverdin-induced responses and TLR4 inhibition. PP242 7-12 toll like receptor 4 Homo sapiens 116-120 30968418-12 2019 Combination therapy of (FCA+PP242) resulted in a remarkable rise in LIF, Msx-1, HB-EGF, ERK1/2, and mTOR levels, in comparison with the PP242 group. PP242 28-33 heparin-binding EGF-like growth factor Mus musculus 80-86 30968418-12 2019 Combination therapy of (FCA+PP242) resulted in a remarkable rise in LIF, Msx-1, HB-EGF, ERK1/2, and mTOR levels, in comparison with the PP242 group. PP242 28-33 mitogen-activated protein kinase 3 Mus musculus 88-94 30968418-12 2019 Combination therapy of (FCA+PP242) resulted in a remarkable rise in LIF, Msx-1, HB-EGF, ERK1/2, and mTOR levels, in comparison with the PP242 group. PP242 28-33 mechanistic target of rapamycin kinase Mus musculus 100-104 30968418-13 2019 Furthermore, combination therapy of (FCA+PP242) downregulated the expression of MUC1 in comparison with the PP242-treated group. PP242 41-46 mucin 1, transmembrane Mus musculus 80-84 30968418-13 2019 Furthermore, combination therapy of (FCA+PP242) downregulated the expression of MUC1 in comparison with the PP242-treated group. PP242 108-113 mucin 1, transmembrane Mus musculus 80-84 31473880-10 2019 The PRMT5 inhibitor EPZ015666 displayed synergistic anti-GBM effects in vitro and in a xenograft mouse model in combination with PP242. PP242 129-134 protein arginine N-methyltransferase 5 Mus musculus 4-9 31081172-12 2019 However, the administration of mTORC1/2 inhibitor PP242 could recover the phosphorylation of S6K1, which suggested that mTORC2 was involved in the regulation of mTORC1 activity. PP242 50-55 CREB regulated transcription coactivator 1 Mus musculus 31-37 31081172-12 2019 However, the administration of mTORC1/2 inhibitor PP242 could recover the phosphorylation of S6K1, which suggested that mTORC2 was involved in the regulation of mTORC1 activity. PP242 50-55 ribosomal protein S6 kinase B1 Homo sapiens 93-97 31081172-12 2019 However, the administration of mTORC1/2 inhibitor PP242 could recover the phosphorylation of S6K1, which suggested that mTORC2 was involved in the regulation of mTORC1 activity. PP242 50-55 CREB regulated transcription coactivator 2 Mus musculus 120-126 31081172-12 2019 However, the administration of mTORC1/2 inhibitor PP242 could recover the phosphorylation of S6K1, which suggested that mTORC2 was involved in the regulation of mTORC1 activity. PP242 50-55 CREB regulated transcription coactivator 1 Mus musculus 161-167 30300823-3 2018 In this study, we investigated whether an mTORC1/2 kinase inhibitor, PP242, which was reported to activate lysosomal function, potentiates the cytotoxicity of GO in AML cells. PP242 69-74 CREB regulated transcription coactivator 1 Mus musculus 42-48 30075169-5 2019 Pre-incubation of DR slices with the mTOR inhibitor PP242 decreased the frequency of sEPSCs and prevented the effect of ketamine. PP242 52-57 mechanistic target of rapamycin kinase Homo sapiens 37-41 30482887-7 2018 The pp242-treated cells survive due to formation of the non-autophagous LC3-negative vacuoles, which contain the damaged mitochondria and lysosomes with the following excretion the content from the cell. PP242 4-9 microtubule associated protein 1 light chain 3 alpha Homo sapiens 72-75 30346178-2 2018 By reference to the crystal structure of mTOR-PP242, we explored to discover potential ATP-competitive inhibitors of mTOR. PP242 46-51 mechanistic target of rapamycin kinase Homo sapiens 41-45 30346178-2 2018 By reference to the crystal structure of mTOR-PP242, we explored to discover potential ATP-competitive inhibitors of mTOR. PP242 46-51 mechanistic target of rapamycin kinase Homo sapiens 117-121 30300823-7 2018 LysoTracker fluorescence was dramatically increased by treatment with PP242 in U937, THP-1 and SKM-1 cells, and the intensified fluorescence was retained with PP242 + GO. PP242 70-75 GLI family zinc finger 2 Homo sapiens 85-90 30300823-7 2018 LysoTracker fluorescence was dramatically increased by treatment with PP242 in U937, THP-1 and SKM-1 cells, and the intensified fluorescence was retained with PP242 + GO. PP242 70-75 sodium voltage-gated channel alpha subunit 4 Homo sapiens 95-100 30300823-10 2018 Further, PP242 suppressed GO-induced Chk1 activation and G2/M cell cycle arrest, which in turn triggered cell cycle promotion and cell death. PP242 9-14 checkpoint kinase 1 Homo sapiens 37-41 30300823-11 2018 These results indicate that inhibition of mTORC1/2 kinase by PP242 enhanced the cytotoxicity of GO by increasing lysosomal compartments and promoting the cell cycle via suppression of GO-induced Chk1 activation. PP242 61-66 CREB regulated transcription coactivator 1 Mus musculus 42-48 30300823-11 2018 These results indicate that inhibition of mTORC1/2 kinase by PP242 enhanced the cytotoxicity of GO by increasing lysosomal compartments and promoting the cell cycle via suppression of GO-induced Chk1 activation. PP242 61-66 checkpoint kinase 1 Homo sapiens 195-199 30356017-1 2018 We previously reported that PP242 (dual inhibitor of mTORC1/2) plus curcumin induced apoptotic cell death through lysosomal membrane permeabilization (LMP)-mediated autophagy. PP242 28-33 CREB regulated transcription coactivator 2 Mus musculus 53-61 30356017-6 2018 Furthermore, overexpression of HSP70 significantly inhibited PP242 plus curcumin-induced LMP and apoptosis, but the protective effect was abolished by K77R mutation of acetylation site of HSP70. PP242 61-66 heat shock protein family A (Hsp70) member 4 Homo sapiens 31-36 30356017-6 2018 Furthermore, overexpression of HSP70 significantly inhibited PP242 plus curcumin-induced LMP and apoptosis, but the protective effect was abolished by K77R mutation of acetylation site of HSP70. PP242 61-66 heat shock protein family A (Hsp70) member 4 Homo sapiens 188-193 30356017-7 2018 Taken together, our results reveal that regulation of HSP70 through K77 acetylation plays role in combined PP242 and curcumin treatment-induced apoptosis. PP242 107-112 heat shock protein family A (Hsp70) member 4 Homo sapiens 54-59 30356017-7 2018 Taken together, our results reveal that regulation of HSP70 through K77 acetylation plays role in combined PP242 and curcumin treatment-induced apoptosis. PP242 107-112 keratin 77 Homo sapiens 68-71 30154246-6 2018 Overexpression of constitutively active Taz (Taz-S89A) could restore fibroblast activation suppressed by PP242, an mTOR kinase inhibitor in NRK-49F cells. PP242 105-110 tafazzin, phospholipid-lysophospholipid transacylase Rattus norvegicus 40-43 29849119-3 2018 However, PP242 (inhibitor of mTORC1 and mTORC2) alone did not induce human renal carcinoma cell death. PP242 9-14 CREB regulated transcription coactivator 1 Mus musculus 29-35 29849119-6 2018 Furthermore, co-treatment with PP242 and curcumin-induced the downregulation of the Rictor (an mTORC2 complex protein) and Akt protein levels, and ectopic overexpression of Rictor or Akt inhibited PP242 plus curcumin induced cell death. PP242 31-36 RPTOR independent companion of MTOR complex 2 Homo sapiens 84-90 29849119-6 2018 Furthermore, co-treatment with PP242 and curcumin-induced the downregulation of the Rictor (an mTORC2 complex protein) and Akt protein levels, and ectopic overexpression of Rictor or Akt inhibited PP242 plus curcumin induced cell death. PP242 31-36 CREB regulated transcription coactivator 2 Mus musculus 95-101 29849119-6 2018 Furthermore, co-treatment with PP242 and curcumin-induced the downregulation of the Rictor (an mTORC2 complex protein) and Akt protein levels, and ectopic overexpression of Rictor or Akt inhibited PP242 plus curcumin induced cell death. PP242 31-36 AKT serine/threonine kinase 1 Homo sapiens 123-126 29849119-6 2018 Furthermore, co-treatment with PP242 and curcumin-induced the downregulation of the Rictor (an mTORC2 complex protein) and Akt protein levels, and ectopic overexpression of Rictor or Akt inhibited PP242 plus curcumin induced cell death. PP242 31-36 RPTOR independent companion of MTOR complex 2 Homo sapiens 173-179 29849119-6 2018 Furthermore, co-treatment with PP242 and curcumin-induced the downregulation of the Rictor (an mTORC2 complex protein) and Akt protein levels, and ectopic overexpression of Rictor or Akt inhibited PP242 plus curcumin induced cell death. PP242 31-36 AKT serine/threonine kinase 1 Homo sapiens 183-186 29849119-11 2018 Altogether, our results reveal that combined PP242 and curcumin treatment could induce autophagy-mediated cell death by reducing the expression of Rictor and Akt in renal carcinoma cells. PP242 45-50 RPTOR independent companion of MTOR complex 2 Homo sapiens 147-153 29849119-11 2018 Altogether, our results reveal that combined PP242 and curcumin treatment could induce autophagy-mediated cell death by reducing the expression of Rictor and Akt in renal carcinoma cells. PP242 45-50 AKT serine/threonine kinase 1 Homo sapiens 158-161 30131696-9 2018 The disruption on mTORC2/AKT could be reversed by mTORC2 inducer insulin and promoted by mTORC2 inhibitor PP242. PP242 106-111 CREB regulated transcription coactivator 2 Mus musculus 18-24 29755672-7 2018 Specific inhibition of mTOR activity through siRNA targeting RICTOR and dual mTOR inhibitor PP242 reduced the MM-ECs angiogenic functions, including cell migration, chemotaxis, adhesion, invasion, in vitro angiogenesis on Matrigel , and cytoskeleton reorganization. PP242 92-97 mechanistic target of rapamycin kinase Homo sapiens 23-27 29755672-7 2018 Specific inhibition of mTOR activity through siRNA targeting RICTOR and dual mTOR inhibitor PP242 reduced the MM-ECs angiogenic functions, including cell migration, chemotaxis, adhesion, invasion, in vitro angiogenesis on Matrigel , and cytoskeleton reorganization. PP242 92-97 mechanistic target of rapamycin kinase Homo sapiens 77-81 29755672-9 2018 PP242 exhibited a synergistic effect with lenalidomide and bortezomib, suggesting that mTOR inhibition can enhance the anti-angiogenic effect of these drugs. PP242 0-5 mechanistic target of rapamycin kinase Homo sapiens 87-91 29755672-10 2018 Data to be shown indicate that mTORC2 is involved in MM angiogenesis, and suggest that the dual mTOR inhibitor PP242 may be useful for the anti-angiogenic management of MM patients. PP242 111-116 CREB regulated transcription coactivator 2 Mus musculus 31-37 29755672-10 2018 Data to be shown indicate that mTORC2 is involved in MM angiogenesis, and suggest that the dual mTOR inhibitor PP242 may be useful for the anti-angiogenic management of MM patients. PP242 111-116 mechanistic target of rapamycin kinase Homo sapiens 31-35 29692710-0 2018 PP242 Counteracts Glioblastoma Cell Proliferation, Migration, Invasiveness and Stemness Properties by Inhibiting mTORC2/AKT. PP242 0-5 CREB regulated transcription coactivator 2 Mus musculus 113-119 29692710-0 2018 PP242 Counteracts Glioblastoma Cell Proliferation, Migration, Invasiveness and Stemness Properties by Inhibiting mTORC2/AKT. PP242 0-5 AKT serine/threonine kinase 1 Homo sapiens 120-123 29692710-9 2018 In this context, we demonstrate that the novel ATP-competitive mTOR inhibitor PP242 effectively targets both mTORC1 and mTORC2 activation and counteracts cell proliferation via the induction of high autophagy levels, besides reducing cell migration, invasiveness and stemness properties. PP242 78-83 mechanistic target of rapamycin kinase Homo sapiens 63-67 29692710-9 2018 In this context, we demonstrate that the novel ATP-competitive mTOR inhibitor PP242 effectively targets both mTORC1 and mTORC2 activation and counteracts cell proliferation via the induction of high autophagy levels, besides reducing cell migration, invasiveness and stemness properties. PP242 78-83 CREB regulated transcription coactivator 1 Mus musculus 109-115 29692710-9 2018 In this context, we demonstrate that the novel ATP-competitive mTOR inhibitor PP242 effectively targets both mTORC1 and mTORC2 activation and counteracts cell proliferation via the induction of high autophagy levels, besides reducing cell migration, invasiveness and stemness properties. PP242 78-83 CREB regulated transcription coactivator 2 Mus musculus 120-126 30154246-6 2018 Overexpression of constitutively active Taz (Taz-S89A) could restore fibroblast activation suppressed by PP242, an mTOR kinase inhibitor in NRK-49F cells. PP242 105-110 tafazzin, phospholipid-lysophospholipid transacylase Rattus norvegicus 45-49 30154246-6 2018 Overexpression of constitutively active Taz (Taz-S89A) could restore fibroblast activation suppressed by PP242, an mTOR kinase inhibitor in NRK-49F cells. PP242 105-110 mechanistic target of rapamycin kinase Mus musculus 115-119 30154246-8 2018 Ablation of Rictor in fibroblasts/pericytes or blockade of mTOR signaling with PP242 attenuated Yap/Taz activation and UUO nephropathy in mice. PP242 79-84 mechanistic target of rapamycin