PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 30650200-0 2019 Targeting mTORC1/2 with OSI-027 inhibits proliferation and migration of keloid keratinocytes. OSI 027 24-31 CREB regulated transcription coactivator 1 Mus musculus 10-16 30650200-6 2019 Further, OSI-027 almost completely blocked the phosphorylation of the mTORC1 substrates, S6K1, S6 and 4EBP1, and the mTORC2 substrate, AKT, at Ser-473. OSI 027 9-16 CREB regulated transcription coactivator 1 Mus musculus 70-76 30650200-7 2019 The OSI-027 treatment of keloid keratinocytes showed more effectively inhibited cell proliferation and migration compared to the mTORC1 inhibitor, rapamycin. OSI 027 4-11 CREB regulated transcription coactivator 1 Mus musculus 129-135 30650200-8 2019 Moreover, restoring mTORC1 activation by the introduction of the constitutively active S6K1 only partly alleviated OSI-027-induced inhibition of keloid keratinocytes. OSI 027 115-122 CREB regulated transcription coactivator 1 Mus musculus 20-26 30650200-10 2019 Together, our results imply that concurrent targeting of mTORC1/2 by OSI-027 potently inhibits the proliferation and the migration of keloid keratinocytes. OSI 027 69-76 CREB regulated transcription coactivator 1 Mus musculus 57-63 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. OSI 027 60-67 CREB regulated transcription coactivator 1 Mus musculus 30-36 27212159-11 2016 CONCLUSIONS: Dual mTORC1/mTORC2 inhibitors such as OSI-027 are promising therapeutic agents in combination with 5-FU for the treatment of human gallbladder cancer. OSI 027 51-58 CREB regulated transcription coactivator 1 Mus musculus 18-24 27002938-0 2016 A first in man, dose-finding study of the mTORC1/mTORC2 inhibitor OSI-027 in patients with advanced solid malignancies. OSI 027 66-73 CREB regulated transcription coactivator 1 Mus musculus 42-48 26284306-0 2015 The Antipancreatic Cancer Activity of OSI-027, a Potent and Selective Inhibitor of mTORC1 and mTORC2. OSI 027 38-45 CREB regulated transcription coactivator 1 Mus musculus 83-89 26284306-5 2015 At the molecular level, OSI-027 treatment blocked mTORC1 and mTORC2 activation simultaneously, without affecting ERK-mitogen-activated protein kinase activation. OSI 027 24-31 CREB regulated transcription coactivator 1 Mus musculus 50-56 26213847-2 2015 In this study, we investigated the in vitro efficacy of OSI-027, a selective inhibitor of mammalian target of rapamycin complex 1 (mTORC1) and mTORC2, to treat PDAC cell lines alone, and in combination with gemcitabine (GEM). OSI 027 56-63 CREB regulated transcription coactivator 1 Mus musculus 131-137 26026051-4 2015 In this study, we examined the interaction between the dual mTORC1/2 inhibitor OSI-027 and doxorubicin in vitro and in vivo. OSI 027 79-86 CREB regulated transcription coactivator 1 Mus musculus 60-66 26026051-5 2015 OSI-027 was found to reduce phosphorylation of both mTORC1 and mTORC2 substrates, including 4E-BP1, p70S6K, and AKT (Ser473), and inhibit HCC cell proliferation. OSI 027 0-7 CREB regulated transcription coactivator 1 Mus musculus 52-58 26026051-11 2015 Our findings provide a rationale for dual mTORC1/mTORC2 inhibitors, such as OSI-027, as monotherapy or in combination with cytotoxic agents to treat HCC. OSI 027 76-83 CREB regulated transcription coactivator 1 Mus musculus 42-48 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. OSI 027 80-87 CREB regulated transcription coactivator 1 Mus musculus 35-41 22080480-7 2012 Moreover, OSI-027 inhibited phosphorylation of mTORC1 and mTORC2 substrates, up-regulated Puma, and induced regressions in Jeko xenografts. OSI 027 10-17 CREB regulated transcription coactivator 1 Mus musculus 47-53 21673091-0 2011 Preclinical characterization of OSI-027, a potent and selective inhibitor of mTORC1 and mTORC2: distinct from rapamycin. OSI 027 32-39 CREB regulated transcription coactivator 1 Mus musculus 77-83 21673091-4 2011 Here, we report the preclinical characterization of OSI-027, a selective and potent dual inhibitor of mTORC1 and mTORC2 with biochemical IC(50) values of 22 nmol/L and 65 nmol/L, respectively. OSI 027 52-59 CREB regulated transcription coactivator 1 Mus musculus 102-108 21673091-6 2011 OSI-027 inhibits phosphorylation of the mTORC1 substrates 4E-BP1 and S6K1 as well as the mTORC2 substrate AKT in diverse cancer models in vitro and in vivo. OSI 027 0-7 CREB regulated transcription coactivator 1 Mus musculus 40-46 21415215-8 2011 Inhibition of the mTOR catalytic site with OSI-027 results in suppression of both mTORC2 and RI-mTORC1 complexes and elicits much more potent antileukemic responses than selective mTORC1 targeting with rapamycin. OSI 027 43-50 CREB regulated transcription coactivator 1 Mus musculus 96-102 21363918-4 2011 ATP-competitive inhibitors OSI-027 and OXA-01 targeted both mTORC1 and mTORC2 signaling in vitro and in vivo, unlike rapamycin that only inhibited mTORC1 signaling. OSI 027 27-34 CREB regulated transcription coactivator 1 Mus musculus 60-66 20699667-3 2010 We have recently shown that dual targeting of mTORC1 and mTORC2 complexes using a catalytic mTOR inhibitor, OSI-027, results in generation of potent antileukemic effects against BCR-ABL transformed cells. OSI 027 108-115 CREB regulated transcription coactivator 1 Mus musculus 46-52 20616057-4 2010 Our studies establish that a unique dual mTORC2/mTORC1 inhibitor, OSI-027, induces potent suppressive effects on primitive leukemic progenitors from CML patients and generates antileukemic responses in cells expressing the T315I-BCR-ABL mutation, which is refractory to all BCR-ABL kinase inhibitors currently in clinical use. OSI 027 66-73 CREB regulated transcription coactivator 1 Mus musculus 48-54 33222668-7 2021 At the molecular level, OSI-027 simultaneously blocked mTORC1 and mTORC2 activation, and resulted in the downregulation of phosphor-Akt, phpspho-p70S6k, phosphor-4EBP1, cyclin D1, and cyclin-dependent kinase4 (CDK4). OSI 027 24-31 CREB regulated transcription coactivator 1 Mus musculus 55-61 33222668-10 2021 In summary, our results suggest that dual mTORC1/mTORC2 inhibitors (e.g., OSI-027) should be further investigated as a potential valuable treatment for gastric cancer. OSI 027 74-81 CREB regulated transcription coactivator 1 Mus musculus 42-48