Target General Infomation
Target ID
T75243
Former ID
TTDS00265
Target Name
Serine/threonine-protein kinase mTOR
Gene Name
MTOR
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
Target Type
Successful
Disease Advanced kidney cancer [ICD9: 189; ICD10: C64]
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]
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'.
BioChemical Class
Kinase
Target Validation
T75243
UniProt ID
EC Number
EC 2.7.11.1
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
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)
TEP EXP Info
DRM DRM Info
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 522199ClinicalTrials.gov (NCT00589927) Triple Versus Dual Antiplatelet Therapy After ABT578-Eluting Stent. U.S. National Institutes of Health.
Ref 523130ClinicalTrials.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 523484ClinicalTrials.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 523487ClinicalTrials.gov (NCT01357330) Oral SAR245408 (XL147) and Oral MSC1936369B in Patients With Locally Advanced or Metastatic Solid Tumors. U.S. National Institutes of Health.
Ref 523571ClinicalTrials.gov (NCT01407380) Study of PWT33597 Mesylate in Subjects With Advanced Malignancies. U.S. National Institutes of Health.
Ref 523615ClinicalTrials.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 523889ClinicalTrials.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 524214ClinicalTrials.gov (NCT01793636) A Study Comparing AZD2014 vs Everolimus in Patients With Metastatic Renal Cancer. U.S. National Institutes of Health.
Ref 524422ClinicalTrials.gov (NCT01936363) Trial of Pimasertib With SAR245409 or Placebo in Ovarian Cancer. U.S. National Institutes of Health.
Ref 524566ClinicalTrials.gov (NCT02009956) EXCELLA Post-Approval Study. U.S. National Institutes of Health.
Ref 525317ClinicalTrials.gov (NCT02549989) Study of LY3023414 for the Treatment of Recurrent.
Ref 530677Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
Ref 531516Preclinical 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 531639Simultaneous targeting of PI3K and mTOR with NVP-BGT226 is highly effective in multiple myeloma. Anticancer Drugs. 2012 Jan;23(1):131-8.
Ref 531692Phase 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 532167VS-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 532990Advances in kinase targeting: current clinical use and clinical trials. Trends Pharmacol Sci. 2014 Nov;35(11):604-20.
Ref 533132First-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 536361Natural 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 545206Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002452)
Ref 547739Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018935)
Ref 548121Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800022134)
Ref 548508Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026094)
Ref 548607Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026972)
Ref 548781Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028731)
Ref 549261Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800034336)
Ref 549411Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800036731)
Ref 549503Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800038828)
Ref 549817Clinical pipeline report, company report or official report of Elixir.
Ref 550796Clinical pipeline report, company report or official report of Genentech (2011).
Ref 5510382011 Pipeline of Intellikine.
Ref 551603Clinical pipeline report, company report or official report of Roche.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 527216J Med Chem. 2004 Sep 23;47(20):4950-7.A locally active antiinflammatory macrolide (MLD987) for inhalation therapy of asthma.
Ref 527386J 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 528725J 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.
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