kinase Mus musculus 59-63 30154246-8 2018 Ablation of Rictor in fibroblasts/pericytes or blockade of mTOR signaling with PP242 attenuated Yap/Taz activation and UUO nephropathy in mice. PP242 79-84 yes-associated protein 1 Mus musculus 96-99 30154246-8 2018 Ablation of Rictor in fibroblasts/pericytes or blockade of mTOR signaling with PP242 attenuated Yap/Taz activation and UUO nephropathy in mice. PP242 79-84 tafazzin, phospholipid-lysophospholipid transacylase Mus musculus 100-103 29080085-8 2018 In the present study, we report using pp242 which is a dual mTORC1/C2 blocker in cellular model of tauopathy using LUHMES cell line. PP242 38-43 CREB regulated transcription coactivator 1 Mus musculus 60-66 29080085-12 2018 The present study suggests the possible use of pp242 as a dual mTOR blocker to treat tauopathy. PP242 47-52 mechanistic target of rapamycin kinase Homo sapiens 63-67 29195143-1 2018 PP242 is a second generation novel selective ATP-competitive inhibitor of mTOR that displayed promising anti-cancer activity over several cancer types by inhibiting both the complexes of mTOR (mTORC1 and mTORC2). PP242 0-5 CREB regulated transcription coactivator 1 Mus musculus 193-199 29344639-2 2018 In the present study, the potency of PP242, a novel dual inhibitor of mTOR complex 1/2 (mTORC1/2), in the suppression of the growth of human lens epithelial cells (HLECs) was investigated. PP242 37-42 mechanistic target of rapamycin kinase Homo sapiens 70-74 29344639-2 2018 In the present study, the potency of PP242, a novel dual inhibitor of mTOR complex 1/2 (mTORC1/2), in the suppression of the growth of human lens epithelial cells (HLECs) was investigated. PP242 37-42 CREB regulated transcription coactivator 2 Mus musculus 88-96 29344639-4 2018 In addition, western blot analysis indicated that PP242 completely inhibited mTORC1 and mTORC2 downstream signaling activities, whereas rapamycin only partially inhibited mTORC1 activity within LECs. PP242 50-55 CREB regulated transcription coactivator 1 Mus musculus 77-83 29344639-4 2018 In addition, western blot analysis indicated that PP242 completely inhibited mTORC1 and mTORC2 downstream signaling activities, whereas rapamycin only partially inhibited mTORC1 activity within LECs. PP242 50-55 CREB regulated transcription coactivator 2 Mus musculus 88-94 29195143-1 2018 PP242 is a second generation novel selective ATP-competitive inhibitor of mTOR that displayed promising anti-cancer activity over several cancer types by inhibiting both the complexes of mTOR (mTORC1 and mTORC2). PP242 0-5 CREB regulated transcription coactivator 2 Mus musculus 204-210 29154199-6 2018 Importantly, UVB treatment perturbs the conversion of microtubule-associated protein 1 light chain 3 (LC3)-I to LC3-II and LC3-II turnover in response to treatment with MTOR inhibitors (Torin 1 and pp242), as well as endoplasmic reticular stress (A23187 and tunicamycin), inositol pathway (L690,330) and autophagy inducers (resveratrol and STF62247). PP242 198-203 microtubule associated protein 1 light chain 3 alpha Homo sapiens 102-105 29154199-6 2018 Importantly, UVB treatment perturbs the conversion of microtubule-associated protein 1 light chain 3 (LC3)-I to LC3-II and LC3-II turnover in response to treatment with MTOR inhibitors (Torin 1 and pp242), as well as endoplasmic reticular stress (A23187 and tunicamycin), inositol pathway (L690,330) and autophagy inducers (resveratrol and STF62247). PP242 198-203 microtubule associated protein 1 light chain 3 alpha Homo sapiens 112-115 29154199-6 2018 Importantly, UVB treatment perturbs the conversion of microtubule-associated protein 1 light chain 3 (LC3)-I to LC3-II and LC3-II turnover in response to treatment with MTOR inhibitors (Torin 1 and pp242), as well as endoplasmic reticular stress (A23187 and tunicamycin), inositol pathway (L690,330) and autophagy inducers (resveratrol and STF62247). PP242 198-203 microtubule associated protein 1 light chain 3 alpha Homo sapiens 112-115 29154199-6 2018 Importantly, UVB treatment perturbs the conversion of microtubule-associated protein 1 light chain 3 (LC3)-I to LC3-II and LC3-II turnover in response to treatment with MTOR inhibitors (Torin 1 and pp242), as well as endoplasmic reticular stress (A23187 and tunicamycin), inositol pathway (L690,330) and autophagy inducers (resveratrol and STF62247). PP242 198-203 mechanistic target of rapamycin kinase Homo sapiens 169-173 28679058-5 2017 Treatment with mTOR kinase inhibitor, PP242, at Weeks 6-8 after PH induction suppressed both mTORC1 and mTORC2 in small PAs, but only mTORC1 signaling in RV, preserving basal mTORC2-Akt levels. PP242 38-43 mechanistic target of rapamycin kinase Rattus norvegicus 15-19 28679058-5 2017 Treatment with mTOR kinase inhibitor, PP242, at Weeks 6-8 after PH induction suppressed both mTORC1 and mTORC2 in small PAs, but only mTORC1 signaling in RV, preserving basal mTORC2-Akt levels. PP242 38-43 CREB regulated transcription coactivator 1 Mus musculus 93-99 28679058-5 2017 Treatment with mTOR kinase inhibitor, PP242, at Weeks 6-8 after PH induction suppressed both mTORC1 and mTORC2 in small PAs, but only mTORC1 signaling in RV, preserving basal mTORC2-Akt levels. PP242 38-43 CREB regulated transcription coactivator 2 Mus musculus 104-110 28679058-5 2017 Treatment with mTOR kinase inhibitor, PP242, at Weeks 6-8 after PH induction suppressed both mTORC1 and mTORC2 in small PAs, but only mTORC1 signaling in RV, preserving basal mTORC2-Akt levels. PP242 38-43 CREB regulated transcription coactivator 1 Mus musculus 134-140 28679058-5 2017 Treatment with mTOR kinase inhibitor, PP242, at Weeks 6-8 after PH induction suppressed both mTORC1 and mTORC2 in small PAs, but only mTORC1 signaling in RV, preserving basal mTORC2-Akt levels. PP242 38-43 CREB regulated transcription coactivator 2 Mus musculus 175-181 28679058-5 2017 Treatment with mTOR kinase inhibitor, PP242, at Weeks 6-8 after PH induction suppressed both mTORC1 and mTORC2 in small PAs, but only mTORC1 signaling in RV, preserving basal mTORC2-Akt levels. PP242 38-43 AKT serine/threonine kinase 1 Rattus norvegicus 182-185 28671713-9 2017 The functional polarization process triggered by ATP-P2X/Y-purinoceptor interaction was also involved in the C5a-induced shape changes, because pretreatment with suramin blocked not only the shape changes but also the subsequent C5a-dependent chemotactic activity. PP242 53-56 complement C5a receptor 1 Homo sapiens 109-112 28300280-5 2018 Also, PP242, an mTORC1/2 kinase inhibitor, repressed survivin expression, and cell proliferation/viability more potently than rapamycin (mTORC1 inhibitor) in B cells in response to hsBAFF. PP242 6-11 CREB regulated transcription coactivator 1 Mus musculus 16-22 28671713-9 2017 The functional polarization process triggered by ATP-P2X/Y-purinoceptor interaction was also involved in the C5a-induced shape changes, because pretreatment with suramin blocked not only the shape changes but also the subsequent C5a-dependent chemotactic activity. PP242 53-56 complement C5a receptor 1 Homo sapiens 229-232 28402933-0 2017 PDK1 inhibitor GSK2334470 exerts antitumor activity in multiple myeloma and forms a novel multitargeted combination with dual mTORC1/C2 inhibitor PP242. PP242 146-151 pyruvate dehydrogenase kinase 1 Homo sapiens 0-4 28402933-9 2017 Combining PP242, a dual mTORC1/C2 inhibitor, with GSK-470, had greater antimyeloma activity than either one alone in vitro and in MM xenograft model established in immunodeficient mice. PP242 10-15 CREB regulated transcription coactivator 1 Mus musculus 24-30 28442344-9 2017 Likewise, inhibiting the PI3K-AKT-mTOR pathway with the ATP-competitive mTOR inhibitor PP242 reduced CD44 protein in SNU-423 and SNU-449 cells without altering CD44 mRNA levels. PP242 87-92 mechanistic target of rapamycin kinase Homo sapiens 34-38 28442344-9 2017 Likewise, inhibiting the PI3K-AKT-mTOR pathway with the ATP-competitive mTOR inhibitor PP242 reduced CD44 protein in SNU-423 and SNU-449 cells without altering CD44 mRNA levels. PP242 87-92 mechanistic target of rapamycin kinase Homo sapiens 72-76 28442344-9 2017 Likewise, inhibiting the PI3K-AKT-mTOR pathway with the ATP-competitive mTOR inhibitor PP242 reduced CD44 protein in SNU-423 and SNU-449 cells without altering CD44 mRNA levels. PP242 87-92 CD44 molecule (Indian blood group) Homo sapiens 101-105 28592067-1 2017 Objective: To establish the acute myeloid leukemia (AML) mouse model, and to preliminarily investigate the efficiency of dasatinib, a tryosine kinase inhibitor, and PP242, an inhibitor of PI3K/Akt/mTOR signaling pathway in the development of AML. PP242 165-170 thymoma viral proto-oncogene 1 Mus musculus 193-196 28592067-11 2017 Conclusion: Combination of tryosine kinase inhibitor-dasatinib and PI3K/Akt/mTOR signaling pathway inhibitor- PP242 could delay the progression of AML by inducing more leukemia to apoptosis and arrest more leukemia cells in the cell cycle G0 phase, it may be provied a new method for clinical therapy. PP242 110-115 thymoma viral proto-oncogene 1 Mus musculus 72-75 28592067-11 2017 Conclusion: Combination of tryosine kinase inhibitor-dasatinib and PI3K/Akt/mTOR signaling pathway inhibitor- PP242 could delay the progression of AML by inducing more leukemia to apoptosis and arrest more leukemia cells in the cell cycle G0 phase, it may be provied a new method for clinical therapy. PP242 110-115 mechanistic target of rapamycin kinase Mus musculus 76-80 28612529-1 2017 OBJECTIVES: To investigate the anti-leukemia effect and mechanism of mTORC1/2 inhibitor PP242 combined with imatinib (IM) on the proliferation of Ph+ acute lymphoblastic leukemia (ALL) cell line SUP-B15. PP242 88-93 CREB regulated transcription coactivator 2 Mus musculus 69-77 28612529-6 2017 CONCLUSION: The combination of IM and PP242 could increase the inhibition of PI3K/Akt/mTOR signaling pathway and apoptosis mediated by bax and caspase-3 in SUP-B15 cell line. PP242 38-43 AKT serine/threonine kinase 1 Homo sapiens 82-85 28612529-6 2017 CONCLUSION: The combination of IM and PP242 could increase the inhibition of PI3K/Akt/mTOR signaling pathway and apoptosis mediated by bax and caspase-3 in SUP-B15 cell line. PP242 38-43 mechanistic target of rapamycin kinase Homo sapiens 86-90 28612529-6 2017 CONCLUSION: The combination of IM and PP242 could increase the inhibition of PI3K/Akt/mTOR signaling pathway and apoptosis mediated by bax and caspase-3 in SUP-B15 cell line. PP242 38-43 BCL2 associated X, apoptosis regulator Homo sapiens 135-138 28612529-6 2017 CONCLUSION: The combination of IM and PP242 could increase the inhibition of PI3K/Akt/mTOR signaling pathway and apoptosis mediated by bax and caspase-3 in SUP-B15 cell line. PP242 38-43 caspase 3 Homo sapiens 143-152 28106723-7 2017 Moreover, both qualitative and quantitative method confirmed the increase of lysosomal pH, and mammalian target of rapamycin (mTOR) inhibitor PP242 treatment relieved this elevation. PP242 142-147 mechanistic target of rapamycin kinase Homo sapiens 95-124 28106723-7 2017 Moreover, both qualitative and quantitative method confirmed the increase of lysosomal pH, and mammalian target of rapamycin (mTOR) inhibitor PP242 treatment relieved this elevation. PP242 142-147 mechanistic target of rapamycin kinase Homo sapiens 126-130 28106723-8 2017 Moreover, PP242 treatment also alleviated the change of autophagy flux, TER, and claudin-2 expression induced by TNF-alpha. PP242 10-15 claudin 2 Homo sapiens 81-90 28106723-8 2017 Moreover, PP242 treatment also alleviated the change of autophagy flux, TER, and claudin-2 expression induced by TNF-alpha. PP242 10-15 tumor necrosis factor Homo sapiens 113-122 28400912-9 2017 Finally, MTOR inhibition by Rapamycin, everolimus, or pp242 did not affect the series of biological events in keratinocytes exposed to UVB, including the downregulation of BiP and PERK, activation of Histone H2A and JNK, and cleavage of caspase-3 and PARP. PP242 54-59 mechanistic target of rapamycin kinase Homo sapiens 9-13 27566137-7 2016 Treatment with rapamycin and PP242, that target the PI3K/AKT/mTOR signaling pathway, modified starvation-induced autophagy and apoptosis in IPF fibroblasts. PP242 29-34 AKT serine/threonine kinase 1 Homo sapiens 57-60 27566137-7 2016 Treatment with rapamycin and PP242, that target the PI3K/AKT/mTOR signaling pathway, modified starvation-induced autophagy and apoptosis in IPF fibroblasts. PP242 29-34 mechanistic target of rapamycin kinase Homo sapiens 61-65 26891668-7 2016 In addition, PP242, a mammalian target rapamycin (mTOR) inhibitor, was used to study the involvement of the mTOR pathway in DADS-induced apoptosis and autophagy. PP242 13-18 mechanistic target of rapamycin kinase Homo sapiens 50-54 26894601-3 2016 However, ovarian cancer cells are resistant to PP242, a dual inhibitor of mTORC1 