Target Information
Target General Infomation | |||||
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Target ID |
T75243
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Former ID |
TTDS00265
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Target Name |
Serine/threonine-protein kinase mTOR
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Gene Name |
MTOR
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Synonyms |
FK506-binding protein 12-rapamycin complex-associated protein 1; FKBP-rapamycin associated protein; FKBP12-rapamycin complex-associated protein; FRAP; FRAP1; Mammalian target of rapamycin; RAPT1; Rapamycin target protein; TOR kinase; Target of rapamycin; mTOR; MTOR
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Target Type |
Successful
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Disease | Advanced solid tumor; Non-hodgkin's lymphoma [ICD9: 140-199, 200, 202, 202.8, 210-229; ICD10: C00-C75, C7A, C7B, C81-C86, C82-C85, D10-D36, D3A] | ||||
Advanced kidney cancer [ICD9: 189; ICD10: C64] | |||||
Bladder cancer [ICD9: 188; ICD10: C67] | |||||
Cancer [ICD9: 140-229; ICD10: C00-C96] | |||||
Coronary artery restenosis; Multiple myeloma [ICD9:203; ICD10: I51.89, C90] | |||||
Dutch elm disease [ICD10: B81-B83] | |||||
Endometrial cancer [ICD9: 182; ICD10: C54.1] | |||||
Inflammatory disease [ICD9: 140-229, 147, 173, 573.3, 710-719; ICD10: C11, C44, K75.9, M00-M25] | |||||
Multiple myeloma [ICD9: 203; ICD10: C90] | |||||
Non-hodgkin's lymphoma [ICD10: C85] | |||||
Non-small cell lung cancer [ICD10: C33-C34] | |||||
Organ rejection [ICD9: 279.5, 996; ICD10: D89.8, T86] | |||||
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89] | |||||
Pancreatic cancer [ICD9: 140-199, 140-229, 157, 210-229; ICD10: C25] | |||||
Renal cancer [ICD9: 140-229, 189; ICD10: C64] | |||||
Restenosis [ICD10: I51.89] | |||||
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48] | |||||
Sarcoma [ICD9: 202.8; ICD10: C81-C86] | |||||
Solid cancer; Lymphoma [ICD9: 140-199, 140-229, 202.8; ICD10: C81-C86] | |||||
Transplant rejection [ICD9: 279.5, 996; ICD10: D89.8, T86] | |||||
Ulcerative colitis [ICD9: 556; ICD10: K51] | |||||
Function |
Serine/threonine protein kinase which is a central regulator of cellular metabolism, growth and survival in response to hormones, growth factors, nutrients, energy and stress signals. MTOR directly or indirectly regulates the phosphorylation of at least 800 proteins. Functions as part of 2 structurally and functionally distinct signaling complexes mTORC1 and mTORC2 (mTOR complex 1 and 2). Activated mTORC1 up-regulates protein synthesis by phosphorylating key regulators of mRNA translation and ribosome synthesis. This includes phosphorylation of EIF4EBP1 and release of its inhibition toward the elongation initiation factor 4E (eiF4E). Moreover, phosphorylates and activates RPS6KB1 and RPS6KB2 that promote protein synthesis by modulating the activity of their downstream targets including ribosomal protein S6, eukaryotic translation initiation factor EIF4B, and the inhibitor of translation initiation PDCD4. Stimulates the pyrimidine biosynthesis pathway, both by acute regulation through RPS6KB1- mediated phosphorylation of the biosynthetic enzyme CAD, and delayed regulation, through transcriptional enhancement of the pentose phosphate pathway which produces 5-phosphoribosyl-1- pyrophosphate (PRPP), an allosteric activatorof CAD at a later step in synthesis, this function is dependent on the mTORC1 complex. Regulates ribosome synthesis by activating RNA polymerase III-dependent transcription through phosphorylation and inhibition of MAF1 an RNA polymerase III-repressor. In parallel to protein synthesis, also regulates lipid synthesis through SREBF1/SREBP1 and LPIN1. To maintain energy homeostasis mTORC1 may also regulate mitochondrial biogenesis through regulation of PPARGC1A. mTORC1 also negatively regulates autophagy through phosphorylation of ULK1. Under nutrient sufficiency, phosphorylates ULK1 at 'Ser- 758', disrupting the interaction with AMPK and preventing activation of ULK1. Also prevents autophagy through phosphorylation of the autophagy inhibitor DAP. mTORC1 exerts a feedback control on upstreamgrowth factor signaling that includes phosphorylation and activation of GRB10 a INSR-dependent signaling suppressor. Among other potential targets mTORC1 may phosphorylate CLIP1 and regulate microtubules. As part of the mTORC2 complex MTOR may regulate other cellular processes including survival and organization of the cytoskeleton. Plays a critical role in the phosphorylation at 'Ser-473' of AKT1, a pro-survival effector of phosphoinositide 3-kinase, facilitating its activation by PDK1. mTORC2 may regulate the actin cytoskeleton, through phosphorylation of PRKCA, PXN and activation of the Rho-type guanine nucleotide exchange factors RHOA and RAC1A or RAC1B. mTORC2 also regulates the phosphorylation of SGK1 at 'Ser-422'.
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BioChemical Class |
Kinase
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Target Validation |
T75243
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UniProt ID | |||||
EC Number |
EC 2.7.11.1
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Sequence |
MLGTGPAAATTAATTSSNVSVLQQFASGLKSRNEETRAKAAKELQHYVTMELREMSQEES
TRFYDQLNHHIFELVSSSDANERKGGILAIASLIGVEGGNATRIGRFANYLRNLLPSNDP VVMEMASKAIGRLAMAGDTFTAEYVEFEVKRALEWLGADRNEGRRHAAVLVLRELAISVP TFFFQQVQPFFDNIFVAVWDPKQAIREGAVAALRACLILTTQREPKEMQKPQWYRHTFEE AEKGFDETLAKEKGMNRDDRIHGALLILNELVRISSMEGERLREEMEEITQQQLVHDKYC KDLMGFGTKPRHITPFTSFQAVQPQQSNALVGLLGYSSHQGLMGFGTSPSPAKSTLVESR CCRDLMEEKFDQVCQWVLKCRNSKNSLIQMTILNLLPRLAAFRPSAFTDTQYLQDTMNHV LSCVKKEKERTAAFQALGLLSVAVRSEFKVYLPRVLDIIRAALPPKDFAHKRQKAMQVDA TVFTCISMLARAMGPGIQQDIKELLEPMLAVGLSPALTAVLYDLSRQIPQLKKDIQDGLL KMLSLVLMHKPLRHPGMPKGLAHQLASPGLTTLPEASDVGSITLALRTLGSFEFEGHSLT QFVRHCADHFLNSEHKEIRMEAARTCSRLLTPSIHLISGHAHVVSQTAVQVVADVLSKLL VVGITDPDPDIRYCVLASLDERFDAHLAQAENLQALFVALNDQVFEIRELAICTVGRLSS MNPAFVMPFLRKMLIQILTELEHSGIGRIKEQSARMLGHLVSNAPRLIRPYMEPILKALI LKLKDPDPDPNPGVINNVLATIGELAQVSGLEMRKWVDELFIIIMDMLQDSSLLAKRQVA LWTLGQLVASTGYVVEPYRKYPTLLEVLLNFLKTEQNQGTRREAIRVLGLLGALDPYKHK VNIGMIDQSRDASAVSLSESKSSQDSSDYSTSEMLVNMGNLPLDEFYPAVSMVALMRIFR DQSLSHHHTMVVQAITFIFKSLGLKCVQFLPQVMPTFLNVIRVCDGAIREFLFQQLGMLV SFVKSHIRPYMDEIVTLMREFWVMNTSIQSTIILLIEQIVVALGGEFKLYLPQLIPHMLR VFMHDNSPGRIVSIKLLAAIQLFGANLDDYLHLLLPPIVKLFDAPEAPLPSRKAALETVD RLTESLDFTDYASRIIHPIVRTLDQSPELRSTAMDTLSSLVFQLGKKYQIFIPMVNKVLV RHRINHQRYDVLICRIVKGYTLADEEEDPLIYQHRMLRSGQGDALASGPVETGPMKKLHV STINLQKAWGAARRVSKDDWLEWLRRLSLELLKDSSSPSLRSCWALAQAYNPMARDLFNA AFVSCWSELNEDQQDELIRSIELALTSQDIAEVTQTLLNLAEFMEHSDKGPLPLRDDNGI VLLGERAAKCRAYAKALHYKELEFQKGPTPAILESLISINNKLQQPEAAAGVLEYAMKHF GELEIQATWYEKLHEWEDALVAYDKKMDTNKDDPELMLGRMRCLEALGEWGQLHQQCCEK WTLVNDETQAKMARMAAAAAWGLGQWDSMEEYTCMIPRDTHDGAFYRAVLALHQDLFSLA QQCIDKARDLLDAELTAMAGESYSRAYGAMVSCHMLSELEEVIQYKLVPERREIIRQIWW ERLQGCQRIVEDWQKILMVRSLVVSPHEDMRTWLKYASLCGKSGRLALAHKTLVLLLGVD PSRQLDHPLPTVHPQVTYAYMKNMWKSARKIDAFQHMQHFVQTMQQQAQHAIATEDQQHK QELHKLMARCFLKLGEWQLNLQGINESTIPKVLQYYSAATEHDRSWYKAWHAWAVMNFEA VLHYKHQNQARDEKKKLRHASGANITNATTAATTAATATTTASTEGSNSESEAESTENSP TPSPLQKKVTEDLSKTLLMYTVPAVQGFFRSISLSRGNNLQDTLRVLTLWFDYGHWPDVN EALVEGVKAIQIDTWLQVIPQLIARIDTPRPLVGRLIHQLLTDIGRYHPQALIYPLTVAS KSTTTARHNAANKILKNMCEHSNTLVQQAMMVSEELIRVAILWHEMWHEGLEEASRLYFG ERNVKGMFEVLEPLHAMMERGPQTLKETSFNQAYGRDLMEAQEWCRKYMKSGNVKDLTQA WDLYYHVFRRISKQLPQLTSLELQYVSPKLLMCRDLELAVPGTYDPNQPIIRIQSIAPSL QVITSKQRPRKLTLMGSNGHEFVFLLKGHEDLRQDERVMQLFGLVNTLLANDPTSLRKNL SIQRYAVIPLSTNSGLIGWVPHCDTLHALIRDYREKKKILLNIEHRIMLRMAPDYDHLTL MQKVEVFEHAVNNTAGDDLAKLLWLKSPSSEVWFDRRTNYTRSLAVMSMVGYILGLGDRH PSNLMLDRLSGKILHIDFGDCFEVAMTREKFPEKIPFRLTRMLTNAMEVTGLDGNYRITC HTVMEVLREHKDSVMAVLEAFVYDPLLNWRLMDTNTKGNKRSRTRTDSYSAGQSVEILDG VELGEPAHKKTGTTVPESIHSFIGDGLVKPEALNKKAIQIINRVRDKLTGRDFSHDDTLD VPTQVELLIKQATSHENLCQCYIGWCPFW |
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Drugs and Mode of Action | |||||
