Id: | acc1361 |
Group: | 2sens |
Protein: | Raptor |
Gene Symbol: | RPTOR |
Protein Id: | Q8N122 |
Protein Name: | RPTOR_HUMAN |
PTM: | phosphorylation |
Site: | Ser792 |
Site Sequence: | TIDKMRRASSYSSLNSLIGVS |
Disease Category: | Cancer |
Disease: | Prostate Cancer |
Disease Subtype: | CRPC |
Disease Cellline: | C4-2 |
Disease Info: | |
Drug: | salinomycin |
Drug Info: | "Salinomycin is a polyether ionophore antibiotic primarily used as an anticoccidial agent in poultry and as a growth promoter in livestock, with emerging research interest in its potential anticancer properties. " |
Effect: | modulate |
Effect Info: | "Salinomycin inhibits the phosphorylation of AR and promotes the phosphorylation of AMPK. The activation of AMPK leads to an increase in the phosphorylation of Raptor and TSC2 at Ser1387. Meanwhile, salinomycin also blocks the inhibitory phosphorylation of TSC2 (Ser939/Thr1462) by AKT, thereby inhibiting AR and mTORC1 through a dual - effect mechanism." |
Note: | |
Score: | 4.0 |
Pubmed(PMID): | 27557496 |
Sentence Index: | 27557496_11-12 |
Sentence: | AMPK-mediated raptor phosphorylation further reduced mTOR's kinase function and mTORC1 activity. Our novel finding on dual inhibition of AR and mTORC1 suggests that salinomycin is potentially active as monotherapy against advanced prostate cancer. |
Sequence & Structure:
MESEMLQSPLLGLGEEDEADLTDWNLPLAFMKKRHCEKIEGSKSLAQSWRMKDRMKTVSVALVLCLNVGVDPPDVVKTTPCARLECWIDPLSMGPQKALETIGANLQKQYENWQPRARYKQSLDPTVDEVKKLCTSLRRNAKEERVLFHYNGHGVPRPTVNGEVWVFNKNYTQYIPLSIYDLQTWMGSPSIFVYDCSNAGLIVKSFKQFALQREQELEVAAINPNHPLAQMPLPPSMKNCIQLAACEATELLPMIPDLPADLFTSCLTTPIKIALRWFCMQKCVSLVPGVTLDLIEKIPGRLNDRRTPLGELNWIFTAITDTIAWNVLPRDLFQKLFRQDLLVASLFRNFLLAERIMRSYNCTPVSSPRLPPTYMHAMWQAWDLAVDICLSQLPTIIEEGTAFRHSPFFAEQLTAFQVWLTMGVENRNPPEQLPIVLQVLLSQVHRLRALDLLGRFLDLGPWAVSLALSVGIFPYVLKLLQSSARELRPLLVFIWAKILAVDSSCQADLVKDNGHKYFLSVLADPYMPAEHRTMTAFILAVIVNSYHTGQEACLQGNLIAICLEQLNDPHPLLRQWVAICLGRIWQNFDSARWCGVRDSAHEKLYSLLSDPIPEVRCAAVFALGTFVGNSAERTDHSTTIDHNVAMMLAQLVSDGSPMVRKELVVALSHLVVQYESNFCTVALQFIEEEKNYALPSPATTEGGSLTPVRDSPCTPRLRSVSSYGNIRAVATARSLNKSLQNLSLTEESGGAVAFSPGNLSTSSSASSTLGSPENEEHILSFETIDKMRRASSYSSLNSLIGVSFNSVYTQIWRVLLHLAADPYPEVSDVAMKVLNSIAYKATVNARPQRVLDTSSLTQSAPASPTNKGVHIHQAGGSPPASSTSSSSLTNDVAKQPVSRDLPSGRPGTTGPAGAQYTPHSHQFPRTRKMFDKGPEQTADDADDAAGHKSFISATVQTGFCDWSARYFAQPVMKIPEEHDLESQIRKEREWRFLRNSRVRRQAQQVIQKGITRLDDQIFLNRNPGVPSVVKFHPFTPCIAVADKDSICFWDWEKGEKLDYFHNGNPRYTRVTAMEYLNGQDCSLLLTATDDGAIRVWKNFADLEKNPEMVTAWQGLSDMLPTTRGAGMVVDWEQETGLLMSSGDVRIVRIWDTDREMKVQDIPTGADSCVTSLSCDSHRSLIVAGLGDGSIRVYDRRMALSECRVMTYREHTAWVVKASLQKRPDGHIVSVSVNGDVRIFDPRMPESVNVLQIVKGLTALDIHPQADLIACGSVNQFTAIYNSSGELINNIKYYDGFMGQRVGAISCLAFHPHWPHLAVGSNDYYISVYSVEKRVR
Select PDB:
Target | Drug name | MOA | Phase | Status | Disease | Source |