and mTORC2. PP242 47-52 CREB regulated transcription coactivator 1 Mus musculus 74-80 26894601-3 2016 However, ovarian cancer cells are resistant to PP242, a dual inhibitor of mTORC1 and mTORC2. PP242 47-52 CREB regulated transcription coactivator 2 Mus musculus 85-91 26894601-4 2016 Interestingly, blockage of GLS1 with a selective inhibitor, CB839, or siRNA dramatically sensitized the PP242-induced cell death, as evident from increased PARP cleavage. PP242 104-109 glutaminase Homo sapiens 27-31 26894601-4 2016 Interestingly, blockage of GLS1 with a selective inhibitor, CB839, or siRNA dramatically sensitized the PP242-induced cell death, as evident from increased PARP cleavage. PP242 104-109 collagen type XI alpha 2 chain Homo sapiens 156-160 26894601-5 2016 The anti-cancer activity of CB-839 and PP242 was abrogated by the addition of the TCA cycle product alpha-ketoglutarate, indicating the critical function of GLS1 in ovarian cancer cell survival. PP242 39-44 glutaminase Homo sapiens 157-161 26894601-6 2016 Finally, glutaminolysis inhibition activated apoptosis and synergistically sensitized ovarian cancer cells to priming with the mTOR inhibitor PP242. PP242 142-147 mechanistic target of rapamycin kinase Homo sapiens 127-131 27226604-4 2016 Here we demonstrate that C11 also blocks cyclin D1 IRES-dependent initiation and demonstrates synergistic anti-GBM properties when combined with the mechanistic target of rapamycin kinase inhibitor PP242. PP242 198-203 mechanistic target of rapamycin kinase Mus musculus 149-180 27196780-4 2016 We show that platinum-resistant OVCAR-3 ovarian cancer cells are resensitized to low levels of carboplatin in culture by mTOR inhibition, demonstrating reduced survival after treatment with either mTORC1 inhibitor everolimus or mTORC1/2 inhibitor PP242. PP242 247-252 CREB regulated transcription coactivator 2 Mus musculus 228-236 27358039-2 2016 Here, we report that the dual mTORC1/2 inhibitors PP242 and OSI-027 decreased cell viability but did not induce apoptosis in the non-small cell lung cancer (NSCLC) cell lines H460 and A549. PP242 50-55 CREB regulated transcription coactivator 1 Mus musculus 30-36 27358039-4 2016 JNK was activated by PP242, and PP242-induced autophagy was blocked by inhibiting JNK pathway with SP600125 or JNK siRNA, suggesting that JNK activation is required for the mTORC1/2 inhibitor-mediated induction of autophagy in NSCLC cells. PP242 21-26 mitogen-activated protein kinase 8 Homo sapiens 0-3 27358039-4 2016 JNK was activated by PP242, and PP242-induced autophagy was blocked by inhibiting JNK pathway with SP600125 or JNK siRNA, suggesting that JNK activation is required for the mTORC1/2 inhibitor-mediated induction of autophagy in NSCLC cells. PP242 32-37 mitogen-activated protein kinase 8 Homo sapiens 82-85 27358039-4 2016 JNK was activated by PP242, and PP242-induced autophagy was blocked by inhibiting JNK pathway with SP600125 or JNK siRNA, suggesting that JNK activation is required for the mTORC1/2 inhibitor-mediated induction of autophagy in NSCLC cells. PP242 32-37 mitogen-activated protein kinase 8 Homo sapiens 82-85 27358039-4 2016 JNK was activated by PP242, and PP242-induced autophagy was blocked by inhibiting JNK pathway with SP600125 or JNK siRNA, suggesting that JNK activation is required for the mTORC1/2 inhibitor-mediated induction of autophagy in NSCLC cells. PP242 32-37 mitogen-activated protein kinase 8 Homo sapiens 82-85 27358039-4 2016 JNK was activated by PP242, and PP242-induced autophagy was blocked by inhibiting JNK pathway with SP600125 or JNK siRNA, suggesting that JNK activation is required for the mTORC1/2 inhibitor-mediated induction of autophagy in NSCLC cells. PP242 32-37 CREB regulated transcription coactivator 2 Mus musculus 173-181 26956871-7 2016 Mutated MTOR identified in CNS GCTs upregulated phosphorylation of the AKT pathway proteins including AKT and 4EBP1 in nutrient-deprived conditions and enhanced soft-agar colony formation; both events were suppressed in a dose-dependent manner by addition of the MTOR inhibitor pp242. PP242 278-283 mechanistic target of rapamycin kinase Homo sapiens 8-12 26956871-7 2016 Mutated MTOR identified in CNS GCTs upregulated phosphorylation of the AKT pathway proteins including AKT and 4EBP1 in nutrient-deprived conditions and enhanced soft-agar colony formation; both events were suppressed in a dose-dependent manner by addition of the MTOR inhibitor pp242. PP242 278-283 AKT serine/threonine kinase 1 Homo sapiens 71-74 26956871-7 2016 Mutated MTOR identified in CNS GCTs upregulated phosphorylation of the AKT pathway proteins including AKT and 4EBP1 in nutrient-deprived conditions and enhanced soft-agar colony formation; both events were suppressed in a dose-dependent manner by addition of the MTOR inhibitor pp242. PP242 278-283 AKT serine/threonine kinase 1 Homo sapiens 102-115 26956871-7 2016 Mutated MTOR identified in CNS GCTs upregulated phosphorylation of the AKT pathway proteins including AKT and 4EBP1 in nutrient-deprived conditions and enhanced soft-agar colony formation; both events were suppressed in a dose-dependent manner by addition of the MTOR inhibitor pp242. PP242 278-283 mechanistic target of rapamycin kinase Homo sapiens 263-267 26940200-4 2016 In this study, we demonstrate that mTOR inhibitors-rapamycin (RAP), temisirolimus (TEM), torin-1 (TOR) and PP242 suppress invasion and migration induced by Tumor Necrosis Factor-alpha (TNFalpha) and tumor promoter, Phorbol 12-myristate 13-acetate (PMA) and also reduce the expression of the TNFalpha and IL1beta suggesting their potential to regulate factors in microenvironment that support tumor progression. PP242 107-112 tumor necrosis factor Homo sapiens 156-183 26984042-8 2016 The mTOR inhibitor PP242, metformin, and DMSO reverted EMT to different extent and through different pathways, depending on the cell lines. PP242 19-24 mechanistic target of rapamycin kinase Homo sapiens 4-8 26940200-4 2016 In this study, we demonstrate that mTOR inhibitors-rapamycin (RAP), temisirolimus (TEM), torin-1 (TOR) and PP242 suppress invasion and migration induced by Tumor Necrosis Factor-alpha (TNFalpha) and tumor promoter, Phorbol 12-myristate 13-acetate (PMA) and also reduce the expression of the TNFalpha and IL1beta suggesting their potential to regulate factors in microenvironment that support tumor progression. PP242 107-112 mechanistic target of rapamycin kinase Homo sapiens 35-39 26940200-4 2016 In this study, we demonstrate that mTOR inhibitors-rapamycin (RAP), temisirolimus (TEM), torin-1 (TOR) and PP242 suppress invasion and migration induced by Tumor Necrosis Factor-alpha (TNFalpha) and tumor promoter, Phorbol 12-myristate 13-acetate (PMA) and also reduce the expression of the TNFalpha and IL1beta suggesting their potential to regulate factors in microenvironment that support tumor progression. PP242 107-112 tumor necrosis factor Homo sapiens 185-193 26940200-4 2016 In this study, we demonstrate that mTOR inhibitors-rapamycin (RAP), temisirolimus (TEM), torin-1 (TOR) and PP242 suppress invasion and migration induced by Tumor Necrosis Factor-alpha (TNFalpha) and tumor promoter, Phorbol 12-myristate 13-acetate (PMA) and also reduce the expression of the TNFalpha and IL1beta suggesting their potential to regulate factors in microenvironment that support tumor progression. PP242 107-112 tumor necrosis factor Homo sapiens 291-299 26940200-4 2016 In this study, we demonstrate that mTOR inhibitors-rapamycin (RAP), temisirolimus (TEM), torin-1 (TOR) and PP242 suppress invasion and migration induced by Tumor Necrosis Factor-alpha (TNFalpha) and tumor promoter, Phorbol 12-myristate 13-acetate (PMA) and also reduce the expression of the TNFalpha and IL1beta suggesting their potential to regulate factors in microenvironment that support tumor progression. PP242 107-112 interleukin 1 beta Homo sapiens 304-311 26776341-6 2016 Rapamycin and PP242 inhibit phosphorylation of Akt, ribosomal S6 kinase, 4EBP1 and mTOR. PP242 14-19 AKT serine/threonine kinase 1 Homo sapiens 47-50 26719046-5 2016 Herein, we provide evidence that the combined inhibition of mTORC1/2, using the ATP-competitive binding inhibitor PP242, would effectively suppress GBM growth and dissemination as compared to an allosteric binding inhibitor of mTOR. PP242 114-119 CREB regulated transcription coactivator 2 Mus musculus 60-68 26719046-5 2016 Herein, we provide evidence that the combined inhibition of mTORC1/2, using the ATP-competitive binding inhibitor PP242, would effectively suppress GBM growth and dissemination as compared to an allosteric binding inhibitor of mTOR. PP242 114-119 mechanistic target of rapamycin kinase Homo sapiens 60-64 26719046-6 2016 GBM cells treated with PP242 demonstrated significantly decreased activation of mTORC1 and mTORC2, as shown by reduced phosphorylation of their substrate levels, p70 S6K(Thr389) and AKT(Ser473), respectively, in a dose-dependent manner. PP242 23-28 CREB regulated transcription coactivator 1 Mus musculus 80-86 26719046-6 2016 GBM cells treated with PP242 demonstrated significantly decreased activation of mTORC1 and mTORC2, as shown by reduced phosphorylation of their substrate levels, p70 S6K(Thr389) and AKT(Ser473), respectively, in a dose-dependent manner. PP242 23-28 CREB regulated transcription coactivator 2 Mus musculus 91-97 26719046-6 2016 GBM cells treated with PP242 demonstrated significantly decreased activation of mTORC1 and mTORC2, as shown by reduced phosphorylation of their substrate levels, p70 S6K(Thr389) and AKT(Ser473), respectively, in a dose-dependent manner. PP242 23-28 ubiquitin associated and SH3 domain containing B Homo sapiens 162-165 26719046-7 2016 Furthermore, insulin induced activation of these kinases was abrogated by pretreatment with PP242 as compared with rapamycin. PP242 92-97 insulin Homo sapiens 13-20 26719046-8 2016 Unlike rapamycin, PP242 modestly activates extracellular regulated kinase (ERK1/2), as shown by expression of pERK(Thr202/Tyr204). PP242 18-23 mitogen-activated protein kinase 3 Homo sapiens 75-81 26719046-8 2016 Unlike rapamycin, PP242 modestly activates extracellular regulated kinase (ERK1/2), as shown by expression of pERK(Thr202/Tyr204). PP242 18-23 eukaryotic translation initiation factor 2 alpha kinase 3 Homo sapiens 110-114 26719046-11 2016 In conclusion, these results underscore the potential therapeutic use of the PP242, a novel ATP-competitive binding inhibitor of mTORC1/2 kinase, in suppression of GBM growth and dissemination. PP242 77-82 CREB regulated transcription coactivator 1 Mus musculus 129-135 26163195-5 2016 The mTOR catalytic site inhibitor, PP242, but not mTORC1 inhibitor rapamycin, inhibits ENaC, decreases Na(+) flux in isolated perfused tubules and induces natriuresis in wild-type mice. PP242 35-40 mechanistic target of rapamycin kinase Mus musculus 4-8 26163195-5 2016 The mTOR catalytic site inhibitor, PP242, but not mTORC1 inhibitor rapamycin, inhibits ENaC, decreases Na(+) flux in isolated perfused tubules and induces natriuresis in wild-type mice. PP242 35-40 sodium channel, nonvoltage-gated 1 alpha Mus musculus 87-91 26548560-0 2016 PP242 suppresses bladder cancer cell proliferation and migration through deactivating the mammalian target of rapamycin complex 2/AKT1 signaling pathway. PP242 0-5 AKT serine/threonine kinase 1 Homo sapiens 130-134 26548560-2 2016 The present study assessed the effects of mTORC2 inhibitor PP242 on the proliferation and migration of bladder cancer cells by using Cell Counting Kit-8, 5-ethynyl-2"-deoxyuridine incorporation, wound healing and Transwell assays. PP242 59-64 CREB regulated transcription coactivator 2 Mus musculus 42-48 26548560-6 2016 In addition, PP242 markedly restrained the phosphorylation of AKT1 and mTORC2, while the phosphorylation status of S6K1 and mTORC1 was not affected. PP242 13-18 AKT serine/threonine kinase 1 Homo sapiens 62-66 26548560-6 2016 In addition, PP242 markedly restrained the phosphorylation of AKT1 and mTORC2, while the phosphorylation status of S6K1 and mTORC1 was not affected. PP242 13-18 CREB regulated transcription coactivator 2 Mus musculus 71-77 26548560-7 2016 These results suggested that PP242 exerts potent inhibitory effects on bladder cancer cells by modulating the activity of the mTORC2/AKT1 pathway. PP242 29-34 CREB regulated transcription coactivator 2 Mus musculus 126-132 26548560-7 2016 These results suggested that PP242 exerts potent inhibitory effects on bladder cancer cells by modulating the activity of the mTORC2/AKT1 pathway. PP242 29-34 AKT serine/threonine kinase 1 Homo sapiens 133-137 26776341-6 2016 Rapamycin and PP242 inhibit phosphorylation of Akt, ribosomal S6 kinase, 4EBP1 and mTOR. PP242 14-19 mechanistic target of rapamycin kinase Homo sapiens 83-87 30188618-1 2016 pp242, a TORC1/C2 kinase