Target Information
Target General Information | Top | |||||
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Target ID |
T75243
(Former ID: TTDS00265)
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Target Name |
Serine/threonine-protein kinase mTOR (mTOR)
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Synonyms |
Target of rapamycin; TOR kinase; Rapamycin target protein 1; Rapamycin target protein; Rapamycin and FKBP12 target 1; RAPT1; RAFT1; Mechanistic target of rapamycin; Mammalian target of rapamycin; FRAP2; FRAP1; FRAP; FKBP12-rapamycin complex-associated protein; FKBP-rapamycin associated protein; FK506-binding protein 12-rapamycin complex-associated protein 1
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Gene Name |
MTOR
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Target Type |
Successful target
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[1] | ||||
Disease | [+] 6 Target-related Diseases | + | ||||
1 | Arteries/arterioles disorder [ICD-11: BD52] | |||||
2 | Chronic myelomonocytic leukaemia [ICD-11: 2A40] | |||||
3 | Multiple myeloma [ICD-11: 2A83] | |||||
4 | Renal cell carcinoma [ICD-11: 2C90] | |||||
5 | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | |||||
6 | Transplant rejection [ICD-11: NE84] | |||||
Function |
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 activator of 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. Also prevents autophagy by phosphorylating RUBCNL/Pacer under nutrient-rich conditions. mTORC1 exerts a feedback control on upstream growth 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'. Regulates osteoclastogenesis by adjusting the expression of CEBPB isoforms. Plays an important regulatory role in the circadian clock function; regulates period length and rhythm amplitude of the suprachiasmatic nucleus (SCN) and liver clocks. 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.
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BioChemical Class |
Kinase
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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 Click to Show/Hide
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3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
ADReCS ID | BADD_A06952 | |||||
HIT2.0 ID | T74QXI |
Drugs and Modes of Action | Top | |||||
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Approved Drug(s) | [+] 6 Approved Drugs | + | ||||
1 | Everolimus | Drug Info | Approved | Renal cell carcinoma | [2], [3] | |
2 | Novolimus | Drug Info | Approved | Artery stenosis | [4], [5] | |
3 | PF-04449913 | Drug Info | Approved | Chronic myelomonocytic leukaemia | [6] | |
4 | Sirolimus | Drug Info | Approved | Organ transplant rejection | [7], [8] | |
5 | Temsirolimus | Drug Info | Approved | Renal cell carcinoma | [1], [9] | |
6 | Zotarolimus | Drug Info | Approved | Solid tumour/cancer | [10], [11], [12] | |
Clinical Trial Drug(s) | [+] 25 Clinical Trial Drugs | + | ||||
1 | Ridaforolimus | Drug Info | Phase 3 | Sarcoma | [13], [14] | |
2 | ABI-009 | Drug Info | Phase 2 | Solid tumour/cancer | [15] | |
3 | AZD2014 | Drug Info | Phase 2 | Solid tumour/cancer | [16], [17] | |
4 | BEZ235 | Drug Info | Phase 2 | Solid tumour/cancer | [18], [19] | |
5 | GDC-0980/RG7422 | Drug Info | Phase 2 | Non-hodgkin lymphoma | [20] | |
6 | INK128 | Drug Info | Phase 2 | Breast cancer | [21] | |
7 | LY3023414 | Drug Info | Phase 2 | Solid tumour/cancer | [22] | |
8 | MM-141 | Drug Info | Phase 2 | Solid tumour/cancer | [23] | |
9 | OSI-027 | Drug Info | Phase 2 | Renal cell carcinoma | [24] | |
10 | PF-04691502 | Drug Info | Phase 2 | Endometrial cancer | [25], [26] | |
11 | PF-05212384 | Drug Info | Phase 2 | Solid tumour/cancer | [21], [27], [28] | |
12 | PQR309 | Drug Info | Phase 2 | Squamous head and neck cell carcinom | [29] | |
13 | Salirasib | Drug Info | Phase 2 | Lung cancer | [30], [31] | |
14 | SAR245409 | Drug Info | Phase 2 | Solid tumour/cancer | [32] | |
15 | SF1126 | Drug Info | Phase 2 | Head and neck cancer | [21] | |
16 | BGT226 | Drug Info | Phase 1/2 | Solid tumour/cancer | [33], [34] | |
17 | CC-223 | Drug Info | Phase 1/2 | Solid tumour/cancer | [35] | |
18 | ME-344 | Drug Info | Phase 1/2 | Breast cancer | [21] | |
19 | BI 860585 | Drug Info | Phase 1 | Solid tumour/cancer | [36] | |
20 | DS-3078 | Drug Info | Phase 1 | Lymphoma | [37] | |
21 | DS-7423 | Drug Info | Phase 1 | Solid tumour/cancer | [38] | |
22 | GDC-0349 | Drug Info | Phase 1 | Non-hodgkin lymphoma | [39] | |
23 | LAM-001 | Drug Info | Phase 1 | Lymphangioleiomyomatosis | [40] | |
24 | PWT-33597 | Drug Info | Phase 1 | Solid tumour/cancer | [41] | |
25 | VS-5584 | Drug Info | Phase 1 | Solid tumour/cancer | [42], [43] | |
Discontinued Drug(s) | [+] 3 Discontinued Drugs | + | ||||
1 | AZD8055 | Drug Info | Discontinued in Phase 1/2 | Solid tumour/cancer | [44], [45] | |
2 | TAFA-93 | Drug Info | Discontinued in Phase 1 | Transplant rejection | [46] | |
3 | SCR-44001 | Drug Info | Terminated | Solid tumour/cancer | [47] | |
Mode of Action | [+] 2 Modes of Action | + | ||||
Inhibitor | [+] 56 Inhibitor drugs | + | ||||
1 | Everolimus | Drug Info | [48] | |||
2 | Novolimus | Drug Info | [49] | |||
3 | PF-04449913 | Drug Info | [50] | |||
4 | Sirolimus | Drug Info | [51] | |||
5 | Temsirolimus | Drug Info | [1], [11] | |||
6 | Ridaforolimus | Drug Info | [53], [54] | |||
7 | ABI-009 | Drug Info | [21] | |||
8 | AZD2014 | Drug Info | [55] | |||
9 | INK128 | Drug Info | [58] | |||
10 | MM-141 | Drug Info | [21] | |||
11 | OSI-027 | Drug Info | [60] | |||
12 | PQR309 | Drug Info | [49] | |||
13 | SAR245409 | Drug Info | [49], [62] | |||
14 | SF1126 | Drug Info | [21] | |||
15 | ME-344 | Drug Info | [64] | |||
16 | BI 860585 | Drug Info | [65] | |||
17 | GDC-0349 | Drug Info | [68] | |||
18 | LAM-001 | Drug Info | [40] | |||
19 | PMID25726713-Compound-47 | Drug Info | [70] | |||
20 | PMID25726713-Compound-48 | Drug Info | [70] | |||
21 | PMID25726713-Compound-49 | Drug Info | [70] | |||
22 | PMID25726713-Compound-50 | Drug Info | [70] | |||
23 | PMID25726713-Compound-51 | Drug Info | [70] | |||
24 | AZD8055 | Drug Info | [71] | |||
25 | TAFA-93 | Drug Info | [72] | |||
26 | SCR-44001 | Drug Info | [73] | |||
27 | (4-(6-morpholino-9H-purin-2-yl)phenyl)methanol | Drug Info | [74] | |||
28 | 2-(2-Methyl-morpholin-4-yl)-benzo[h]chromen-4-one | Drug Info | [75] | |||
29 | 2-(6-morpholino-9H-purin-2-yl)phenol | Drug Info | [74] | |||
30 | 2-chloro-N-(6-cyanopyridin-3-yl)propanamide | Drug Info | [76] | |||
31 | 2-Morpholin-4-yl-pyrimido[2,1-a]isoquinolin-4-one | Drug Info | [75] | |||
32 | 3-(6-morpholino-9H-purin-2-yl)phenol | Drug Info | [74] | |||
33 | 4-(2-(1H-indol-6-yl)-9H-purin-6-yl)morpholine | Drug Info | [74] | |||
34 | 4-(2-(thiophen-2-yl)-9H-purin-6-yl)morpholine | Drug Info | [74] | |||
35 | 4-(2-(thiophen-3-yl)-9H-purin-6-yl)morpholine | Drug Info | [74] | |||
36 | 4-(6-morpholino-9H-purin-2-yl)phenol | Drug Info | [74] | |||
37 | AP-21967 | Drug Info | [77] | |||
38 | AR-mTOR-26 | Drug Info | [49] | |||
39 | C-16-(S)-3-methylindolerapamycin | Drug Info | [77] | |||
40 | CU-906 | Drug Info | [49] | |||
41 | EC-0565 | Drug Info | [49] | |||
42 | EM-101 | Drug Info | [49] | |||
43 | Ethyl 1-[(1H-benzimidazol-2(3H)one-5-yl)sulfonyl]-1H-pyrrole-2-carboxylate | Drug Info | [75] | |||
44 | HM-5016699 | Drug Info | [49] | |||
45 | OXA-01 | Drug Info | [49] | |||
46 | P-2281 | Drug Info | [49] | |||
47 | P-6915 | Drug Info | [49] | |||
48 | PF-03772304 | Drug Info | [78] | |||
49 | PF-05094037 | Drug Info | [49] | |||
50 | PP-242 | Drug Info | [79] | |||
51 | PP121 | Drug Info | [79] | |||
52 | Rapamycin complexed with immunophilin FKBP12 | Drug Info | [80] | |||
53 | SB-2280 | Drug Info | [49] | |||
54 | torin 1 | Drug Info | [81] | |||
55 | Torin2 | Drug Info | [82] | |||
56 | X-387 | Drug Info | [49] | |||
Modulator | [+] 15 Modulator drugs | + | ||||
1 | Zotarolimus | Drug Info | [52] | |||
2 | BEZ235 | Drug Info | [56] | |||
3 | GDC-0980/RG7422 | Drug Info | [49], [57] | |||
4 | LY3023414 | Drug Info | [59] | |||
5 | PF-04691502 | Drug Info | [61] | |||
6 | PF-05212384 | Drug Info | [28] | |||
7 | Salirasib | Drug Info | [49] | |||
8 | BGT226 | Drug Info | [34] | |||
9 | CC-223 | Drug Info | [63] | |||
10 | DS-3078 | Drug Info | [66] | |||
11 | DS-7423 | Drug Info | [67] | |||
12 | PWT-33597 | Drug Info | [69] | |||
13 | VS-5584 | Drug Info | [43], [49] | |||
14 | EC-0845 | Drug Info | [49] | |||
15 | SX-MTR1 | Drug Info | [49] |
Chemical Structure based Activity Landscape of Target | Top |
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Drug Property Profile of Target | Top | |
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(1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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(5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five |
Co-Targets | Top | |||||
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Co-Targets |
Target Poor or Non Binders | Top | |||||
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Target Poor or Non Binders |
Target Regulators | Top | |||||
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Target-regulating microRNAs | ||||||
Target-interacting Proteins |
Target Profiles in Patients | Top | |||||
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Target Expression Profile (TEP) | ||||||
Drug Resistance Mutation (DRM) |
Target-Related Models and Studies | Top | |||||
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Target Validation |
References | Top | |||||
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REF 1 | Advances in kinase targeting: current clinical use and clinical trials. Trends Pharmacol Sci. 2014 Nov;35(11):604-20. | |||||
REF 2 | URL: 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 3 | Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92. | |||||
REF 4 | Clinical pipeline report, company report or official report of Elixir. | |||||
REF 5 | ClinicalTrials.gov (NCT02009956) EXCELLA Post-Approval Study. U.S. National Institutes of Health. | |||||
REF 6 | 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89. | |||||
REF 7 | URL: 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 8 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. | |||||
REF 9 | URL: 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 10 | URL: 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 11 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
REF 12 | ClinicalTrials.gov (NCT00589927) Triple Versus Dual Antiplatelet Therapy After ABT578-Eluting Stent. U.S. National Institutes of Health. | |||||
REF 13 | URL: 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 14 | 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 15 | ClinicalTrials.gov (NCT02494570) A Phase 2 Study of ABI-009 in Patients With Advanced Malignant PEComa. | |||||
REF 16 | URL: 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 17 | ClinicalTrials.gov (NCT01793636) A Study Comparing AZD2014 vs Everolimus in Patients With Metastatic Renal Cancer. U.S. National Institutes of Health. | |||||
REF 18 | URL: 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 19 | 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 20 | Clinical pipeline report, company report or official report of Roche. | |||||
REF 21 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
REF 22 | ClinicalTrials.gov (NCT02549989) Study of LY3023414 for the Treatment of Recurrent. | |||||
REF 23 | ClinicalTrials.gov (NCT02399137) A Phase 2 Study of MM-141 Plus Nab-paclitaxel and Gemcitabine in Front-line Metastatic Pancreatic Cancer. U.S. National Institutes of Health. | |||||
REF 24 | 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 25 | URL: 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 26 | 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 27 | URL: 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 28 | 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 29 | ClinicalTrials.gov (NCT03740100) Single-arm Study With Bimiralisib in Patients With HNSCC Harboring NOTCH1 Loss of Function Mutations (HNSCC). U.S. National Institutes of Health. | |||||
REF 30 | URL: 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: 6281). | |||||
REF 31 | 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 32 | ClinicalTrials.gov (NCT01936363) Trial of Pimasertib With SAR245409 or Placebo in Ovarian Cancer. U.S. National Institutes of Health. | |||||
REF 33 | URL: 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 34 | Simultaneous targeting of PI3K and mTOR with NVP-BGT226 is highly effective in multiple myeloma. Anticancer Drugs. 2012 Jan;23(1):131-8. | |||||
REF 35 | 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 36 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800038828) | |||||
REF 37 | 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 38 | 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 39 | 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 40 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
REF 41 | ClinicalTrials.gov (NCT01407380) Study of PWT33597 Mesylate in Subjects With Advanced Malignancies. U.S. National Institutes of Health. | |||||
REF 42 | URL: 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 43 | 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. | |||||
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