---|---|---|---|---|---|---|
RPTOR | INDOXIMOD | mTORC1 activator | 2 | Completed | metastatic prostate cancer | ClinicalTrials |
RPTOR | INDOXIMOD | mTORC1 activator | 2 | Terminated | melanoma | ClinicalTrials |
RPTOR | INDOXIMOD | mTORC1 activator | 2 | Completed | breast cancer | ClinicalTrials |
RPTOR | INDOXIMOD | mTORC1 activator | 1 | Completed | acute myeloid leukemia | ClinicalTrials |
RPTOR | INDOXIMOD | mTORC1 activator | 1 | Completed | glioblastoma multiforme | ClinicalTrials |
RPTOR | INDOXIMOD | mTORC1 activator | 1 | Withdrawn | neoplasm | ClinicalTrials |
RPTOR | INDOXIMOD | mTORC1 activator | 1 | Completed | metastatic melanoma | ClinicalTrials |
RPTOR | INDOXIMOD | mTORC1 activator | 1 | Completed | pancreatic carcinoma | ClinicalTrials |
RPTOR | INDOXIMOD | mTORC1 activator | 1 | Completed | medulloblastoma | ClinicalTrials |
RPTOR | INDOXIMOD | mTORC1 activator | 1 | Terminated | non-small cell lung carcinoma | ClinicalTrials |
RPTOR | INDOXIMOD | mTORC1 activator | 1 | Completed | ependymoma | ClinicalTrials |
RPTOR | INDOXIMOD | mTORC1 activator | 1 | Completed | pancreatic adenocarcinoma | ClinicalTrials |
RPTOR | INDOXIMOD | mTORC1 activator | 1 | Completed | Paraganglioma | ClinicalTrials ClinicalTrials |
RPTOR | INDOXIMOD | mTORC1 activator | 1 | Completed | gliosarcoma | ClinicalTrials ClinicalTrials |
RPTOR | INDOXIMOD | mTORC1 activator | 1 | Completed | brain cancer | ClinicalTrials |
Note: Only show clinically investigational or approved drugs with protein targets.
Protein Tractability:
source: Open TargetsPTM Intensity:
source: CPTACNo intensity data of this site,
show all other sites!
RPTOR-Ser538 | |
---|---|
Cancer | Intensity |
BRCA | |
COAD | |
HGSC | -2.105 |
ccRCC | 0.199 |
GBM | -0.127 |
HNSC | 1.471 |
LUAD | 0.179 |
LUSC | 0.328 |
non_ccRCC | |
PDAC | -0.294 |
UCEC | 0.349 |
RPTOR-Ser546 | |
---|---|
Cancer | Intensity |
BRCA | |
COAD | |
HGSC | -1.002 |
ccRCC | 0.116 |
GBM | 0.758 |
HNSC | 1.261 |
LUAD | -1.333 |
LUSC | |
non_ccRCC | |
PDAC | |
UCEC | 0.201 |
RPTOR-Ser561 | |
---|---|
Cancer | Intensity |
BRCA | 0.611 |
COAD | 1.039 |
HGSC | 2.041 |
ccRCC | -1.116 |
GBM | 0.372 |
HNSC | -0.804 |
LUAD | -0.716 |
LUSC | 0.15 |
non_ccRCC | 0.268 |
PDAC | -1.07 |
UCEC | -0.774 |
RPTOR-Ser563 | |
---|---|
Cancer | Intensity |
BRCA | |
COAD | |
HGSC | 1.094 |
ccRCC | |
GBM | |
HNSC | |
LUAD | -0.227 |
LUSC | -0.867 |
non_ccRCC | |
PDAC | |
UCEC |
RPTOR-Ser564 | |
---|---|
Cancer | Intensity |
BRCA | |
COAD | -1.082 |
HGSC | 0.89 |
ccRCC | |
GBM | |
HNSC | |
LUAD | |
LUSC | |
non_ccRCC | 0.192 |
PDAC | |
UCEC |
RPTOR-Ser701 | |
---|---|
Cancer | Intensity |
BRCA | -1.62 |
COAD | 0.741 |
HGSC | -1.71 |
ccRCC | -0.602 |
GBM | 0.636 |
HNSC | 1.239 |
LUAD | 0.522 |
LUSC | -0.209 |
non_ccRCC | 1.07 |