inhibitor, was used as a trigger of cell autophagy. PP242 0-5 CREB regulated transcription coactivator 1 Rattus norvegicus 9-14 30188621-0 2016 CHLOROQUINE DOES NOT CANCEL E1A+cHa-Ras TRANSFORMANTS" DEATH INDUCED BY mTOR KINASE INHIBITOR pp242. PP242 94-99 mechanistic target of rapamycin kinase Rattus norvegicus 72-76 30188621-2 2016 pp242, a TORC1/C2 kinase inhibitor, was used as a trigger of cell autophagy. PP242 0-5 CREB regulated transcription coactivator 1 Rattus norvegicus 9-14 26636543-0 2015 mTOR kinase inhibitor pp242 causes mitophagy terminated by apoptotic cell death in E1A-Ras transformed cells. PP242 22-27 mechanistic target of rapamycin kinase Homo sapiens 0-4 26636543-6 2015 The ATP-competitive mTORC1/mTORC2 kinase inhibitor pp242 is highly cytotoxic by suppressing the function of mTORC1-4EBP1 axis and mTORC1-dependent phosphorylation of mTORC1 target--ULK1-Ser757 (Atg1). PP242 51-56 CREB regulated transcription coactivator 1 Mus musculus 20-26 26636543-6 2015 The ATP-competitive mTORC1/mTORC2 kinase inhibitor pp242 is highly cytotoxic by suppressing the function of mTORC1-4EBP1 axis and mTORC1-dependent phosphorylation of mTORC1 target--ULK1-Ser757 (Atg1). PP242 51-56 CREB regulated transcription coactivator 2 Mus musculus 27-33 26636543-6 2015 The ATP-competitive mTORC1/mTORC2 kinase inhibitor pp242 is highly cytotoxic by suppressing the function of mTORC1-4EBP1 axis and mTORC1-dependent phosphorylation of mTORC1 target--ULK1-Ser757 (Atg1). PP242 51-56 CREB regulated transcription coactivator 1 Mus musculus 108-114 26636543-6 2015 The ATP-competitive mTORC1/mTORC2 kinase inhibitor pp242 is highly cytotoxic by suppressing the function of mTORC1-4EBP1 axis and mTORC1-dependent phosphorylation of mTORC1 target--ULK1-Ser757 (Atg1). PP242 51-56 CREB regulated transcription coactivator 1 Mus musculus 108-114 26636543-6 2015 The ATP-competitive mTORC1/mTORC2 kinase inhibitor pp242 is highly cytotoxic by suppressing the function of mTORC1-4EBP1 axis and mTORC1-dependent phosphorylation of mTORC1 target--ULK1-Ser757 (Atg1). PP242 51-56 CREB regulated transcription coactivator 1 Mus musculus 108-114 26636543-6 2015 The ATP-competitive mTORC1/mTORC2 kinase inhibitor pp242 is highly cytotoxic by suppressing the function of mTORC1-4EBP1 axis and mTORC1-dependent phosphorylation of mTORC1 target--ULK1-Ser757 (Atg1). PP242 51-56 unc-51 like autophagy activating kinase 1 Homo sapiens 181-185 26636543-6 2015 The ATP-competitive mTORC1/mTORC2 kinase inhibitor pp242 is highly cytotoxic by suppressing the function of mTORC1-4EBP1 axis and mTORC1-dependent phosphorylation of mTORC1 target--ULK1-Ser757 (Atg1). PP242 51-56 unc-51 like autophagy activating kinase 1 Homo sapiens 194-198 26636543-10 2015 According to transmission electron microscopy data, short-term pp242-treated ERas cells exhibit numerous heavily damaged mitochondria, which are included in single membrane-bound autophagic/autolysophagic vacuoles (mitophagy). PP242 63-68 ES cell expressed Ras Homo sapiens 77-81 26885449-3 2015 The effect of metformin alone or in combination with pp242 (an mTOR inhibitor) on salivary adenocarcinoma cells growth were determined in vitro and in vivo. PP242 53-58 mechanistic target of rapamycin kinase Homo sapiens 63-67 26885449-6 2015 The distinctive effects of metformin and PP242 on MYC reduction and P53 restoration suggested that metformin inhibited cell growth through a different pathway from PP242 in salivary carcinoma cells. PP242 41-46 MYC proto-oncogene, bHLH transcription factor Homo sapiens 50-53 26586952-2 2015 On the other hand, although the second-generation mTOR inhibitor, PP242, has exerted substantial efficacy, it was revealed that independent inhibition by PP242 was transient, which could lead to positive-feedback loop to EGFR. PP242 66-71 mechanistic target of rapamycin kinase Homo sapiens 50-54 26586952-2 2015 On the other hand, although the second-generation mTOR inhibitor, PP242, has exerted substantial efficacy, it was revealed that independent inhibition by PP242 was transient, which could lead to positive-feedback loop to EGFR. PP242 66-71 epidermal growth factor receptor Homo sapiens 221-225 26586952-2 2015 On the other hand, although the second-generation mTOR inhibitor, PP242, has exerted substantial efficacy, it was revealed that independent inhibition by PP242 was transient, which could lead to positive-feedback loop to EGFR. PP242 154-159 mechanistic target of rapamycin kinase Homo sapiens 50-54 26586952-2 2015 On the other hand, although the second-generation mTOR inhibitor, PP242, has exerted substantial efficacy, it was revealed that independent inhibition by PP242 was transient, which could lead to positive-feedback loop to EGFR. PP242 154-159 epidermal growth factor receptor Homo sapiens 221-225 26586952-6 2015 Interestingly, the percentage of CD44-positive cancer cells was substantially decreased by the combination therapy in comparison with PP242 alone through fluorescence-activated cell sorting. PP242 134-139 CD44 molecule (Indian blood group) Homo sapiens 33-37 26416965-5 2015 Blocking mTOR signaling with rapamycin or PP242 or mitochondrial ATP production (e.g., with CCCP) reduced mitochondrial Ca(2+) uptake and membrane potential, and impaired cellular ATP release and neutrophil chemotaxis. PP242 42-47 mechanistic target of rapamycin kinase Homo sapiens 9-13 26041412-5 2015 We inhibited mTOR activity in gSSCs with PP242 and found that MEF2C phosphorylation was decreased and that muscle creatine kinase (MCK) expression was suppressed. PP242 41-46 mechanistic target of rapamycin kinase Homo sapiens 13-17 26001614-8 2015 Co-treatment with mammalian target of rapamycin kinase complex 1 (mTORC1) inhibitor PP242, which activated transcription factor EB (TFEB) signaling and lysosome biogenesis, partially rescued the accumulation of alpha-SYN in PC12 cells and midbrain neurons. PP242 84-89 CREB regulated transcription coactivator 1 Mus musculus 66-72 26134617-16 2015 Upon treatments of RICTOR siRNA or PP242, phosphorylated FLNA levels at the regulatory residue (Ser2152) decreased. PP242 35-40 RPTOR independent companion of MTOR complex 2 Homo sapiens 19-25 26001614-8 2015 Co-treatment with mammalian target of rapamycin kinase complex 1 (mTORC1) inhibitor PP242, which activated transcription factor EB (TFEB) signaling and lysosome biogenesis, partially rescued the accumulation of alpha-SYN in PC12 cells and midbrain neurons. PP242 84-89 transcription factor EB Homo sapiens 107-130 26001614-8 2015 Co-treatment with mammalian target of rapamycin kinase complex 1 (mTORC1) inhibitor PP242, which activated transcription factor EB (TFEB) signaling and lysosome biogenesis, partially rescued the accumulation of alpha-SYN in PC12 cells and midbrain neurons. PP242 84-89 transcription factor EB Homo sapiens 132-136 26001614-8 2015 Co-treatment with mammalian target of rapamycin kinase complex 1 (mTORC1) inhibitor PP242, which activated transcription factor EB (TFEB) signaling and lysosome biogenesis, partially rescued the accumulation of alpha-SYN in PC12 cells and midbrain neurons. PP242 84-89 synuclein alpha Homo sapiens 211-220 26002467-6 2015 Administration of PP242 or knock-down of eIF4E suppressed RACK1-stimulated collagen 1alpha1 production, proliferation and migration in primary HSCs. PP242 18-23 receptor for activated C kinase 1 Homo sapiens 58-63 26134617-16 2015 Upon treatments of RICTOR siRNA or PP242, phosphorylated FLNA levels at the regulatory residue (Ser2152) decreased. PP242 35-40 filamin A Homo sapiens 57-61 25535978-1 2015 PP242 is a novel dual mammalian target of rapamycin (mTOR) inhibitor that simultaneously inhibits mTORC1 and mTORC2, and its antileukemia effect has been sufficiently investigated here. PP242 0-5 mechanistic target of rapamycin kinase Homo sapiens 22-51 25814662-6 2015 At the same time, mTORC1 inhibitors rapamycin and PP242 suppress expression of the Egr1 protein and have an opposite effect on the Egr1 mRNA. PP242 50-55 CREB regulated transcription coactivator 1 Mus musculus 18-24 25814662-6 2015 At the same time, mTORC1 inhibitors rapamycin and PP242 suppress expression of the Egr1 protein and have an opposite effect on the Egr1 mRNA. PP242 50-55 early growth response 1 Mus musculus 83-87 25814662-6 2015 At the same time, mTORC1 inhibitors rapamycin and PP242 suppress expression of the Egr1 protein and have an opposite effect on the Egr1 mRNA. PP242 50-55 early growth response 1 Mus musculus 131-135 25918246-4 2015 Mcl-1 levels in cancer cells were decreased by mTOR kinase inhibitors (TORKinibs), which inhibit both mTORCs, by knocking down rictor and by knocking out rictor or Sin1 but not by silencing raptor. PP242 71-80 MCL1 apoptosis regulator, BCL2 family member Homo sapiens 0-5 25918246-4 2015 Mcl-1 levels in cancer cells were decreased by mTOR kinase inhibitors (TORKinibs), which inhibit both mTORCs, by knocking down rictor and by knocking out rictor or Sin1 but not by silencing raptor. PP242 71-80 RPTOR independent companion of MTOR complex 2 Homo sapiens 127-133 25918246-4 2015 Mcl-1 levels in cancer cells were decreased by mTOR kinase inhibitors (TORKinibs), which inhibit both mTORCs, by knocking down rictor and by knocking out rictor or Sin1 but not by silencing raptor. PP242 71-80 RPTOR independent companion of MTOR complex 2 Homo sapiens 154-160 25918246-4 2015 Mcl-1 levels in cancer cells were decreased by mTOR kinase inhibitors (TORKinibs), which inhibit both mTORCs, by knocking down rictor and by knocking out rictor or Sin1 but not by silencing raptor. PP242 71-80 MAPK associated protein 1 Homo sapiens 164-168 25918246-6 2015 Moreover, TORKinib-induced Mcl-1 reduction was rescued by proteasome inhibition. PP242 10-18 MCL1 apoptosis regulator, BCL2 family member Homo sapiens 27-32 25918246-7 2015 Consistently, TORKinib increased Mcl-1 ubiquitination. PP242 14-22 MCL1 apoptosis regulator, BCL2 family member Homo sapiens 33-38 25918246-9 2015 Suppression of glycogen synthase kinase 3 (GSK3) or FBXW7 rescued Mcl-1 reduction induced by TORKinibs or rictor knockdown. PP242 93-102 F-box and WD repeat domain containing 7 Homo sapiens 52-57 25918246-9 2015 Suppression of glycogen synthase kinase 3 (GSK3) or FBXW7 rescued Mcl-1 reduction induced by TORKinibs or rictor knockdown. PP242 93-102 MCL1 apoptosis regulator, BCL2 family member Homo sapiens 66-71 25918246-11 2015 Intriguingly, we detected a direct association between mTORC2 and SCF-FBXW7; this association could be inhibited by TORKinib treatment, suggesting that mTORC2 may directly associate with and inhibit the SCF-FBXW7 complex, resulting in delayed Mcl-1 degradation. PP242 116-124 CREB regulated transcription coactivator 2 Mus musculus 55-61 25918246-11 2015 Intriguingly, we detected a direct association between mTORC2 and SCF-FBXW7; this association could be inhibited by TORKinib treatment, suggesting that mTORC2 may directly associate with and inhibit the SCF-FBXW7 complex, resulting in delayed Mcl-1 degradation. PP242 116-124 KIT ligand Homo sapiens 66-69 25918246-11 2015 Intriguingly, we detected a direct association between mTORC2 and SCF-FBXW7; this association could be inhibited by TORKinib treatment, suggesting that mTORC2 may directly associate with and inhibit the SCF-FBXW7 complex, resulting in delayed Mcl-1 degradation. PP242 116-124 F-box and WD repeat domain containing 7 Homo sapiens 70-75 25918246-11 2015 Intriguingly, we detected a direct association between mTORC2 and SCF-FBXW7; this association could be inhibited by TORKinib treatment, suggesting that mTORC2 may directly associate with and inhibit the SCF-FBXW7 complex, resulting in delayed Mcl-1 degradation. PP242 116-124 CREB regulated transcription coactivator 2 Mus musculus 152-158 25918246-11 2015 Intriguingly, we detected a direct association between mTORC2 and SCF-FBXW7; this association could be inhibited by TORKinib treatment, suggesting that mTORC2 may directly associate with and inhibit the SCF-FBXW7 complex, resulting in delayed Mcl-1 degradation. PP242 116-124 KIT ligand Homo sapiens 203-206 25918246-11 2015 Intriguingly, we detected a direct association between mTORC2 and SCF-FBXW7; this association could be inhibited by TORKinib treatment, suggesting that mTORC2 may directly associate with and inhibit the SCF-FBXW7 complex, resulting in delayed Mcl-1 degradation. PP242 116-124 F-box and WD repeat domain containing 7 Homo sapiens 207-212 25918246-11 2015 Intriguingly, we detected a direct association between mTORC2 and SCF-FBXW7; this association could be inhibited by TORKinib treatment, suggesting that mTORC2 may directly associate with and inhibit the SCF-FBXW7 complex, resulting in delayed Mcl-1 degradation. PP242 116-124 MCL1 apoptosis regulator, BCL2 family member Homo sapiens 243-248 25151963-9 2015 Conversely, suppression of mTOR with the chemical