Id: acc1879
Group: 2sens
Protein: mTOR
Gene Symbol: MTOR
Protein Id: P42345
Protein Name: MTOR_HUMAN
PTM: phosphorylation
Site: Ser2448
Site Sequence: NKRSRTRTDSYSAGQSVEILD
Disease Category: Cancer
Disease: Colorectal Cancer
Disease Subtype:
Disease Cellline: HCT116
Disease Info:
Drug: PD98059 + rapamycin
Drug Info: "PD98059 is a non-ATP competitive MEK inhibitor with an IC50 of 2 μM, specifically inhibiting MEK-1-mediated MAPK activation without directly suppressing ERK1 and ERK2. rapamycin: -"
Effect: modulate
Effect Info: Drug therapy reduces the phosphorylation level and inhibits tumors.
Note: drug comb
Score: 4.0
Pubmed(PMID): 19194827
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-Ser2448
Cancer Intensity
BRCA
COAD -0.707
HGSC 0.707
ccRCC
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
S 2448 A Prostate cancer/carcinoma/adenocarcinoma Phosphorylation 22886792
S 2448 U Adrenocortical carcinoma Phosphorylation 20484036
S 2448 U Breast cancer Phosphorylation 36797347
S 2448 U Cervical squamous cell cancer Phosphorylation 19079619
S 2448 U Granulomatosis with polyangiitis Phosphorylation 37720230
S 2448 U Head and neck squamous cell carcinoma Phosphorylation 21281788
S 2448 U Ovarian cancer Phosphorylation 15208673
S 2448 U Pancreatic cancer/carcinoma/adenocarcinoma Phosphorylation 21474066
S 2448 U Liver cancer Phosphorylation 23537100
S 2448 U Non-small cell lung cancer Phosphorylation 33523588

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 Ser2448 TRTDS(ph)YSAGQSVEILDGVELGEPAHKK K562 Dasatinib 7.5641 -
P42345 MTOR P Ser2448 TDS(ph)YSAGQSVEILDGVELGEPAHK BT-474 Lapatinib 6.6312 -
P42345 MTOR P Ser2448 TDS(ph)YSAGQSVEILDGVELGEPAHKK BT-474 Pertuzumab -1.5374 -
P42345 MTOR P Ser2448 TRTDS(ph)YSAGQSVEILDGVELGEPAHKK BT-474 Trastuzumab -1.8853 -
P42345 MTOR P Ser2448 TDS(ph)YSAGQSVEILDGVELGEPAHKK BT-474 Trastuzumab -2.8992 -
P42345 MTOR P Ser2448 TDS(ph)YSAGQSVEILDGVELGEPAHKK HeLa A485 9.9669 -
P42345 MTOR P Ser2448 TRTDS(ph)YSAGQSVEILDGVELGEPAHKK HeLa A485 6.4419 -
P42345 MTOR P Ser2448 TDS(ph)YSAGQSVEILDGVELGEPAHK HeLa A486 5.2648 -
P42345 MTOR P Ser2448 TDS(ph)YSAGQSVEILDGVELGEPAHKK HeLa A486 5.2308 -
P42345 MTOR P Ser2448 TRTDS(ph)YSAGQSVEILDGVELGEPAHKK HeLa A486 5.2273 -
P42345 MTOR P Ser2448 TRTDS(ph)YSAGQSVEILDGVELGEPAHKK K562 Dasatinib 9.2779 -
P42345 MTOR P Ser2448 TDS(ph)YSAGQSVEILDGVELGEPAHKK K562 Dasatinib 9.2546 -
P42345 MTOR P Ser2448 TRTDS(ph)YSAGQSVEILDGVELGEPAHKK K562 Dasatinib 9.2353 -
P42345 MTOR P Ser2448 TDS(ph)YSAGQSVEILDGVELGEPAHK K562 Dasatinib 8.9987 -
P42345 MTOR P Ser2448 TRTDS(ph)YSAGQSVEILDGVELGEPAHK K562 Dasatinib 7.7586 -
P42345 MTOR P Ser2448 TDS(ph)YSAGQSVEILDGVELGEPAHKK BT-474 Lapatinib 6.9171 -
P42345 MTOR P Ser2448 TRTDS(ph)YSAGQSVEILDGVELGEPAHKK K562 Dasatinib 10.7673 -
P42345 MTOR P Ser2448 TRTDS(ph)YSAGQSVEILDGVELGEPAHKK K562 Dasatinib 8.7783 -
P42345 MTOR P Ser2448;Ser2454 TRTDS(ph)YSAGQS(ph)VEILDGVELGEPAHKK K562 Imatinib 8.2056 -
P42345 MTOR P Ser2448 TDS(ph)YSAGQSVEILDGVELGEPAHKK K562 Imatinib 5.4862 -
P42345 MTOR P Ser2448 TDS(ph)YSAGQSVEILDGVELGEPAHKK KYSE-520 SHP099 10.0734 -