PDAC | 0.229 |
UCEC | -0.296 |
RPTOR-Ser705 | |
---|---|
Cancer | Intensity |
BRCA | 1.313 |
COAD | 0.847 |
HGSC | -0.085 |
ccRCC | -0.686 |
GBM | -0.814 |
HNSC | 0.98 |
LUAD | -1.463 |
LUSC | 1.334 |
non_ccRCC | 0.141 |
PDAC | -0.401 |
UCEC | -1.165 |
RPTOR-Ser719 | |
---|---|
Cancer | Intensity |
BRCA | -1.177 |
COAD | -0.534 |
HGSC | 1.727 |
ccRCC | 0.003 |
GBM | 0.631 |
HNSC | -0.167 |
LUAD | -0.06 |
LUSC | 1.458 |
non_ccRCC | -1.489 |
PDAC | -0.695 |
UCEC | 0.304 |
RPTOR-Ser723 | |
---|---|
Cancer | Intensity |
BRCA | |
COAD | 0.037 |
HGSC | |
ccRCC | |
GBM | 0.447 |
HNSC | -1.4 |
LUAD | |
LUSC | |
non_ccRCC | |
PDAC | |
UCEC | 0.916 |
RPTOR-Ser724 | |
---|---|
Cancer | Intensity |
BRCA | |
COAD | -0.707 |
HGSC | |
ccRCC | |
GBM | 0.707 |
HNSC | |
LUAD | |
LUSC | |
non_ccRCC | |
PDAC | |
UCEC |
RPTOR-Ser726 | |
---|---|
Cancer | Intensity |
BRCA | |
COAD | 0.288 |
HGSC | |
ccRCC | -0.985 |
GBM | 1.396 |
HNSC | |
LUAD | -0.964 |
LUSC | |
non_ccRCC | |
PDAC | |
UCEC | 0.264 |
RPTOR-Ser727 | |
---|---|
Cancer | Intensity |
BRCA | |
COAD | 0.131 |
HGSC | |
ccRCC | 1.489 |
GBM | -0.574 |
HNSC | |
LUAD | 0.143 |
LUSC | |
non_ccRCC | |
PDAC | |
UCEC | -1.19 |
RPTOR-Ser729 | |
---|---|
Cancer | Intensity |
BRCA | |
COAD | 1.067 |
HGSC | |
ccRCC | 1.493 |
GBM | -1.426 |
HNSC | -0.694 |
LUAD | -0.226 |
LUSC | 0.039 |
non_ccRCC | |
PDAC | |
UCEC | -0.253 |
RPTOR-Thr541 | |
---|---|
Cancer | Intensity |
BRCA | |
COAD | |
HGSC | |
ccRCC | -0.558 |
GBM | |
HNSC | |
LUAD | -0.596 |
LUSC | |
non_ccRCC | |
PDAC | |
UCEC | 1.154 |
RPTOR-Thr542 | |
---|---|
Cancer | Intensity |
BRCA | |
COAD | |
HGSC | -0.443 |
ccRCC | |
GBM | |
HNSC | |
LUAD | -0.702 |
LUSC | |
non_ccRCC | |
PDAC | |
UCEC | 1.145 |
RPTOR-Thr548 | |
---|---|
Cancer | Intensity |
BRCA | -0.574 |
COAD | |
HGSC | 0.94 |
ccRCC | -0.645 |
GBM | 0.28 |
HNSC | 0.05 |
LUAD | -1.178 |
LUSC | 2.253 |
non_ccRCC | -0.633 |
PDAC | -0.639 |
UCEC | 0.146 |
RPTOR-Thr556 | |
---|---|
Cancer | Intensity |
BRCA | |
COAD | |
HGSC | -0.707 |
ccRCC | |
GBM | |
HNSC | |
LUAD | |
LUSC | |
non_ccRCC | |
PDAC | |
UCEC | 0.707 |
RPTOR-Thr699 | |
---|---|
Cancer | Intensity |
BRCA | |
COAD | |
HGSC | |
ccRCC | -0.559 |
GBM | |
HNSC | 1.155 |
LUAD | -0.595 |
LUSC | |
non_ccRCC | |
PDAC | |
UCEC |
RPTOR-Thr725 | |
---|---|
Cancer | Intensity |
BRCA | |
COAD | -0.07 |
HGSC | 0.448 |
ccRCC | -0.985 |
GBM | 1.266 |
HNSC | -0.906 |
LUAD | -0.965 |
LUSC | |
non_ccRCC | |
PDAC | |
UCEC | 1.212 |
RPTOR-Tyr534 | |
---|---|
Cancer | Intensity |
BRCA | |
COAD | |
HGSC | |
ccRCC | -0.927 |
GBM | |
HNSC | |
LUAD | -0.132 |
LUSC | |
non_ccRCC | |
PDAC | |
UCEC | 1.059 |
PTM-Disease Association:
source: PTMDNo data.
PTM-Drug Perturbation Response:
source: DecryptMNo data.
Function score:
source: funscoRNo data.