inhibitors PP242 or rapamycin-sensitized DOV13, an ovarian cancer cell line incapable of inducing REDD1, to orlistat-induced cell death through caspase-2. PP242 61-66 mechanistic target of rapamycin kinase Homo sapiens 27-31 25762619-5 2015 Also, PP242, an mTORC1/2 kinase inhibitor, inhibited cell adhesion more potently than rapamycin (mTORC1 inhibitor). PP242 6-11 CREB regulated transcription coactivator 1 Mus musculus 16-22 25535978-1 2015 PP242 is a novel dual mammalian target of rapamycin (mTOR) inhibitor that simultaneously inhibits mTORC1 and mTORC2, and its antileukemia effect has been sufficiently investigated here. PP242 0-5 mechanistic target of rapamycin kinase Homo sapiens 53-57 25535978-1 2015 PP242 is a novel dual mammalian target of rapamycin (mTOR) inhibitor that simultaneously inhibits mTORC1 and mTORC2, and its antileukemia effect has been sufficiently investigated here. PP242 0-5 CREB regulated transcription coactivator 1 Mus musculus 98-104 25535978-1 2015 PP242 is a novel dual mammalian target of rapamycin (mTOR) inhibitor that simultaneously inhibits mTORC1 and mTORC2, and its antileukemia effect has been sufficiently investigated here. PP242 0-5 CREB regulated transcription coactivator 2 Mus musculus 109-115 25535978-7 2015 The phosphorylation levels of eIF4E (p-eIF4E) at Ser209 influence the antileukemia roles of PP242. PP242 92-97 eukaryotic translation initiation factor 4E Homo sapiens 30-35 25535978-7 2015 The phosphorylation levels of eIF4E (p-eIF4E) at Ser209 influence the antileukemia roles of PP242. PP242 92-97 eukaryotic translation initiation factor 4E Homo sapiens 37-44 25535978-9 2015 Surprisingly, the effects of PP242 in leukemia cells with high p-eIF4E expression, such as the acute myelomonocytic leukemia THP-1 cell line and M4-M5 primary blasts, were also weak. PP242 29-34 eukaryotic translation initiation factor 4E Homo sapiens 63-70 25535978-10 2015 In contrast, PP242 exerted a significant antiproliferative effect in the Ph+ acute lymphoblastic leukemia SUP-B15 cell line and the mantle cell lymphoma JEKO-1 cell line, which had intermediate p-eIF4E levels. PP242 13-18 eukaryotic translation initiation factor 4E Homo sapiens 194-201 25535978-11 2015 PP242 inhibited the translation of the antiapoptotic protein Mcl-1 by downregulating the Akt/mTORC1/eIF4E signaling pathway. PP242 0-5 MCL1 apoptosis regulator, BCL2 family member Homo sapiens 61-66 25535978-11 2015 PP242 inhibited the translation of the antiapoptotic protein Mcl-1 by downregulating the Akt/mTORC1/eIF4E signaling pathway. PP242 0-5 AKT serine/threonine kinase 1 Homo sapiens 89-92 25535978-11 2015 PP242 inhibited the translation of the antiapoptotic protein Mcl-1 by downregulating the Akt/mTORC1/eIF4E signaling pathway. PP242 0-5 CREB regulated transcription coactivator 1 Mus musculus 93-99 25535978-11 2015 PP242 inhibited the translation of the antiapoptotic protein Mcl-1 by downregulating the Akt/mTORC1/eIF4E signaling pathway. PP242 0-5 eukaryotic translation initiation factor 4E Homo sapiens 100-105 25265063-7 2015 Finally, we testified the role of mTORC2 in vivo by demonstrating that PP242 prevented insulin-stimulated SGK1 activation and ENaC increase during ALI. PP242 71-76 CREB regulated transcription coactivator 2 Mus musculus 34-40 25265063-7 2015 Finally, we testified the role of mTORC2 in vivo by demonstrating that PP242 prevented insulin-stimulated SGK1 activation and ENaC increase during ALI. PP242 71-76 insulin Homo sapiens 87-94 25265063-7 2015 Finally, we testified the role of mTORC2 in vivo by demonstrating that PP242 prevented insulin-stimulated SGK1 activation and ENaC increase during ALI. PP242 71-76 serum/glucocorticoid regulated kinase 1 Mus musculus 106-110 25415435-4 2015 We found that 2 structurally distinct competitive inhibitors (PP242 and AZD8055), both of which prevent all mTOR-dependent phosphorylation, including that of SGK1, caused substantial natriuresis, but not kaliuresis, in WT mice, which indicates that mTOR preferentially influences ENaC function. PP242 62-67 mechanistic target of rapamycin kinase Mus musculus 108-112 25415435-4 2015 We found that 2 structurally distinct competitive inhibitors (PP242 and AZD8055), both of which prevent all mTOR-dependent phosphorylation, including that of SGK1, caused substantial natriuresis, but not kaliuresis, in WT mice, which indicates that mTOR preferentially influences ENaC function. PP242 62-67 serum/glucocorticoid regulated kinase 1 Mus musculus 158-162 25415435-4 2015 We found that 2 structurally distinct competitive inhibitors (PP242 and AZD8055), both of which prevent all mTOR-dependent phosphorylation, including that of SGK1, caused substantial natriuresis, but not kaliuresis, in WT mice, which indicates that mTOR preferentially influences ENaC function. PP242 62-67 mechanistic target of rapamycin kinase Mus musculus 249-253 25239638-4 2015 The aim of the study was to determine the therapeutic effect of an mTOR kinase inhibitor, PP242, in the Han:SPRD rat (Cy/+) model of PKD. PP242 90-95 mechanistic target of rapamycin kinase Rattus norvegicus 67-71 25239638-7 2015 On immunoblot of kidneys, PP242 resulted in a decrease in pS6, a marker of mTORC1 signaling and pAkt(Ser473), a marker of mTORC2 signaling. PP242 26-31 CREB regulated transcription coactivator 1 Mus musculus 75-81 25239638-7 2015 On immunoblot of kidneys, PP242 resulted in a decrease in pS6, a marker of mTORC1 signaling and pAkt(Ser473), a marker of mTORC2 signaling. PP242 26-31 CREB regulated transcription coactivator 2 Mus musculus 122-128 25440763-0 2015 The dual mTORC1 and mTORC2 inhibitor PP242 shows strong antitumor activity in a pheochromocytoma PC12 cell tumor model. PP242 37-42 CREB regulated transcription coactivator 2 Mus musculus 20-26 25440763-1 2015 OBJECTIVE: To assess the activity of mTOR and downstream effector proteins in the mTOR pathway after treatment with a dual mTOR complex 1 and 2 (mTORC1/2) inhibitor (PP242) compared with that of mTOR complex 1 (mTORC1) inhibitor (rapamycin) using a xenograft tumor model. PP242 166-171 mechanistic target of rapamycin kinase Rattus norvegicus 37-41 25440763-1 2015 OBJECTIVE: To assess the activity of mTOR and downstream effector proteins in the mTOR pathway after treatment with a dual mTOR complex 1 and 2 (mTORC1/2) inhibitor (PP242) compared with that of mTOR complex 1 (mTORC1) inhibitor (rapamycin) using a xenograft tumor model. PP242 166-171 mechanistic target of rapamycin kinase Rattus norvegicus 82-86 25440763-1 2015 OBJECTIVE: To assess the activity of mTOR and downstream effector proteins in the mTOR pathway after treatment with a dual mTOR complex 1 and 2 (mTORC1/2) inhibitor (PP242) compared with that of mTOR complex 1 (mTORC1) inhibitor (rapamycin) using a xenograft tumor model. PP242 166-171 mechanistic target of rapamycin kinase Rattus norvegicus 82-86 25440763-1 2015 OBJECTIVE: To assess the activity of mTOR and downstream effector proteins in the mTOR pathway after treatment with a dual mTOR complex 1 and 2 (mTORC1/2) inhibitor (PP242) compared with that of mTOR complex 1 (mTORC1) inhibitor (rapamycin) using a xenograft tumor model. PP242 166-171 CREB regulated transcription coactivator 2 Mus musculus 145-153 25440763-1 2015 OBJECTIVE: To assess the activity of mTOR and downstream effector proteins in the mTOR pathway after treatment with a dual mTOR complex 1 and 2 (mTORC1/2) inhibitor (PP242) compared with that of mTOR complex 1 (mTORC1) inhibitor (rapamycin) using a xenograft tumor model. PP242 166-171 mechanistic target of rapamycin kinase Rattus norvegicus 82-86 24949720-12 2014 Importantly, PP242, a specific mTOR inhibitor, abolished both cardioprotection and protein phosphorylation in isolated heart and reduced apoptotic effects in H9c2 cells. PP242 13-18 mechanistic target of rapamycin kinase Rattus norvegicus 31-35 25035961-0 2014 PP242 suppresses cell proliferation, metastasis, and angiogenesis of gastric cancer through inhibition of the PI3K/AKT/mTOR pathway. PP242 0-5 AKT serine/threonine kinase 1 Homo sapiens 115-118 25035961-0 2014 PP242 suppresses cell proliferation, metastasis, and angiogenesis of gastric cancer through inhibition of the PI3K/AKT/mTOR pathway. PP242 0-5 mechanistic target of rapamycin kinase Homo sapiens 119-123 25035961-9 2014 Then, an inhibitory effect of PP242 on metastasis was observed in gastric cancer cell AGS, along with the cytoskeletal rearrangements and suppression of the phosphorylation of PI3K downstream factors including AKT, mTOR, and P70S6K. PP242 30-35 AKT serine/threonine kinase 1 Homo sapiens 210-213 25035961-9 2014 Then, an inhibitory effect of PP242 on metastasis was observed in gastric cancer cell AGS, along with the cytoskeletal rearrangements and suppression of the phosphorylation of PI3K downstream factors including AKT, mTOR, and P70S6K. PP242 30-35 mechanistic target of rapamycin kinase Homo sapiens 215-219 25035961-9 2014 Then, an inhibitory effect of PP242 on metastasis was observed in gastric cancer cell AGS, along with the cytoskeletal rearrangements and suppression of the phosphorylation of PI3K downstream factors including AKT, mTOR, and P70S6K. PP242 30-35 ribosomal protein S6 kinase B1 Homo sapiens 225-231 25035961-12 2014 These results show that PP242 suppresses cell proliferation and angiogenesis of gastric cancer through inhibition of the PI3K/AKT/mTOR pathway, which might be an effective novel therapeutic candidate against gastric cancer in the future. PP242 24-29 AKT serine/threonine kinase 1 Homo sapiens 126-129 25035961-12 2014 These results show that PP242 suppresses cell proliferation and angiogenesis of gastric cancer through inhibition of the PI3K/AKT/mTOR pathway, which might be an effective novel therapeutic candidate against gastric cancer in the future. PP242 24-29 mechanistic target of rapamycin kinase Homo sapiens 130-134 25392452-5 2014 In this report, we use two small molecule inhibitors, PP242 (dual mTOR (mammalian target of rapamycin) kinase inhibitor) and hippuristanol (eIF4A inhibitor), to define IRES regulation via a Bcr-Abl-mTOR-eIF4A axis in CML cell lines and primary patient leukaemias. PP242 54-59 mechanistic target of rapamycin kinase Homo sapiens 66-70 25392452-5 2014 In this report, we use two small molecule inhibitors, PP242 (dual mTOR (mammalian target of rapamycin) kinase inhibitor) and hippuristanol (eIF4A inhibitor), to define IRES regulation via a Bcr-Abl-mTOR-eIF4A axis in CML cell lines and primary patient leukaemias. PP242 54-59 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 190-197 25055139-7 2014 Markers of glutamatergic afferents, VGluT1, and GABAergic afferents, GAD67, were induced by lipopolysaccharides and coexpressed with P2X in small-sized TG neurons. PP242 133-136 glutamate decarboxylase 1 Rattus norvegicus 69-74 24396066-4 2014 The Paip1-eIF3 interaction is impaired by the mTORC1 inhibitors, rapamycin and PP242. PP242 79-84 poly(A) binding protein interacting protein 1 Homo sapiens 4-9 23542178-3 2014 We screened a panel of over 600 human cancer cell lines to identify markers of resistance and sensitivity to the mTOR inhibitor PP242. PP242 128-133 mechanistic target of rapamycin kinase Homo sapiens 113-117 23542178-7 2014 Immunoblot analysis of the signaling targets downstream of mTOR revealed that the degree of cellular growth inhibition induced by PP242 was correlated with inhibition of phosphorylation of the translational repressor eIF4E-binding protein 1 (4E-BP1), but not ribosomal protein S6 (rpS6). PP242 130-135 mechanistic target of rapamycin kinase Homo sapiens 59-63 23542178-7 2014 Immunoblot analysis of the signaling targets downstream of mTOR revealed that the degree of cellular growth inhibition induced by PP242 was correlated with inhibition of phosphorylation of the translational repressor eIF4E-binding protein 1 (4E-BP1), but not ribosomal protein S6 (rpS6). PP242 130-135 eukaryotic translation initiation factor 4E binding protein 1 Homo sapiens 217-240 23542178-7 2014 Immunoblot analysis of the signaling targets downstream of mTOR revealed that the degree of cellular growth inhibition induced by PP242 was correlated with inhibition of phosphorylation of the translational repressor eIF4E-binding protein 1 (4E-BP1), but not ribosomal protein S6 (rpS6). PP242 130-135 eukaryotic translation initiation factor 4E binding protein 1 Homo sapiens 242-248 23542178-7 2014 Immunoblot analysis of the signaling targets downstream of mTOR revealed that the degree of cellular growth inhibition induced by PP242 was correlated with inhibition of phosphorylation of the translational repressor eIF4E-binding protein 1 (4E-BP1), but not ribosomal protein S6 (rpS6). PP242 130-135 ribosomal protein S6 Homo sapiens 259-279 23542178-7 2014 Immunoblot analysis of the signaling targets downstream of mTOR revealed that the degree of cellular growth inhibition induced by PP242 was correlated with inhibition of phosphorylation of the translational repressor eIF4E-binding protein 1 (4E-BP1), but not ribosomal protein S6 (rpS6). PP242 130-135 ribosomal protein S6 Homo sapiens 281-285 24396066-4 2014 The Paip1-eIF3 interaction is impaired by the mTORC1 inhibitors, rapamycin and PP242. PP242 79-84 eukaryotic translation initiation factor 3 subunit A Homo sapiens 10-14 24209570-0 2013 Re: Extracellular UDP enhances P2X-mediated bladder smooth muscle contractility via P2Y6 activation of the phospholipase C/Inositol trisphosphate pathway. PP242 31-34 pyrimidinergic receptor P2Y6 Homo sapiens 84-88 24270265-8 2014 Treatment with the mTOR kinase inhibitor PP242 at days 15 to 28 suppressed mTORC2 but not Nox4, induced smooth muscle-specific apoptosis in small pulmonary arteries, and reversed hypoxia-induced pulmonary vascular remodeling in rats. PP242 41-46 mechanistic target of rapamycin kinase Rattus norvegicus 19-23 24270265-8 2014 Treatment with the mTOR kinase inhibitor PP242 at days 15 to 28 suppressed mTORC2 but not Nox4, induced smooth muscle-specific apoptosis in small pulmonary arteries, and reversed hypoxia-induced pulmonary vascular remodeling in rats. PP242 41-46 CREB regulated transcription coactivator 2 Mus musculus 75-81 24270265-8 2014 Treatment with the mTOR kinase inhibitor PP242 at days 15 to 28 suppressed mTORC2 but not Nox4, induced smooth muscle-specific apoptosis in small pulmonary arteries, and reversed hypoxia-induced pulmonary vascular remodeling in rats. PP242 41-46 NADPH oxidase 4 Rattus norvegicus 90-94 24316308-3 2014 Using a xenograft tumor model of endometrial cancer, we assessed the activity of mTOR and downstream effector proteins in the mTOR translational control pathway after treatment with a dual mTOR complex 1 and 2 (mTORC1/2) catalytic inhibitor (PP242) compared to that of an allosteric mTOR complex 1 (mTORC1) inhibitor (everolimus, RAD001). PP242 242-247 mechanistic target of rapamycin kinase Mus musculus 81-85 24316308-3 2014 Using a xenograft tumor model of endometrial cancer, we assessed the activity of mTOR and downstream effector proteins in the mTOR translational control pathway after treatment with a dual mTOR complex 1 and 2 (mTORC1/2) catalytic inhibitor (PP242) compared to that of an allosteric mTOR complex 1 (mTORC1) inhibitor (everolimus, RAD001). PP242 242-247 CREB regulated transcription coactivator 2 Mus musculus 211-219 23907312-5 2014 mTOR signaling was activated in stem-like colorectal cancer cells, and mTOR inhibitors (rapamycin and PP242) decreased the capacity of sphere formation as well as ALDH activity. PP242 102-107 mechanistic target of rapamycin kinase Homo sapiens 0-4 23907312-5 2014 mTOR signaling was activated in stem-like colorectal cancer cells, and mTOR inhibitors (rapamycin and PP242) decreased the capacity of sphere formation as well as ALDH activity. PP242 102-107 mechanistic target of rapamycin kinase Homo sapiens 71-75 25482947-7 2014 Synthetic inhibitors of mTOR (temsirolimus, LY294.002 and PP242) also impaired actinomycin D triggered p53 stabilization and induction of p21. PP242 58-63 mechanistic target of rapamycin kinase Homo sapiens 24-28 25482947-7 2014 Synthetic inhibitors of mTOR (temsirolimus, LY294.002 and PP242) also impaired actinomycin D triggered p53 stabilization and induction of p21. PP242 58-63 tumor protein p53 Homo sapiens 103-106 25482947-7 2014 Synthetic inhibitors of mTOR (temsirolimus, LY294.002 and PP242) also impaired actinomycin D triggered p53 stabilization and induction of p21. PP242 58-63 H3 histone pseudogene 16 Homo sapiens 138-141 24008673-4 2013 Indeed, inhibition of mTOR pathway by mTOR inhibitors (rapamycin and PP242) or 2DG promoted not only apoptosis but also autophagy in the polyploidy cells induced by Aurora inhibitors. PP242 69-74 mechanistic target of rapamycin kinase Homo sapiens 22-26 24008673-4 2013 Indeed, inhibition of mTOR pathway by mTOR inhibitors (rapamycin and PP242) or 2DG promoted not only apoptosis but also autophagy in the polyploidy cells induced by Aurora inhibitors. PP242 69-74 mechanistic target of rapamycin kinase Homo sapiens 38-42 23670294-5 2013 Indeed, pharmacological antagonism of Bcl-xL, with ABT-263, combined with PP242-induced activation of BAD markedly augmented apoptosis of CML-BC cell lines and primary CD34(+) progenitors but not those from healthy donors, regardless of drug resistance induced by bone marrow stromal cell-generated signals. PP242 74-79 CD34 molecule Homo sapiens 168-172 23838676-3 2013 In the present study, we examined the antitumor effects of a specific mTOR kinase inhibitor, PP242, which blocks both mTOR complex 1 (mTORC1) and mTOR complex 2 (mTORC2) pathways, in two ESCC cell lines: Eca-109 and TE-1. PP242 93-98 mechanistic target of rapamycin kinase Homo sapiens 70-74 23838676-3 2013 In the present study, we examined the antitumor effects of a specific mTOR kinase inhibitor, PP242, which blocks both mTOR complex 1 (mTORC1) and mTOR complex 2 (mTORC2) pathways, in two ESCC cell lines: Eca-109 and TE-1. PP242 93-98 mechanistic target of rapamycin kinase Homo sapiens 118-122 23838676-3 2013 In the present study, we examined the antitumor effects of a specific mTOR kinase inhibitor, PP242, which blocks both mTOR complex 1 (mTORC1) and mTOR complex 2 (mTORC2) pathways, in two ESCC cell lines: Eca-109 and TE-1. PP242 93-98 CREB regulated transcription coactivator 1 Mus musculus 134-140 23838676-3 2013 In the present study, we examined the antitumor effects of a specific mTOR kinase inhibitor, PP242, which blocks both mTOR complex 1 (mTORC1) and mTOR complex 2 (mTORC2) pathways, in two ESCC cell lines: Eca-109 and TE-1. PP242 93-98 mechanistic target of rapamycin kinase Homo sapiens 118-122 23838676-3 2013 In the present study, we examined the antitumor effects of a specific mTOR kinase inhibitor, PP242, which blocks both mTOR complex 1 (mTORC1) and mTOR complex 2 (mTORC2) pathways, in two ESCC cell lines: Eca-109 and TE-1. PP242 93-98 CREB regulated transcription coactivator 2 Mus musculus 162-168 23838676-4 2013 We showed that PP242, but not rapamycin, attenuated the activities of both mTORC1 and mTORC2 signaling in ESCC. PP242 15-20 CREB regulated transcription coactivator 1 Mus musculus 75-81 23838676-4 2013 We showed that PP242, but not rapamycin, attenuated the activities of both mTORC1 and mTORC2 signaling in ESCC. PP242 15-20 CREB regulated transcription coactivator 2 Mus musculus 86-92 23838676-5 2013 PP242 inhibited 4E-binding protein-1 phosphorylation and abrogated mTORC1-dependent PI3K/Akt feedback activation. PP242 0-5 CREB regulated transcription coactivator 1 Mus musculus 67-73 23838676-5 2013 PP242 inhibited 4E-binding protein-1 phosphorylation and abrogated mTORC1-dependent PI3K/Akt feedback activation. PP242 0-5 AKT serine/threonine kinase 1 Homo sapiens 89-92 23838676-7 2013 Furthermore, PP242 promoted cisplatin-induced apoptosis and enhanced the antitumor efficacy of cisplatin in ESCC cells, which was likely to be associated with inhibition of Akt activity. PP242 13-18 AKT serine/threonine kinase 1 Homo sapiens 173-176 23528835-3 2013 Perifosine and PP242, selective inhibitors of Akt and mTORC1/2, respectively, efficiently suppressed the Akt phosphorylation that was induced by the sustained overexpression of Redd1 and increased the sensitivity of the cells to cisplatin. PP242 15-20 AKT serine/threonine kinase 1 Homo sapiens 46-49 23991179-2 2013 The second generation of mTOR inhibitors such as PP242 targets mTOR kinase; thus, they are capable of inhibiting both mTORC1 and mTORC2. PP242 49-54 mechanistic target of rapamycin kinase Homo sapiens 25-29 23991179-2 2013 The second generation of mTOR inhibitors such as PP242 targets mTOR kinase; thus, they are capable of inhibiting both mTORC1 and mTORC2. PP242 49-54 mechanistic target of rapamycin kinase Homo sapiens 63-67 23991179-2 2013 The second generation of mTOR inhibitors such as PP242 targets mTOR kinase; thus, they are capable of inhibiting both mTORC1 and mTORC2. PP242 49-54 CREB regulated transcription coactivator 1 Mus musculus 118-124 23991179-2 2013 The second generation of mTOR inhibitors such as PP242 targets mTOR kinase; thus, they are capable of inhibiting both mTORC1 and mTORC2. PP242 49-54 CREB regulated transcription coactivator 2 Mus musculus 129-135 23991179-3 2013 To examine the therapeutic potential of the mTOR kinase inhibitors, we treated a panel of colorectal carcinoma cell lines with PP242. PP242 127-132 mechanistic target of rapamycin kinase Homo sapiens 44-48 23991179-4 2013 Western blotting showed that the PP242 inhibition of mTORC2-mediated AKT phosphorylation at Ser 473 (AKT(S473)) was transient only in the first few hours of the PP242 treatment. PP242 33-38 CREB regulated transcription coactivator 2 Mus musculus 53-59 23991179-4 2013 Western blotting showed that the PP242 inhibition of mTORC2-mediated AKT phosphorylation at Ser 473 (AKT(S473)) was transient only in the first few hours of the PP242 treatment. PP242 33-38 AKT serine/threonine kinase 1 Homo sapiens 69-72 23991179-4 2013 Western blotting showed that the PP242 inhibition of mTORC2-mediated AKT phosphorylation at Ser 473 (AKT(S473)) was transient only in the first few hours of the PP242 treatment. PP242 33-38 AKT serine/threonine kinase 1 Homo sapiens 101-104 23991179-4 2013 Western blotting showed that the PP242 inhibition of mTORC2-mediated AKT phosphorylation at Ser 473 (AKT(S473)) was transient only in the first few hours of the PP242 treatment. PP242 161-166 CREB regulated transcription coactivator 2 Mus musculus 53-59 23991179-4 2013 Western blotting showed that the PP242 inhibition of mTORC2-mediated AKT phosphorylation at Ser 473 (AKT(S473)) was transient only in the first few hours of the PP242 treatment. PP242 161-166 AKT serine/threonine kinase 1 Homo sapiens 69-72 23991179-4 2013 Western blotting showed that the PP242 inhibition of mTORC2-mediated AKT phosphorylation at Ser 473 (AKT(S473)) was transient only in the first few hours of the PP242 treatment. PP242 161-166 AKT serine/threonine kinase 1 Homo sapiens 101-104 23991179-5 2013 Receptor tyrosine kinase arrays further revealed that PP242 treatment increased the phosphorylated epidermal growth factor receptor (EGFR) at Tyr 1068 (EGFR(T1068)). PP242 54-59 epidermal growth factor receptor Homo sapiens 99-131 23991179-5 2013 Receptor tyrosine kinase arrays further revealed that PP242 treatment increased the phosphorylated epidermal growth factor receptor (EGFR) at Tyr 1068 (EGFR(T1068)). PP242 54-59 epidermal growth factor receptor Homo sapiens 133-137 23991179-5 2013 Receptor tyrosine kinase arrays further revealed that PP242 treatment increased the phosphorylated epidermal growth factor receptor (EGFR) at Tyr 1068 (EGFR(T1068)). PP242 54-59 epidermal growth factor receptor Homo sapiens 152-156 23991179-7 2013 To test this notion, we showed that the combination of PP242 with erlotinib, an EGFR small molecule inhibitor, blocked both mTORC1 and mTORC2 kinase activity. PP242 55-60 epidermal growth factor receptor Homo sapiens 80-84 23991179-7 2013 To test this notion, we showed that the combination of PP242 with erlotinib, an EGFR small molecule inhibitor, blocked both mTORC1 and mTORC2 kinase activity. PP242 55-60 CREB regulated transcription coactivator 1 Mus musculus 124-130 23991179-7 2013 To test this notion, we showed that the combination of PP242 with erlotinib, an EGFR small molecule inhibitor, blocked both mTORC1 and mTORC2 kinase activity. PP242 55-60 CREB regulated transcription coactivator 2 Mus musculus 135-141 23528835-3 2013 Perifosine and PP242, selective inhibitors of Akt and mTORC1/2, respectively, efficiently suppressed the Akt phosphorylation that was induced by the sustained overexpression of Redd1 and increased the sensitivity of the cells to cisplatin. PP242 15-20 CREB regulated transcription coactivator 2 Mus musculus 54-62 23528835-3 2013 Perifosine and PP242, selective inhibitors of Akt and mTORC1/2, respectively, efficiently suppressed the Akt phosphorylation that was induced by the sustained overexpression of Redd1 and increased the sensitivity of the cells to cisplatin. PP242 15-20 AKT serine/threonine kinase 1 Homo sapiens 105-108 23528835-3 2013 Perifosine and PP242, selective inhibitors of Akt and mTORC1/2, respectively, efficiently suppressed the Akt phosphorylation that was induced by the sustained overexpression of Redd1 and increased the sensitivity of the cells to cisplatin. PP242 15-20 DNA damage inducible transcript 4 Homo sapiens 177-182 23722550-4 2013 Radiation treatment transiently enhanced autophagic flux for a period of 72 hours in these cells and treatment with rapamycin or the mTOR inhibitor PP242 potentiated this effect. PP242 148-153 mechanistic target of rapamycin kinase Homo sapiens 133-137 23915343-10 2013 Inhibition of mTOR by PP242 abolished the positive effects of PLD1 on myotubes, whereas modulating PLD influenced the phosphorylation of both S6K1 and Akt, which are respectively substrates of mTORC1 and mTORC2 complexes. PP242 22-27 mechanistic target of rapamycin kinase Mus musculus 14-18 23362118-0 2013 Extracellular UDP enhances P2X-mediated bladder smooth muscle contractility via P2Y(6) activation of the phospholipase C/inositol trisphosphate pathway. PP242 27-30 pyrimidinergic receptor P2Y, G-protein coupled, 6 Mus musculus 80-86 23547259-7 2013 Disrupting formation of SG by inactivation of mTOR with its specific inhibitor pp242 or by depletion of eIF4E or eIF4GI blocks the SG-associated antiapoptotic p21 pathway. PP242 79-84 mechanistic target of rapamycin kinase Homo sapiens 46-50 23547259-7 2013 Disrupting formation of SG by inactivation of mTOR with its specific inhibitor pp242 or by depletion of eIF4E or eIF4GI blocks the SG-associated antiapoptotic p21 pathway. PP242 79-84 H3 histone pseudogene 16 Homo sapiens 159-162 23730416-2 2013 The goal of this study was to compare the radiosensitizing activities of the allosteric mTOR inhibitor rapamycin with that of the competitive mTOR inhibitor PP242. PP242 157-162 mechanistic target of rapamycin kinase Homo sapiens 142-146 23147251-5 2013 MATERIALS AND METHODS: We used PP242, a dual inhibitor of mTORC1/mTORC2 and the mTORC1 specific inhibitor rapamycin. PP242 31-36 CREB regulated transcription coactivator 1 Mus musculus 58-64 23147251-10 2013 In 786-O cells HIF-2alpha inhibition induced by the dual mTORC1/C2 inhibitor PP242 (0.05 to 0.5 mumol/L) resulted in a dose dependent increase in E-cadherin expression and the restored E-cadherin was localized at cell-to-cell junctions. PP242 77-82 endothelial PAS domain protein 1 Homo sapiens 15-25 23147251-10 2013 In 786-O cells HIF-2alpha inhibition induced by the dual mTORC1/C2 inhibitor PP242 (0.05 to 0.5 mumol/L) resulted in a dose dependent increase in E-cadherin expression and the restored E-cadherin was localized at cell-to-cell junctions. PP242 77-82 CREB regulated transcription coactivator 1 Mus musculus 57-63 23147251-10 2013 In 786-O cells HIF-2alpha inhibition induced by the dual mTORC1/C2 inhibitor PP242 (0.05 to 0.5 mumol/L) resulted in a dose dependent increase in E-cadherin expression and the restored E-cadherin was localized at cell-to-cell junctions. PP242 77-82 cadherin 1 Homo sapiens 146-156 23147251-10 2013 In 786-O cells HIF-2alpha inhibition induced by the dual mTORC1/C2 inhibitor PP242 (0.05 to 0.5 mumol/L) resulted in a dose dependent increase in E-cadherin expression and the restored E-cadherin was localized at cell-to-cell junctions. PP242 77-82 cadherin 1 Homo sapiens 185-195 23319802-4 2013 Using the mTOR kinase inhibitor, PP242, as a research tool, we found that it synergized with TRAIL to augment apoptosis of cancer cells. PP242 33-38 mechanistic target of rapamycin kinase Homo sapiens 10-14 23362262-6 2013 Using the mTOR inhibitor PP242, we found that TGFbeta-induced both early and sustained activation of TORC1 and TORC2 was necessary for deptor suppression. PP242 25-30 mechanistic target of rapamycin kinase Homo sapiens 10-14 23362262-6 2013 Using the mTOR inhibitor PP242, we found that TGFbeta-induced both early and sustained activation of TORC1 and TORC2 was necessary for deptor suppression. PP242 25-30 transforming growth factor beta 1 Homo sapiens 46-53 23362262-6 2013 Using the mTOR inhibitor PP242, we found that TGFbeta-induced both early and sustained activation of TORC1 and TORC2 was necessary for deptor suppression. PP242 25-30 CREB regulated transcription coactivator 1 Homo sapiens 101-106 23362262-6 2013 Using the mTOR inhibitor PP242, we found that TGFbeta-induced both early and sustained activation of TORC1 and TORC2 was necessary for deptor suppression. PP242 25-30 CREB regulated transcription coactivator 2 Homo sapiens 111-116 23362262-7 2013 PP242-induced reversal of deptor suppression by TGFbeta was associated with a significant inhibition of TGFbeta-stimulated protein synthesis and hypertrophy. PP242 0-5 transforming growth factor beta 1 Homo sapiens 48-55 23362262-7 2013 PP242-induced reversal of deptor suppression by TGFbeta was associated with a significant inhibition of TGFbeta-stimulated protein synthesis and hypertrophy. PP242 0-5 transforming growth factor beta 1 Homo sapiens 104-111 23482748-0 2013 Comparative effects of PP242 and rapamycin on mTOR signalling and NOTCH signalling in leukemia cells. PP242 23-28 mechanistic target of rapamycin kinase Homo sapiens 46-50 23482748-1 2013 AIM: PP242 is a compound which inhibits both mammalian target of rapamycin complex-1 (mTORC1) and mTORC2. PP242 5-10 CREB regulated transcription coactivator 1 Mus musculus 86-92 23482748-1 2013 AIM: PP242 is a compound which inhibits both mammalian target of rapamycin complex-1 (mTORC1) and mTORC2. PP242 5-10 CREB regulated transcription coactivator 2 Mus musculus 98-104 23319802-4 2013 Using the mTOR kinase inhibitor, PP242, as a research tool, we found that it synergized with TRAIL to augment apoptosis of cancer cells. PP242 33-38 TNF superfamily member 10 Homo sapiens 93-98 23319802-9 2013 Moreover, knockdown of the E3 ligase Cbl (CBL) abolished PP242-induced FLIP(S) reduction. PP242 57-62 Cbl proto-oncogene Homo sapiens 37-40 23319802-9 2013 Moreover, knockdown of the E3 ligase Cbl (CBL) abolished PP242-induced FLIP(S) reduction. PP242 57-62 Cbl proto-oncogene Homo sapiens 42-45 23319802-10 2013 Thus, PP242 induces Cbl-dependent degradation of FLIP(S), leading to FLIP(S) downregulation. PP242 6-11 Cbl proto-oncogene Homo sapiens 20-23 23533410-5 2013 Mice challenged with p27-VEGF transfected tumor cells were more resistant to the antiangiogenic and apoptotic effects of the rapalog, temsirolimus, and active site mTOR inhibitor, pp242. PP242 180-185 cyclin-dependent kinase inhibitor 1B Mus musculus 21-24 23533410-5 2013 Mice challenged with p27-VEGF transfected tumor cells were more resistant to the antiangiogenic and apoptotic effects of the rapalog, temsirolimus, and active site mTOR inhibitor, pp242. PP242 180-185 vascular endothelial growth factor A Mus musculus 25-29 23533410-5 2013 Mice challenged with p27-VEGF transfected tumor cells were more resistant to the antiangiogenic and apoptotic effects of the rapalog, temsirolimus, and active site mTOR inhibitor, pp242. PP242 180-185 mechanistic target of rapamycin kinase Mus musculus 164-168 23437362-5 2013 Rapamycin caused a striking increase in Akt phosphorylation at Ser(473) while the active-site inhibitors of mTOR (KU63794 and PP242) completely abrogated Akt phosphorylation at this site. PP242 126-131 mechanistic target of rapamycin kinase Homo sapiens 108-112 23437362-5 2013 Rapamycin caused a striking increase in Akt phosphorylation at Ser(473) while the active-site inhibitors of mTOR (KU63794 and PP242) completely abrogated Akt phosphorylation at this site. PP242 126-131 AKT serine/threonine kinase 1 Homo sapiens 154-157 22843885-10 2012 pp242, a novel combined mTORC1/2 inhibitor, and rapamycin limited proliferation by reducing the S-Phase entry as assessed by EdU incorporation, while PDGF increased EdU incorporation. PP242 0-5 CREB regulated transcription coactivator 2 Mus musculus 24-32 23026799-6 2012 Moreover, inhibition of MTOR by PP242, an inhibitor of MTOR complex1/2, abrogated the changes in both LC3-II and SQSTM1 in AURKA-overexpressing BT-549 cells, suggesting that AURKA-suppressed autophagy might be associated with MTOR activation. PP242 32-37 mechanistic target of rapamycin kinase Homo sapiens 24-28 23026799-6 2012 Moreover, inhibition of MTOR by PP242, an inhibitor of MTOR complex1/2, abrogated the changes in both LC3-II and SQSTM1 in AURKA-overexpressing BT-549 cells, suggesting that AURKA-suppressed autophagy might be associated with MTOR activation. PP242 32-37 mechanistic target of rapamycin kinase Homo sapiens 55-59 23026799-6 2012 Moreover, inhibition of MTOR by PP242, an inhibitor of MTOR complex1/2, abrogated the changes in both LC3-II and SQSTM1 in AURKA-overexpressing BT-549 cells, suggesting that AURKA-suppressed autophagy might be associated with MTOR activation. PP242 32-37 microtubule associated protein 1 light chain 3 alpha Homo sapiens 102-105 23026799-6 2012 Moreover, inhibition of MTOR by PP242, an inhibitor of MTOR complex1/2, abrogated the changes in both LC3-II and SQSTM1 in AURKA-overexpressing BT-549 cells, suggesting that AURKA-suppressed autophagy might be associated with MTOR activation. PP242 32-37 sequestosome 1 Homo sapiens 113-119 23026799-6 2012 Moreover, inhibition of MTOR by PP242, an inhibitor of MTOR complex1/2, abrogated the changes in both LC3-II and SQSTM1 in AURKA-overexpressing BT-549 cells, suggesting that AURKA-suppressed autophagy might be associated with MTOR activation. PP242 32-37 aurora kinase A Homo sapiens 123-128 23026799-6 2012 Moreover, inhibition of MTOR by PP242, an inhibitor of MTOR complex1/2, abrogated the changes in both LC3-II and SQSTM1 in AURKA-overexpressing BT-549 cells, suggesting that AURKA-suppressed autophagy might be associated with MTOR activation. PP242 32-37 aurora kinase A Homo sapiens 174-179 23026799-6 2012 Moreover, inhibition of MTOR by PP242, an inhibitor of MTOR complex1/2, abrogated the changes in both LC3-II and SQSTM1 in AURKA-overexpressing BT-549 cells, suggesting that AURKA-suppressed autophagy might be associated with MTOR activation. PP242 32-37 mechanistic target of rapamycin kinase Homo sapiens 55-59 22826565-0 2012 Targeting of mTORC1/2 by the mTOR kinase inhibitor PP242 induces apoptosis in AML cells under conditions mimicking the bone marrow microenvironment. PP242 51-56 CREB regulated transcription coactivator 2 Mus musculus 13-21 22826565-0 2012 Targeting of mTORC1/2 by the mTOR kinase inhibitor PP242 induces apoptosis in AML cells under conditions mimicking the bone marrow microenvironment. PP242 51-56 mechanistic target of rapamycin kinase Mus musculus 13-17 22826565-6 2012 Mechanistically, PP242 attenuated the activities of mTORC1 and mTORC2, sequentially inhibited phosphorylated AKT, S6K, and 4EBP1, and concurrently suppressed chemokine receptor CXCR4 expression in primary leukemic cells and in stromal cells cultured alone or cocultured with leukemic cells. PP242 17-22 CREB regulated transcription coactivator 1 Mus musculus 52-58 22826565-6 2012 Mechanistically, PP242 attenuated the activities of mTORC1 and mTORC2, sequentially inhibited phosphorylated AKT, S6K, and 4EBP1, and concurrently suppressed chemokine receptor CXCR4 expression in primary leukemic cells and in stromal cells cultured alone or cocultured with leukemic cells. PP242 17-22 CREB regulated transcription coactivator 2 Mus musculus 63-69 22826565-6 2012 Mechanistically, PP242 attenuated the activities of mTORC1 and mTORC2, sequentially inhibited phosphorylated AKT, S6K, and 4EBP1, and concurrently suppressed chemokine receptor CXCR4 expression in primary leukemic cells and in stromal cells cultured alone or cocultured with leukemic cells. PP242 17-22 thymoma viral proto-oncogene 1 Mus musculus 109-112 22826565-6 2012 Mechanistically, PP242 attenuated the activities of mTORC1 and mTORC2, sequentially inhibited phosphorylated AKT, S6K, and 4EBP1, and concurrently suppressed chemokine receptor CXCR4 expression in primary leukemic cells and in stromal cells cultured alone or cocultured with leukemic cells. PP242 17-22 ribosomal protein S6 kinase, polypeptide 1 Mus musculus 117-128 22826565-6 2012 Mechanistically, PP242 attenuated the activities of mTORC1 and mTORC2, sequentially inhibited phosphorylated AKT, S6K, and 4EBP1, and concurrently suppressed chemokine receptor CXCR4 expression in primary leukemic cells and in stromal cells cultured alone or cocultured with leukemic cells. PP242 17-22 chemokine (C-X-C motif) receptor 4 Mus musculus 177-182 22826565-7 2012 In the in vivo leukemia mouse model, PP242 inhibited mTOR signaling in leukemic cells and demonstrated a greater antileukemia effect than rapamycin. PP242 37-42 mechanistic target of rapamycin kinase Mus musculus 53-57 22476852-4 2012 We demonstrated that inhibition of mTORC1/2 by mTOR kinase inhibitors PP242 and OSI-027 effectively suppress phosphorylation of Akt (S473) and breast cancer cell proliferation. PP242 70-75 CREB regulated transcription coactivator 1 Mus musculus 35-41 22476852-4 2012 We demonstrated that inhibition of mTORC1/2 by mTOR kinase inhibitors PP242 and OSI-027 effectively suppress phosphorylation of Akt (S473) and breast cancer cell proliferation. PP242 70-75 mechanistic target of rapamycin kinase Homo sapiens 35-39 22476852-4 2012 We demonstrated that inhibition of mTORC1/2 by mTOR kinase inhibitors PP242 and OSI-027 effectively suppress phosphorylation of Akt (S473) and breast cancer cell proliferation. PP242 70-75 AKT serine/threonine kinase 1 Homo sapiens 128-131 22685175-8 2012 The PI3K/mTOR pathway inhibitors rapamycin, PI103, and PP242 also inhibited activated signal transduction and translational machinery proteins of the PI3K/mTOR pathway, suggesting that signal transduction inhibitors targeting this pathway also may have therapeutic relevance for patients with CRLF2-rearranged ALL and merit further preclinical testing. PP242 55-60 mechanistic target of rapamycin kinase Homo sapiens 9-13 22685175-8 2012 The PI3K/mTOR pathway inhibitors rapamycin, PI103, and PP242 also inhibited activated signal transduction and translational machinery proteins of the PI3K/mTOR pathway, suggesting that signal transduction inhibitors targeting this pathway also may have therapeutic relevance for patients with CRLF2-rearranged ALL and merit further preclinical testing. PP242 55-60 mechanistic target of rapamycin kinase Homo sapiens 155-159 22685175-8 2012 The PI3K/mTOR pathway inhibitors rapamycin, PI103, and PP242 also inhibited activated signal transduction and translational machinery proteins of the PI3K/mTOR pathway, suggesting that signal transduction inhibitors targeting this pathway also may have therapeutic relevance for patients with CRLF2-rearranged ALL and merit further preclinical testing. PP242 55-60 cytokine receptor like factor 2 Homo sapiens 293-298 22566604-7 2012 Finally, we show that the mTOR inhibitors rapamycin and pp242 work together with 17-AAG to inhibit leukemia cell growth to a greater extent than either drug alone. PP242 56-61 mechanistic target of rapamycin kinase Homo sapiens 26-30 22556409-2 2012 Newer mTOR inhibitors (like pp242) can overcome feedback activation of AKT in multiple myeloma (MM) cells. PP242 28-33 mechanistic target of rapamycin kinase Homo sapiens 6-10 22556409-4 2012 PP242 induced ERK activation in MM cell lines as well as primary cells. PP242 0-5 mitogen-activated protein kinase 1 Homo sapiens 14-17 22556409-10 2012 Furthermore, ectopic expression of eIF-4E blunted pp242-induced ERK phosphorylation. PP242 50-55 eukaryotic translation initiation factor 4E Homo sapiens 35-41 22556409-10 2012 Furthermore, ectopic expression of eIF-4E blunted pp242-induced ERK phosphorylation. PP242 50-55 mitogen-activated protein kinase 1 Homo sapiens 64-67 22556409-11 2012 Since pp242 was more potent than rapamycin in causing sequestering of eIF-4E, a TORC1/4E-BP1/eIF-4E-mediated mechanism of ERK activation could explain the greater effectiveness of pp242. PP242 6-11 eukaryotic translation initiation factor 4E Homo sapiens 70-76 22556409-11 2012 Since pp242 was more potent than rapamycin in causing sequestering of eIF-4E, a TORC1/4E-BP1/eIF-4E-mediated mechanism of ERK activation could explain the greater effectiveness of pp242. PP242 180-185 eukaryotic translation initiation factor 4E Homo sapiens 70-76 22556409-11 2012 Since pp242 was more potent than rapamycin in causing sequestering of eIF-4E, a TORC1/4E-BP1/eIF-4E-mediated mechanism of ERK activation could explain the greater effectiveness of pp242. PP242 180-185 CREB regulated transcription coactivator 1 Homo sapiens 80-85 22556409-11 2012 Since pp242 was more potent than rapamycin in causing sequestering of eIF-4E, a TORC1/4E-BP1/eIF-4E-mediated mechanism of ERK activation could explain the greater effectiveness of pp242. PP242 180-185 eukaryotic translation initiation factor 4E binding protein 1 Homo sapiens 86-92 22556409-11 2012 Since pp242 was more potent than rapamycin in causing sequestering of eIF-4E, a TORC1/4E-BP1/eIF-4E-mediated mechanism of ERK activation could explain the greater effectiveness of pp242. PP242 180-185 eukaryotic translation initiation factor 4E Homo sapiens 93-99 22556409-11 2012 Since pp242 was more potent than rapamycin in causing sequestering of eIF-4E, a TORC1/4E-BP1/eIF-4E-mediated mechanism of ERK activation could explain the greater effectiveness of pp242. PP242 180-185 mitogen-activated protein kinase 1 Homo sapiens 122-125 22556409-12 2012 Use of MEK inhibitors confirmed ERK activation served as a mechanism of resistance to the lethal effects of pp242. PP242 108-113 mitogen-activated protein kinase kinase 7 Homo sapiens 7-10 22556409-12 2012 Use of MEK inhibitors confirmed ERK activation served as a mechanism of resistance to the lethal effects of pp242. PP242 108-113 mitogen-activated protein kinase 1 Homo sapiens 32-35 22927967-11 2012 Furthermore, MHY1485 induced mTOR activation and correspondingly showed a higher docking score than PP242, a well-known ATP-competitive mTOR inhibitor, in docking simulation. PP242 100-105 mechanistic target of rapamycin kinase Rattus norvegicus 136-140 22223645-1 2012 An intensive recent effort to develop ATP-competitive mTOR inhibitors has resulted in several potent and selective molecules such as Torin1, PP242, KU63794, and WYE354. PP242 141-146 mechanistic target of rapamycin kinase Homo sapiens 54-58 22401294-5 2012 METHODS: LS174T, SW480 and DLD-1 colon cancer cell lines were treated with PP242 an ATP-competitive inhibitor of mTOR, NVP-BEZ235, a dual PI3K/mTOR inhibitor or rapamycin. PP242 75-80 mechanistic target of rapamycin kinase Homo sapiens 113-117 22241218-6 2012 Targeting mTORC1/2 with PP242 was also effective, either as a monotherapy or, more generally, in combination with ABT-737. PP242 24-29 CREB regulated transcription coactivator 1 Mus musculus 10-16 22157018-12 2012 However, transient inhibition of mTORC2 by PP242 completely abolished the phosphorylation of 4EBP1 and decreased basal as well as putrescine-induced AZ1 expression. PP242 43-48 CREB regulated transcription coactivator 2 Mus musculus 33-39 22157018-12 2012 However, transient inhibition of mTORC2 by PP242 completely abolished the phosphorylation of 4EBP1 and decreased basal as well as putrescine-induced AZ1 expression. PP242 43-48 eukaryotic translation initiation factor 4E binding protein 1 Homo sapiens 93-98 22157018-12 2012 However, transient inhibition of mTORC2 by PP242 completely abolished the phosphorylation of 4EBP1 and decreased basal as well as putrescine-induced AZ1 expression. PP242 43-48 ornithine decarboxylase antizyme 1 Homo sapiens 149-152 21615676-4 2011 Here we report that inhibition of the mammalian target of rapamycin (mTOR) pathway by rapamycin or PP242 enhances the efficiency of reprogramming to induced pluripotent stem cells (iPSCs). PP242 99-104 mechanistic target of rapamycin kinase Homo sapiens 38-67 23285076-6 2012 Specific suppression of YB-1 synthesis resulted from inhibition of the mTOR signaling pathway with inhibitor PP242, but not rapamycin. PP242 109-114 Y-box-binding protein 1 Oryctolagus cuniculus 24-28 23285076-6 2012 Specific suppression of YB-1 synthesis resulted from inhibition of the mTOR signaling pathway with inhibitor PP242, but not rapamycin. PP242 109-114 serine/threonine-protein kinase mTOR Oryctolagus cuniculus 71-75 21615676-4 2011 Here we report that inhibition of the mammalian target of rapamycin (mTOR) pathway by rapamycin or PP242 enhances the efficiency of reprogramming to induced pluripotent stem cells (iPSCs). PP242 99-104 mechanistic target of rapamycin kinase Homo sapiens 69-73 21876130-5 2011 We show that the ATP-competitive inhibitor PP242, but not rapamycin, significantly down-regulates cholesterol biosynthesis genes in a 4E-BP1-dependent manner in NIH 3T3 cells, whereas S6 kinase 1 is the dominant regulator in hepatocellular carcinoma cells. PP242 43-48 eukaryotic translation initiation factor 4E binding protein 1 Mus musculus 134-140 21876130-6 2011 To identify other rapamycin-resistant transcriptional outputs of mTOR, we compared the expression profiles of NIH 3T3 cells treated with rapamycin versus PP242. PP242 154-159 mechanistic target of rapamycin kinase Mus musculus 65-69 21592956-6 2011 In contrast, Akt2 activity was significantly reduced, concurrent with inhibition of PRAS40 phosphorylation, in the presence of PP242 and Torin1. PP242 127-132 AKT serine/threonine kinase 2 Homo sapiens 13-17 20686120-3 2010 To assess if the mammalian target of rapamycin within the TORC2 complex could be a better target in MM, we tested a new agent, pp242, which prevents activation of TORC2 as well as TORC1. PP242 127-132 CREB regulated transcription coactivator 2 Homo sapiens 58-63 20861467-10 2010 mTOR overexpression suppressed LPS-induced secretion of IL-6 (P < 0.001), and the mTOR inhibitors rapamycin and PP242 abolished this inhibitory effect of mTOR. PP242 115-120 mechanistic target of rapamycin kinase Mus musculus 85-89 20861467-10 2010 mTOR overexpression suppressed LPS-induced secretion of IL-6 (P < 0.001), and the mTOR inhibitors rapamycin and PP242 abolished this inhibitory effect of mTOR. PP242 115-120 mechanistic target of rapamycin kinase Mus musculus 85-89 20686120-3 2010 To assess if the mammalian target of rapamycin within the TORC2 complex could be a better target in MM, we tested a new agent, pp242, which prevents activation of TORC2 as well as TORC1. PP242 127-132 CREB regulated transcription coactivator 2 Homo sapiens 163-168 20686120-3 2010 To assess if the mammalian target of rapamycin within the TORC2 complex could be a better target in MM, we tested a new agent, pp242, which prevents activation of TORC2 as well as TORC1. PP242 127-132 CREB regulated transcription coactivator 1 Homo sapiens 180-185 20686120-4 2010 Although comparable to rapamycin against phosphorylation of the TORC1 substrates p70S6kinase and 4E-BP-1, pp242 could also inhibit phosphorylation of AKT on serine 473, a TORC2 substrate, while rapamycin was ineffective. PP242 106-111 CREB regulated transcription coactivator 1 Homo sapiens 64-69 20686120-4 2010 Although comparable to rapamycin against phosphorylation of the TORC1 substrates p70S6kinase and 4E-BP-1, pp242 could also inhibit phosphorylation of AKT on serine 473, a TORC2 substrate, while rapamycin was ineffective. PP242 106-111 AKT serine/threonine kinase 1 Homo sapiens 150-153 20686120-4 2010 Although comparable to rapamycin against phosphorylation of the TORC1 substrates p70S6kinase and 4E-BP-1, pp242 could also inhibit phosphorylation of AKT on serine 473, a TORC2 substrate, while rapamycin was ineffective. PP242 106-111 CREB regulated transcription coactivator 2 Homo sapiens 171-176 20072130-3 2010 We compared rapamycin with PP242, an inhibitor of the active site of mTOR in both TORC1 and TORC2 (hereafter referred to as TORC1/2), in models of acute leukemia harboring the Philadelphia chromosome (Ph) translocation. PP242 27-32 mechanistic target of rapamycin kinase Homo sapiens 69-73 20227039-4 2010 By using an active site inhibitor of mTOR, PP242, we show a marked therapeutic response in rapamycin-resistant tumors. PP242 43-48 mechanistic target of rapamycin kinase Homo sapiens 37-41 20227039-5 2010 The therapeutic benefit of PP242 is mediated through inhibition of mTORC1-dependent 4EBP-eIF4E hyperactivation. PP242 27-32 CREB regulated transcription coactivator 1 Mus musculus 67-73 20227039-5 2010 The therapeutic benefit of PP242 is mediated through inhibition of mTORC1-dependent 4EBP-eIF4E hyperactivation. PP242 27-32 eukaryotic translation initiation factor 4E Homo sapiens 89-94 20072130-3 2010 We compared rapamycin with PP242, an inhibitor of the active site of mTOR in both TORC1 and TORC2 (hereafter referred to as TORC1/2), in models of acute leukemia harboring the Philadelphia chromosome (Ph) translocation. PP242 27-32 CREB regulated transcription coactivator 1 Homo sapiens 82-87 20072130-3 2010 We compared rapamycin with PP242, an inhibitor of the active site of mTOR in both TORC1 and TORC2 (hereafter referred to as TORC1/2), in models of acute leukemia harboring the Philadelphia chromosome (Ph) translocation. PP242 27-32 CREB regulated transcription coactivator 2 Homo sapiens 92-97 20072130-3 2010 We compared rapamycin with PP242, an inhibitor of the active site of mTOR in both TORC1 and TORC2 (hereafter referred to as TORC1/2), in models of acute leukemia harboring the Philadelphia chromosome (Ph) translocation. PP242 27-32 CREB regulated transcription coactivator 2 Homo sapiens 124-131 19209957-8 2009 We investigated mTOR signaling in cells and animals with two novel and specific mTOR kinase domain inhibitors (TORKinibs). PP242 111-120 mechanistic target of rapamycin kinase Homo sapiens 16-20 19209957-8 2009 We investigated mTOR signaling in cells and animals with two novel and specific mTOR kinase domain inhibitors (TORKinibs). PP242 111-120 mechanistic target of rapamycin kinase Homo sapiens 80-84 18602931-9 2009 The pharmacological profile for P2X antagonists to inhibit [3H]A-804598 binding correlated with their ability to block functional activation of P2X7 receptors (r=0.95, P<0.05). PP242 32-35 purinergic receptor P2X 7 Homo sapiens 144-148