Drug(s) | Everolimus | Drug Info | Approved | Renal cancer | [530677], [541186] |
Novolimus | Drug Info | Approved | Restenosis | [524566], [549817] | |
Rapamycin | Drug Info | Approved | Coronary artery restenosis; Multiple myeloma | [545206], [551871] | |
Sirolimus | Drug Info | Approved | Organ rejection | [536361], [541290] | |
Temsirolimus | Drug Info | Approved | Renal cancer | [532990], [541190] | |
Zotarolimus | Drug Info | Approved | Cancer | [522199], [542890], [551871] | |
Everolimus | Drug Info | Phase 3 | Advanced kidney cancer | [530677], [541186] | |
Ridaforolimus | Drug Info | Phase 3 | Sarcoma | [531692], [542809] | |
AZD2014 | Drug Info | Phase 2 | Cancer | [524214], [542674] | |
BEZ235 | Drug Info | Phase 2 | Solid tumours | [542866], [548508] | |
GDC-0980/RG7422 | Drug Info | Phase 2 | Non-hodgkin's lymphoma | [551603] | |
LY3023414 | Drug Info | Phase 2 | Cancer | [525317] | |
OSI-027 | Drug Info | Phase 2 | Renal cancer | [531516] | |
PF-04691502 | Drug Info | Phase 2 | Endometrial cancer | [523615], [542851] | |
PF-05212384 | Drug Info | Phase 2 | Cancer | [533132], [542855] | |
SAR245409 | Drug Info | Phase 2 | Cancer | [524422] | |
BGT226 | Drug Info | Phase 1/2 | Solid tumours | [531639], [542867] | |
CC-223 | Drug Info | Phase 1/2 | Solid tumours | [523130] | |
Sirolimus | Drug Info | Phase 1/2 | Dutch elm disease | [536361], [541290] | |
BI 860585 | Drug Info | Phase 1 | Solid tumours | [549503] | |
DS-3078 | Drug Info | Phase 1 | Solid cancer; Lymphoma | [523889] | |
DS-7423 | Drug Info | Phase 1 | Solid tumours | [549261] | |
GDC-0349 | Drug Info | Phase 1 | Non-hodgkin's lymphoma | [523484] | |
GDC-0980 | Drug Info | Phase 1 | Advanced solid tumor; Non-hodgkin's lymphoma | [550796] | |
INK128 | Drug Info | Phase 1 | Multiple myeloma | [542848], [551038] | |
PQR309 | Drug Info | Phase 1 | Pain | [543099] | |
PWT-33597 | Drug Info | Phase 1 | Cancer | [523571] | |
SAR245409/MSC1936369B combination therapy | Drug Info | Phase 1 | Solid tumours | [523487] | |
VS-5584 | Drug Info | Phase 1 | Solid tumours | [532167], [543098] | |
ME-344 | Drug Info | Preclinical | Cancer | [542878], [549411] | |
KD032 | Drug Info | Discontinued in Phase 2 | Non-small cell lung cancer | [548607] | |
AZD8055 | Drug Info | Discontinued in Phase 1/2 | Cancer | [542689], [548781] | |
KD032 | Drug Info | Discontinued in Phase 1/2 | Pancreatic cancer | [548607] | |
TAFA-93 | Drug Info | Discontinued in Phase 1 | Transplant rejection | [547739] | |
SCR-44001 | Drug Info | Terminated | Cancer | [548121] | |
Inhibitor | (4-(6-morpholino-9H-purin-2-yl)phenyl)methanol | Drug Info | [530563] | ||
2-(2-Methyl-morpholin-4-yl)-benzo[h]chromen-4-one | Drug Info | [527386] | |||
2-(6-morpholino-9H-purin-2-yl)phenol | Drug Info | [530563] | |||
2-chloro-N-(6-cyanopyridin-3-yl)propanamide | Drug Info | [530099] | |||
2-Morpholin-4-yl-pyrimido[2,1-a]isoquinolin-4-one | Drug Info | [527386] | |||
3-(6-morpholino-9H-purin-2-yl)phenol | Drug Info | [530563] | |||
4-(2-(1H-indol-6-yl)-9H-purin-6-yl)morpholine | Drug Info | [530563] | |||
4-(2-(thiophen-2-yl)-9H-purin-6-yl)morpholine | Drug Info | [530563] | |||
4-(2-(thiophen-3-yl)-9H-purin-6-yl)morpholine | Drug Info | [530563] | |||
4-(6-morpholino-9H-purin-2-yl)phenol | Drug Info | [530563] | |||
AP-21967 | Drug Info | [528725] | |||
AR-mTOR-26 | Drug Info | [543556] | |||
AZD2014 | Drug Info | [532573] | |||
AZD8055 | Drug Info | [550288] | |||
BI 860585 | Drug Info | [550087] | |||
C-16-(S)-3-methylindolerapamycin | Drug Info | [528725] | |||
CU-906 | Drug Info | [543556] | |||
Dual PI3K-alpha/mTOR inhibitors | Drug Info | [543556] | |||
Dual PI3K/mTOR inhibitors | Drug Info | [543556] | |||
EC-0565 | Drug Info | [543556] | |||
EM-101 | Drug Info | [543556] | |||
Everolimus | Drug Info | [537621] | |||
GDC-0349 | Drug Info | [532820] | |||
HM-5016699 | Drug Info | [543556] | |||
INK128 | Drug Info | [551038] | |||
LY-293646 | Drug Info | [527386] | |||
Macrolide derivative | Drug Info | [527216] | |||
ME-344 | Drug Info | [550487] | |||
MTOR inhibitors | Drug Info | [543556] | |||
Novolimus | Drug Info | [543556] | |||
OSI-027 | Drug Info | [537633] | |||
OXA-01 | Drug Info | [543556] | |||
P-2281 | Drug Info | [543556] | |||
P-6915 | Drug Info | [543556] | |||
PF-03772304 | Drug Info | [532819] | |||
PF-05094037 | Drug Info | [543556] | |||
PP-242 | Drug Info | [529744] | |||
PP121 | Drug Info | [529744] | |||
PQR309 | Drug Info | [543556] | |||
Rapamycin | Drug Info | [537114] | |||
Rapamycin complexed with immunophilin FKBP12 | Drug Info | [535318] | |||
Ridaforolimus | Drug Info | [549718], [549940] | |||
SAR245409 | Drug Info | [551615] | |||
SB-2280 | Drug Info | [543556] | |||
SB-2343 | Drug Info | [543556] | |||
SCR-44001 | Drug Info | [531187] | |||
Sirolimus | Drug Info | [535660] | |||
TAFA-93 | Drug Info | [550877] | |||
Temsirolimus | Drug Info | [532990], [551871] | |||
torin 1 | Drug Info | [531173] | |||
VE-822 | Drug Info | [532144] | |||
X-387 | Drug Info | [543556] | |||
Modulator | BEZ235 | Drug Info | |||
BGT226 | Drug Info | [531639] | |||
CC-223 | Drug Info | [533206] | |||
DS-3078 | Drug Info | [549970] | |||
DS-7423 | Drug Info | [532664] | |||
EC-0845 | Drug Info | [543556] | |||
GDC-0980 | Drug Info | [531658] | |||
GDC-0980/RG7422 | Drug Info | [543556] | |||
KD032 | Drug Info | [543556] | |||
LY3023414 | Drug Info | ||||
PF-04691502 | Drug Info | ||||
PF-05212384 | Drug Info | [533132] | |||
PWT-33597 | Drug Info | ||||
SAR245409/MSC1936369B combination therapy | Drug Info | [543556] | |||
SX-MTR1 | Drug Info | [543556] | |||
VS-5584 | Drug Info | [532167] | |||
Zotarolimus | Drug Info | [529484] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
Pathways | |||||
KEGG Pathway | ErbB signaling pathway | ||||
HIF-1 signaling pathway | |||||
mTOR signaling pathway | |||||
PI3K-Akt signaling pathway | |||||
AMPK signaling pathway | |||||
Insulin signaling pathway | |||||
Thyroid hormone signaling pathway | |||||
Adipocytokine signaling pathway | |||||
Type II diabetes mellitus | |||||
Pathways in cancer | |||||
Proteoglycans in cancer | |||||
MicroRNAs in cancer | |||||
Glioma | |||||
Prostate cancer | |||||
Acute myeloid leukemia | |||||
Central carbon metabolism in cancer | |||||
Choline metabolism in cancer | |||||
PANTHER Pathway | Hypoxia response via HIF activation | ||||
Interleukin signaling pathway | |||||
Pathway Interaction Database | IL4-mediated signaling events | ||||
Signaling events mediated by Hepatocyte Growth Factor Receptor (c-Met) | |||||
IL12-mediated signaling events | |||||
CDC42 signaling events | |||||
LKB1 signaling events | |||||
Regulation of Telomerase | |||||
mTOR signaling pathway | |||||
CXCR4-mediated signaling events | |||||
EGFR-dependent Endothelin signaling events | |||||
IL2 signaling events mediated by PI3K | |||||
IFN-gamma pathway | |||||
ErbB1 downstream signaling | |||||
ErbB2/ErbB3 signaling events | |||||
CXCR3-mediated signaling events | |||||
Class I PI3K signaling events mediated by Akt | |||||
PathWhiz Pathway | Leucine Stimulation on Insulin Signaling | ||||
Reactome | PIP3 activates AKT signaling | ||||
Macroautophagy | |||||
mTORC1-mediated signalling | |||||
HSF1-dependent transactivation | |||||
CD28 dependent PI3K/Akt signaling | |||||
VEGFR2 mediated vascular permeability | |||||
TP53 Regulates Metabolic Genes | |||||
Constitutive Signaling by AKT1 E17K in Cancer | |||||
WikiPathways | ErbB Signaling Pathway | ||||
Senescence and Autophagy in Cancer | |||||
Interferon type I signaling pathways | |||||
Insulin Signaling | |||||
EGF/EGFR Signaling Pathway | |||||
Wnt Signaling Pathway Netpath | |||||
Extracellular vesicle-mediated signaling in recipient cells | |||||
Cardiac Hypertrophic Response | |||||
Signaling by Type 1 Insulin-like Growth Factor 1 Receptor (IGF1R) | |||||
PIP3 activates AKT signaling | |||||
Polycystic Kidney Disease Pathway | |||||
Alpha 6 Beta 4 signaling pathway | |||||
BDNF signaling pathway | |||||
Oncostatin M Signaling Pathway | |||||
Prostate Cancer | |||||
TSLP Signaling Pathway | |||||
FSH signaling pathway | |||||
Leptin signaling pathway | |||||
TSH signaling pathway | |||||
RANKL/RANK Signaling Pathway | |||||
SREBF and miR33 in cholesterol and lipid homeostasis | |||||
Integrated Breast Cancer Pathway | |||||
SREBP signalling | |||||
Signaling by Insulin receptor | |||||
Costimulation by the CD28 family | |||||
Type II diabetes mellitus | |||||
MicroRNAs in cardiomyocyte hypertrophy | |||||
TOR Signaling | |||||
AMPK Signaling | |||||
References | |||||
Ref 522199 | ClinicalTrials.gov (NCT00589927) Triple Versus Dual Antiplatelet Therapy After ABT578-Eluting Stent. U.S. National Institutes of Health. | ||||
Ref 523130 | ClinicalTrials.gov (NCT01177397) Study to Assess Safety, Pharmacokinetics, and Efficacy of Oral CC-223 for Patients With Advanced Solid Tumors, Non-Hodgkin Lymphoma or Multiple Myeloma. U.S. NationalInstitutes of Health. | ||||
Ref 523484 | ClinicalTrials.gov (NCT01356173) Evaluating the Safety and Tolerability of GDC-0349 in Patients With Locally Advanced or Metastatic Solid Tumors or Non Hodgkin's Lymphoma. U.S. National Institutes ofHealth. | ||||
Ref 523487 | ClinicalTrials.gov (NCT01357330) Oral SAR245408 (XL147) and Oral MSC1936369B in Patients With Locally Advanced or Metastatic Solid Tumors. U.S. National Institutes of Health. | ||||
Ref 523571 | ClinicalTrials.gov (NCT01407380) Study of PWT33597 Mesylate in Subjects With Advanced Malignancies. U.S. National Institutes of Health. | ||||
Ref 523615 | ClinicalTrials.gov (NCT01430585) Pre-Operative Study of PF-4691502 With Letrozole Compared To Letrozole Alone In Patients With Early Breast Cancer. U.S. National Institutes of Health. | ||||
Ref 523889 | ClinicalTrials.gov (NCT01588678) A Open-Label, Multiple Ascending Dose Study of DS-3078a, an Oral TORC1/2 Kinase Inhibitor, in Subjects With Advanced Solid Tumors or Lymphomas. U.S. National Institutes of Health. | ||||
Ref 524214 | ClinicalTrials.gov (NCT01793636) A Study Comparing AZD2014 vs Everolimus in Patients With Metastatic Renal Cancer. U.S. National Institutes of Health. | ||||
Ref 524422 | ClinicalTrials.gov (NCT01936363) Trial of Pimasertib With SAR245409 or Placebo in Ovarian Cancer. U.S. National Institutes of Health. | ||||
Ref 524566 | ClinicalTrials.gov (NCT02009956) EXCELLA Post-Approval Study. U.S. National Institutes of Health. | ||||
Ref 531516 | Preclinical characterization of OSI-027, a potent and selective inhibitor of mTORC1 and mTORC2: distinct from rapamycin. Mol Cancer Ther. 2011 Aug;10(8):1394-406. | ||||
Ref 531639 | Simultaneous targeting of PI3K and mTOR with NVP-BGT226 is highly effective in multiple myeloma. Anticancer Drugs. 2012 Jan;23(1):131-8. | ||||
Ref 531692 | Phase II study of the mammalian target of rapamycin inhibitor ridaforolimus in patients with advanced bone and soft tissue sarcomas. J Clin Oncol. 2012 Jan 1;30(1):78-84. | ||||
Ref 532167 | VS-5584, a novel and highly selective PI3K/mTOR kinase inhibitor for the treatment of cancer. Mol Cancer Ther. 2013 Feb;12(2):151-61. | ||||
Ref 532990 | Advances in kinase targeting: current clinical use and clinical trials. Trends Pharmacol Sci. 2014 Nov;35(11):604-20. | ||||
Ref 533132 | First-in-Human Study of PF-05212384 (PKI-587), a Small-Molecule, Intravenous, Dual Inhibitor of PI3K and mTOR in Patients with Advanced Cancer. Clin Cancer Res. 2015 Apr 15;21(8):1888-95. | ||||
Ref 536361 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20. | ||||
Ref 541186 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5889). | ||||
Ref 541190 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5892). | ||||
Ref 541290 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6031). | ||||
Ref 542674 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7699). | ||||
Ref 542689 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7714). | ||||