P42345 MTOR P Ser2448 TRTDS(ph)YSAGQSVEILDGVELGEPAHKK KYSE-520 SHP099 5.8963 -
P42345 MTOR P Ser2448 TDS(ph)YSAGQSVEILDGVELGEPAHK KYSE-520 SHP099 5.8317 -
P42345 MTOR P Ser2448 TDS(ph)YSAGQSVEILDGVELGEPAHKK PC-9 AZD4547 9.2645 -
P42345 MTOR P Ser2448 TRTDS(ph)YSAGQSVEILDGVELGEPAHK PC-9 AZD4547 7.8622 -
P42345 MTOR P Ser2448 TDS(ph)YSAGQSVEILDGVELGEPAHK PC-9 GeftinibAZD4547-1to80 9.3258 -
P42345 MTOR P Ser2448 TDS(ph)YSAGQSVEILDGVELGEPAHKK PC-9 GeftinibAZD4547-1to80 8.1698 -
P42345 MTOR P Ser2448 TRTDS(ph)YSAGQSVEILDGVELGEPAHKK PC-9 GeftinibAZD4547-1to80 6.2543 -
P42345 MTOR P Ser2448 TDS(ph)YSAGQSVEILDGVELGEPAHKK SK-BR-3 Lapatinib 7.7904 -
P42345 MTOR P Ser2448 TRTDS(ph)YSAGQSVEILDGVELGEPAHKK SK-BR-3 Trastuzumab -2.0623 -
P42345 MTOR P Ser2448 TDS(ph)YSAGQSVEILDGVELGEPAHK A431 Dasatinib 7.2614 -
P42345 MTOR P Ser2448 TDS(ph)YSAGQSVEILDGVELGEPAHKK A431 Afatinib 7.8778 -
P42345 MTOR P Ser2448 TDS(ph)YSAGQSVEILDGVELGEPAHK A431 Afatinib 7.408 -
P42345 MTOR P Ser2448 TDS(ph)YSAGQSVEILDGVELGEPAHK A431 Afatinib 8.2218 -
P42345 MTOR P Ser2448 TDS(ph)YSAGQSVEILDGVELGEPAHK A431 Afatinib 7.6372 -
P42345 MTOR P Ser2448 TDS(ph)YSAGQSVEILDGVELGEPAHK A431 Afatinib 7.7982 -
P42345 MTOR P Ser2448 TDS(ph)YSAGQSVEILDGVELGEPAHKK A431 Dasatinib 10.6207 -
P42345 MTOR P Ser2448 TDS(ph)YSAGQSVEILDGVELGEPAHK A431 Dasatinib 6.7138 -
P42345 MTOR P Ser2448 TDS(ph)YSAGQSVEILDGVELGEPAHK A431 Dasatinib 5.4223 -
P42345 MTOR P Ser2448 TRTDS(ph)YSAGQSVEILDGVELGEPAHK A431 Dasatinib 5.3723 -
P42345 MTOR P Ser2448 TRTDS(ph)YSAGQSVEILDGVELGEPAHKK A431 Dasatinib 2 -
P42345 MTOR P Ser2448 TDS(ph)YSAGQSVEILDGVELGEPAHKK A431 Dasatinib 9.8622 -
P42345 MTOR P Ser2448 TRTDS(ph)YSAGQSVEILDGVELGEPAHK A431 Dasatinib 6.6761 -
P42345 MTOR P Ser2448;Ser2454 TDS(ph)YSAGQS(ph)VEILDGVELGEPAHK A431 Dasatinib 6.0055 -
P42345 MTOR P Ser2448 TDS(ph)YSAGQSVEILDGVELGEPAHK A431 Dasatinib 2.0001 -
P42345 MTOR P Ser2448 TRTDS(ph)YSAGQSVEILDGVELGEPAHK A431 Afatinib 12.0893 -
P42345 MTOR P Ser2448 TRTDS(ph)YSAGQSVEILDGVELGEPAHK A431 Dasatinib 8.9829 -
P42345 MTOR P Ser2448 TDS(ph)YSAGQSVEILDGVELGEPAHK A431 Dasatinib 8.5089 -
P42345 MTOR P Ser2448 TRTDS(ph)YSAGQSVEILDGVELGEPAHK A431 Gefitinib 7.0119 -
P42345 MTOR P Ser2448 TDS(ph)YSAGQSVEILDGVELGEPAHK A431 Gefitinib 6.3584 -
P42345 MTOR P Ser2448 TDS(ph)YSAGQSVEILDGVELGEPAHKK A431 Gefitinib 9.1286 -
P42345 MTOR P Ser2448 TRTDS(ph)YSAGQSVEILDGVELGEPAHK A431 Gefitinib 7.9143 -
P42345 MTOR P Ser2448 TDS(ph)YSAGQSVEILDGVELGEPAHK A431 Gefitinib 6.013 -
P42345 MTOR P Ser2448 TDS(ph)YSAGQSVEILDGVELGEPAHK A431 Gefitinib 5.4977 -
P42345 MTOR P Ser2448 TDS(ph)YSAGQSVEILDGVELGEPAHKK A431 Gefitinib 8.5642 -
P42345 MTOR P Ser2448 TRTDS(ph)YSAGQSVEILDGVELGEPAHK A431 Gefitinib 8.1262 -
P42345 MTOR P Ser2448 TDS(ph)YSAGQSVEILDGVELGEPAHK A431 Gefitinib 7.2534 -
P42345 MTOR P Ser2448 TDS(ph)YSAGQSVEILDGVELGEPAHK A431 Imatinib 16.5229 -
P42345 MTOR P Ser2448 TRTDS(ph)YSAGQSVEILDGVELGEPAHK A431 Imatinib 13.7382 -
P42345 MTOR P Ser2448 TDS(ph)YSAGQSVEILDGVELGEPAHKK A431 Imatinib 6.5676 -

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: