PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 21651476-8 2011 This review mainly reports the recently discovered mTOR ATP-competitive inhibitors in terms of medicinal chemistry, classified by their chemical structures, focusing on SAR and modelling studies that led to the discovery of very potent and selective agents, such as AZD-8055, OSI-027 and INK128, already entered clinical trials, or WYE-132, Torin1 and others in preclinical studies. WYE 125132 332-339 mechanistic target of rapamycin kinase Homo sapiens 51-55 20233713-2 2010 Here, employing an mTOR active-site inhibitor WYE-125132 (WYE-132), we have performed quantitative phospho-proteomics and identified a Ser-75-containing phosphopeptide from Maf1, a known repressor of RNA polymerase III (Pol III) transcription. WYE 125132 46-56 mechanistic target of rapamycin kinase Homo sapiens 19-23 20233713-2 2010 Here, employing an mTOR active-site inhibitor WYE-125132 (WYE-132), we have performed quantitative phospho-proteomics and identified a Ser-75-containing phosphopeptide from Maf1, a known repressor of RNA polymerase III (Pol III) transcription. WYE 125132 46-56 MAF1 homolog, negative regulator of RNA polymerase III Homo sapiens 173-177 20233713-4 2010 WYE-132-induced Maf1 dephosphorylation correlated with its accumulation in the nucleus and a marked decline in the cellular levels of pre-tRNAs. WYE 125132 0-7 MAF1 homolog, negative regulator of RNA polymerase III Homo sapiens 16-20 26293898-6 2016 Interestingly, introducing a constitutively active AKT (caAKT), which restored mTORC1/2 activation in WYE-132-treated ovarian cancer cells, only mitigated (but not abolished) WYE-132-mediated growth inhibition and apoptosis. WYE 125132 175-182 AKT serine/threonine kinase 1 Homo sapiens 51-54 26293898-7 2016 Further studies showed that WYE-132 inhibited sphingosine kinase-1 (SphK1) activity, leading to pro-apoptotic ceramide production in ovarian cancer cells. WYE 125132 28-35 sphingosine kinase 1 Homo sapiens 46-66 26293898-7 2016 Further studies showed that WYE-132 inhibited sphingosine kinase-1 (SphK1) activity, leading to pro-apoptotic ceramide production in ovarian cancer cells. WYE 125132 28-35 sphingosine kinase 1 Homo sapiens 68-73 26293898-8 2016 Meanwhile, WYE-132-induced cytotoxicity against ovarian cancer cells was inhibited by sphingosine-1-phosphate (S1P) but was aggravated by SphK1 inhibitor SKI-II or C6 ceramide. WYE 125132 11-18 sphingosine kinase 1 Homo sapiens 138-143 26293898-10 2016 These results demonstrate that WYE-132 inhibits ovarian cancer cell proliferation through mTOR-dependent and mTOR-independent mechanisms and indicate a potential value of WYE-132 in ovarian cancer treatment. WYE 125132 31-38 mechanistic target of rapamycin kinase Homo sapiens 90-94 26293898-10 2016 These results demonstrate that WYE-132 inhibits ovarian cancer cell proliferation through mTOR-dependent and mTOR-independent mechanisms and indicate a potential value of WYE-132 in ovarian cancer treatment. WYE 125132 31-38 mechanistic target of rapamycin kinase Homo sapiens 109-113 20068177-0 2010 Beyond rapalog therapy: preclinical pharmacology and antitumor activity of WYE-125132, an ATP-competitive and specific inhibitor of mTORC1 and mTORC2. WYE 125132 75-85 CREB regulated transcription coactivator 1 Mus musculus 132-138 20068177-0 2010 Beyond rapalog therapy: preclinical pharmacology and antitumor activity of WYE-125132, an ATP-competitive and specific inhibitor of mTORC1 and mTORC2. WYE 125132 75-85 CREB regulated transcription coactivator 2 Mus musculus 143-149 20068177-3 2010 Here, we report WYE-125132 (WYE-132), a highly potent, ATP-competitive, and specific mTOR kinase inhibitor (IC(50): 0.19 +/- 0.07 nmol/L; >5,000-fold selective versus PI3Ks). WYE 125132 16-26 mechanistic target of rapamycin kinase Homo sapiens 85-89 20068177-4 2010 WYE-132 inhibited mTORC1 and mTORC2 in diverse cancer models in vitro and in vivo. WYE 125132 0-7 CREB regulated transcription coactivator 1 Mus musculus 18-24 20068177-4 2010 WYE-132 inhibited mTORC1 and mTORC2 in diverse cancer models in vitro and in vivo. WYE 125132 0-7 CREB regulated transcription coactivator 2 Mus musculus 29-35 26293898-0 2016 The anti-ovarian cancer activity by WYE-132, a mTORC1/2 dual inhibitor. WYE 125132 36-43 CREB regulated transcription coactivator 1 Mus musculus 47-53 26293898-6 2016 Interestingly, introducing a constitutively active AKT (caAKT), which restored mTORC1/2 activation in WYE-132-treated ovarian cancer cells, only mitigated (but not abolished) WYE-132-mediated growth inhibition and apoptosis. WYE 125132 102-109 AKT serine/threonine kinase 1 Homo sapiens 51-54