Ref 542809 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7884). | ||||
Ref 542848 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7933). | ||||
Ref 542851 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7936). | ||||
Ref 542855 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7940). | ||||
Ref 542866 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7950). | ||||
Ref 542867 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7951). | ||||
Ref 542878 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7961). | ||||
Ref 542890 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7974). | ||||
Ref 543098 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8382). | ||||
Ref 543099 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8383). | ||||
Ref 545206 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002452) | ||||
Ref 547739 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018935) | ||||
Ref 548121 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800022134) | ||||
Ref 548508 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026094) | ||||
Ref 548607 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026972) | ||||
Ref 548781 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028731) | ||||
Ref 549261 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800034336) | ||||
Ref 549411 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800036731) | ||||
Ref 527216 | J Med Chem. 2004 Sep 23;47(20):4950-7.A locally active antiinflammatory macrolide (MLD987) for inhalation therapy of asthma. | ||||
Ref 527386 | J Med Chem. 2005 Jan 27;48(2):569-85.Selective benzopyranone and pyrimido[2,1-a]isoquinolin-4-one inhibitors of DNA-dependent protein kinase: synthesis, structure-activity studies, and radiosensitization of a human tumor cell line in vitro. | ||||
Ref 528725 | J Biol Chem. 2007 May 4;282(18):13395-401. Epub 2007 Mar 9.The rapamycin-binding domain of the protein kinase mammalian target of rapamycin is a destabilizing domain. | ||||
Ref 529484 | Natural products to drugs: natural product-derived compounds in clinical trials. Nat Prod Rep. 2008 Jun;25(3):475-516. | ||||
Ref 529744 | Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat Chem Biol. 2008 Nov;4(11):691-9. | ||||
Ref 530099 | Bioorg Med Chem Lett. 2009 Jun 1;19(11):2949-52. Epub 2009 Apr 18.Synthesis and therapeutic evaluation of pyridyl based novel mTOR inhibitors. | ||||
Ref 530563 | Bioorg Med Chem Lett. 2010 Jan 15;20(2):636-9. Epub 2009 Dec 5.Novel purine and pyrazolo[3,4-d]pyrimidine inhibitors of PI3 kinase-alpha: Hit to lead studies. | ||||
Ref 531173 | Discovery of 1-(4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one as a highly potent, selective mammalian target of rapamycin (mTOR) inhibitor for the treatment of cancer. J Med Chem. 2010 Oct 14;53(19):7146-55. | ||||
Ref 531187 | Early detection of response to experimental chemotherapeutic Top216 with [18F]FLT and [18F]FDG PET in human ovary cancer xenografts in mice. PLoS One. 2010 Sep 24;5(9):e12965. | ||||
Ref 531639 | Simultaneous targeting of PI3K and mTOR with NVP-BGT226 is highly effective in multiple myeloma. Anticancer Drugs. 2012 Jan;23(1):131-8. | ||||
Ref 531658 | GDC-0980 is a novel class I PI3K/mTOR kinase inhibitor with robust activity in cancer models driven by the PI3K pathway. Mol Cancer Ther. 2011 Dec;10(12):2426-36. | ||||
Ref 532144 | Targeting ATR in vivo using the novel inhibitor VE-822 results in selective sensitization of pancreatic tumors to radiation. Cell Death Dis. 2012 Dec 6;3:e441. | ||||
Ref 532167 | VS-5584, a novel and highly selective PI3K/mTOR kinase inhibitor for the treatment of cancer. Mol Cancer Ther. 2013 Feb;12(2):151-61. | ||||
Ref 532573 | Dramatic suppression of colorectal cancer cell growth by the dual mTORC1 and mTORC2 inhibitor AZD-2014. Biochem Biophys Res Commun. 2014 Jan 10;443(2):406-12. | ||||
Ref 532664 | Antitumor activity and induction of TP53-dependent apoptosis toward ovarian clear cell adenocarcinoma by the dual PI3K/mTOR inhibitor DS-7423. PLoS One. 2014 Feb 4;9(2):e87220. | ||||
Ref 532819 | Discovery of the Highly Potent PI3K/mTOR Dual Inhibitor PF-04979064 through Structure-Based Drug Design. ACS Med Chem Lett. 2012 Nov 7;4(1):91-7. | ||||
Ref 532820 | Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349. ACS Med Chem Lett. 2012 Nov 29;4(1):103-7. | ||||
Ref 532990 | Advances in kinase targeting: current clinical use and clinical trials. Trends Pharmacol Sci. 2014 Nov;35(11):604-20. | ||||
Ref 533132 | First-in-Human Study of PF-05212384 (PKI-587), a Small-Molecule, Intravenous, Dual Inhibitor of PI3K and mTOR in Patients with Advanced Cancer. Clin Cancer Res. 2015 Apr 15;21(8):1888-95. | ||||
Ref 533206 | CC-223, a Potent and Selective Inhibitor of mTOR Kinase: In Vitro and In Vivo Characterization. Mol Cancer Ther. 2015 Jun;14(6):1295-305. | ||||
Ref 535318 | Selected novel anticancer treatments targeting cell signaling proteins. Oncologist. 2001;6(6):517-37. | ||||
Ref 535660 | Knockouts model the 100 best-selling drugs--will they model the next 100? Nat Rev Drug Discov. 2003 Jan;2(1):38-51. | ||||
Ref 537621 | Mammalian target of rapamycin, its mode of action and clinical response in metastatic clear cell carcinoma. Gan To Kagaku Ryoho. 2009 Jul;36(7):1076-9. | ||||
Ref 537633 | Targeting the phosphoinositide 3-kinase pathway in cancer. Nat Rev Drug Discov. 2009 Aug;8(8):627-44. | ||||
Ref 543556 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2109). | ||||
Ref 549718 | A novel c-Met inhibitor, MK8033, synergizes with carboplatin plus paclitaxel to inhibit ovarian cancer cell growth. Oncol Rep. 2013 May;29(5):2011-8. | ||||
Ref 549970 | A first-in-human Phase I study of DS-3078a, an oral TORC1/2 inhibitor, in patients with advanced solid tumors: Preliminary results, Mol Cancer Ther November,2013, 12, C173. |
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