Id: acc0458
Group: 1sens
Protein: mTOR
Gene Symbol: MTOR
Protein Id: P42345
Protein Name: MTOR_HUMAN
PTM: phosphorylation
Site: Ser2481
Site Sequence: GTTVPESIHSFIGDGLVKPEA
Disease Category: Cancer
Disease: Gastric Cancer
Disease Subtype:
Disease Cellline: Hs746T
Disease Info:
Drug: mefloquine
Drug Info: "Mefloquine is a 4-quinolinemethanol derivative antimalarial agent that effectively kills erythrocytic stage parasites, particularly mature trophozoites and schizonts, and is primarily used for the treatment of chloroquine-resistant or multidrug-resistant Plasmodium falciparum malaria, often combined with sulfadoxine and pyrimethamine to enhance efficacy and delay resistance development."
Effect: modulate
Effect Info: "Mefloquine inhibits the PI3K/Akt/mTOR signaling pathway by suppressing the phosphorylation of PI3K, Akt, mTOR, and ribosomal protein S6 (rS6), thereby inhibiting gastric cancer cells."
Note:
Score: 4.0
Pubmed(PMID): 26780727
Sentence Index:
Sentence:

Sequence & Structure:

MLGTGPAAATTAATTSSNVSVLQQFASGLKSRNEETRAKAAKELQHYVTMELREMSQEESTRFYDQLNHHIFELVSSSDANERKGGILAIASLIGVEGGNATRIGRFANYLRNLLPSNDPVVMEMASKAIGRLAMAGDTFTAEYVEFEVKRALEWLGADRNEGRRHAAVLVLRELAISVPTFFFQQVQPFFDNIFVAVWDPKQAIREGAVAALRACLILTTQREPKEMQKPQWYRHTFEEAEKGFDETLAKEKGMNRDDRIHGALLILNELVRISSMEGERLREEMEEITQQQLVHDKYCKDLMGFGTKPRHITPFTSFQAVQPQQSNALVGLLGYSSHQGLMGFGTSPSPAKSTLVESRCCRDLMEEKFDQVCQWVLKCRNSKNSLIQMTILNLLPRLAAFRPSAFTDTQYLQDTMNHVLSCVKKEKERTAAFQALGLLSVAVRSEFKVYLPRVLDIIRAALPPKDFAHKRQKAMQVDATVFTCISMLARAMGPGIQQDIKELLEPMLAVGLSPALTAVLYDLSRQIPQLKKDIQDGLLKMLSLVLMHKPLRHPGMPKGLAHQLASPGLTTLPEASDVGSITLALRTLGSFEFEGHSLTQFVRHCADHFLNSEHKEIRMEAARTCSRLLTPSIHLISGHAHVVSQTAVQVVADVLSKLLVVGITDPDPDIRYCVLASLDERFDAHLAQAENLQALFVALNDQVFEIRELAICTVGRLSSMNPAFVMPFLRKMLIQILTELEHSGIGRIKEQSARMLGHLVSNAPRLIRPYMEPILKALILKLKDPDPDPNPGVINNVLATIGELAQVSGLEMRKWVDELFIIIMDMLQDSSLLAKRQVALWTLGQLVASTGYVVEPYRKYPTLLEVLLNFLKTEQNQGTRREAIRVLGLLGALDPYKHKVNIGMIDQSRDASAVSLSESKSSQDSSDYSTSEMLVNMGNLPLDEFYPAVSMVALMRIFRDQSLSHHHTMVVQAITFIFKSLGLKCVQFLPQVMPTFLNVIRVCDGAIREFLFQQLGMLVSFVKSHIRPYMDEIVTLMREFWVMNTSIQSTIILLIEQIVVALGGEFKLYLPQLIPHMLRVFMHDNSPGRIVSIKLLAAIQLFGANLDDYLHLLLPPIVKLFDAPEAPLPSRKAALETVDRLTESLDFTDYASRIIHPIVRTLDQSPELRSTAMDTLSSLVFQLGKKYQIFIPMVNKVLVRHRINHQRYDVLICRIVKGYTLADEEEDPLIYQHRMLRSGQGDALASGPVETGPMKKLHVSTINLQKAWGAARRVSKDDWLEWLRRLSLELLKDSSSPSLRSCWALAQAYNPMARDLFNAAFVSCWSELNEDQQDELIRSIELALTSQDIAEVTQTLLNLAEFMEHSDKGPLPLRDDNGIVLLGERAAKCRAYAKALHYKELEFQKGPTPAILESLISINNKLQQPEAAAGVLEYAMKHFGELEIQATWYEKLHEWEDALVAYDKKMDTNKDDPELMLGRMRCLEALGEWGQLHQQCCEKWTLVNDETQAKMARMAAAAAWGLGQWDSMEEYTCMIPRDTHDGAFYRAVLALHQDLFSLAQQCIDKARDLLDAELTAMAGESYSRAYGAMVSCHMLSELEEVIQYKLVPERREIIRQIWWERLQGCQRIVEDWQKILMVRSLVVSPHEDMRTWLKYASLCGKSGRLALAHKTLVLLLGVDPSRQLDHPLPTVHPQVTYAYMKNMWKSARKIDAFQHMQHFVQTMQQQAQHAIATEDQQHKQELHKLMARCFLKLGEWQLNLQGINESTIPKVLQYYSAATEHDRSWYKAWHAWAVMNFEAVLHYKHQNQARDEKKKLRHASGANITNATTAATTAATATTTASTEGSNSESEAESTENSPTPSPLQKKVTEDLSKTLLMYTVPAVQGFFRSISLSRGNNLQDTLRVLTLWFDYGHWPDVNEALVEGVKAIQIDTWLQVIPQLIARIDTPRPLVGRLIHQLLTDIGRYHPQALIYPLTVASKSTTTARHNAANKILKNMCEHSNTLVQQAMMVSEELIRVAILWHEMWHEGLEEASRLYFGERNVKGMFEVLEPLHAMMERGPQTLKETSFNQAYGRDLMEAQEWCRKYMKSGNVKDLTQAWDLYYHVFRRISKQLPQLTSLELQYVSPKLLMCRDLELAVPGTYDPNQPIIRIQSIAPSLQVITSKQRPRKLTLMGSNGHEFVFLLKGHEDLRQDERVMQLFGLVNTLLANDPTSLRKNLSIQRYAVIPLSTNSGLIGWVPHCDTLHALIRDYREKKKILLNIEHRIMLRMAPDYDHLTLMQKVEVFEHAVNNTAGDDLAKLLWLKSPSSEVWFDRRTNYTRSLAVMSMVGYILGLGDRHPSNLMLDRLSGKILHIDFGDCFEVAMTREKFPEKIPFRLTRMLTNAMEVTGLDGNYRITCHTVMEVLREHKDSVMAVLEAFVYDPLLNWRLMDTNTKGNKRSRTRTDSYSAGQSVEILDGVELGEPAHKKTGTTVPESIHSFIGDGLVKPEALNKKAIQIINRVRDKLTGRDFSHDDTLDVPTQVELLIKQATSHENLCQCYIGWCPFW

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

Target Drug name MOA Phase Status Disease Source
MTOR PERHEXILINE Serine/threonine-protein kinase mTOR inhibitor 4 - cardiovascular disease ATC
MTOR PERHEXILINE Serine/threonine-protein kinase mTOR inhibitor 3 Withdrawn hypertrophic cardiomyopathy ClinicalTrials
MTOR DACTOLISIB Serine/threonine-protein kinase mTOR inhibitor 3 Completed infection ClinicalTrials
MTOR RIDAFOROLIMUS Serine/threonine-protein kinase mTOR inhibitor 3 - neoplasm ATC
MTOR RIDAFOROLIMUS Serine/threonine-protein kinase mTOR inhibitor 3 Completed soft tissue sarcoma ClinicalTrials
MTOR GEDATOLISIB Serine/threonine-protein kinase mTOR inhibitor 3 Recruiting breast cancer ClinicalTrials
MTOR RIDAFOROLIMUS Serine/threonine-protein kinase mTOR inhibitor 3 Completed bone sarcoma ClinicalTrials
MTOR SF-1126 Serine/threonine-protein kinase mTOR inhibitor 2 Terminated head and neck squamous cell carcinoma ClinicalTrials
MTOR ONATASERTIB Serine/threonine-protein kinase mTOR inhibitor 2 Terminated hepatocellular carcinoma ClinicalTrials
MTOR INDOXIMOD mTORC1 activator 2 Completed metastatic prostate cancer ClinicalTrials
MTOR RIDAFOROLIMUS Serine/threonine-protein kinase mTOR inhibitor 2 Completed myelodysplastic syndrome ClinicalTrials
MTOR GEDATOLISIB Serine/threonine-protein kinase mTOR inhibitor 2 Terminated myelodysplastic syndrome ClinicalTrials
MTOR GEDATOLISIB Serine/threonine-protein kinase mTOR inhibitor 2 Terminated acute myeloid leukemia ClinicalTrials
MTOR SAPANISERTIB Serine/threonine-protein kinase mTOR inhibitor 2 Active, not recruiting T-cell acute lymphoblastic leukemia ClinicalTrials
MTOR VISTUSERTIB Serine/threonine-protein kinase mTOR inhibitor 2 Active, not recruiting adenocarcinoma ClinicalTrials
MTOR VISTUSERTIB Serine/threonine-protein kinase mTOR inhibitor 2 Terminated clear cell renal carcinoma ClinicalTrials
MTOR VISTUSERTIB Serine/threonine-protein kinase mTOR inhibitor 2 Terminated gastric adenocarcinoma ClinicalTrials
MTOR PERHEXILINE Serine/threonine-protein kinase mTOR inhibitor 2 Terminated hypertrophic cardiomyopathy ClinicalTrials
MTOR RIDAFOROLIMUS Serine/threonine-protein kinase mTOR inhibitor 2 Completed leiomyosarcoma ClinicalTrials
MTOR DACTOLISIB Serine/threonine-protein kinase mTOR inhibitor 2 Active, not recruiting infection ClinicalTrials
MTOR RIDAFOROLIMUS Serine/threonine-protein kinase mTOR inhibitor 2 Completed lymphoma ClinicalTrials
MTOR VOXTALISIB Serine/threonine-protein kinase mTOR inhibitor 2 Completed lymphoma ClinicalTrials
MTOR PERHEXILINE Serine/threonine-protein kinase mTOR inhibitor 2 Completed hypertrophic cardiomyopathy ClinicalTrials
MTOR PERHEXILINE Serine/threonine-protein kinase mTOR inhibitor 2 Recruiting hypertrophic cardiomyopathy ClinicalTrials
MTOR RIDAFOROLIMUS Serine/threonine-protein kinase mTOR inhibitor 2 Completed leukemia ClinicalTrials

Note: Only show clinically investigational or approved drugs with protein targets.

Protein Tractability:

source: Open Targets
Small molecule
Antibody
PROTAC
Other modalities
Approved Drug
Advanced Clinical
Phase 1 Clinical
Structure with Ligand
High-Quality Ligand
High-Quality Pocket
Med-Quality Pocket
Druggable Family
Approved Drug
Advanced Clinical
Phase 1 Clinical
UniProt loc high conf
GO CC high conf
UniProt loc med conf
UniProt SigP or TMHMM
GO CC med conf
Human Protein Atlas loc
Approved Drug
Advanced Clinical
Phase 1 Clinical
Literature
UniProt Ubiquitination
Database Ubiquitination
Half-life Data
Small Molecule Binder
Approved Drug
Advanced Clinical
Phase 1 Clinical

PTM Intensity:

source: CPTAC
MTOR-Ser2481
Cancer Intensity
BRCA 0.302
COAD -0.364
HGSC 2.451
ccRCC -0.257
GBM 0.596
HNSC -0.341
LUAD -0.327
LUSC 0.493
non_ccRCC -1.381
PDAC -0.206
UCEC -0.964

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
S 2481 U Breast cancer Phosphorylation 27721400
S 2481 U Breast cancer/tumor/carcinoma Phosphorylation 19956839

State Note: Based on the distinct PTM states in diseases, PTMD classified all disease-associated PTMs into six classes, including whether the up-regulation (U) or down-regulation (D) of PTM levels, the absence (A) or presence (P) of PTMs, and the creation (C) or disruption (N) of PTM sites are associated with diseases.

PTM-Drug Perturbation Response:

source: DecryptM
Protein Gene PTM Position Modified sequence Cell Drug pEC50 Regulation Experiment
P42345 MTOR P Ser2481 TGTTVPESIHS(ph)FIGDGLVKPEALNKK HeLa A486 6.001 -

pEC50 Note: pEC50 is the negative logarithm of EC50 (half-maximal effective concentration, dosage unit Mol), calculated as pEC50 = -log10(EC50), which quantifies the potency of a drug or compound.

Function score:

source: funscoR

No data.

Cross Links: