Id: acc0342
Group: 1sens
Protein: S6K
Gene Symbol: RPS6KB1
Protein Id: P23443
Protein Name: KS6B1_HUMAN
PTM: phosphorylation
Site: Thr389
Site Sequence: SQFDSKFTRQTPVDSPDDSTL
Disease Category: Cancer
Disease: Colorectal Cancer
Disease Subtype:
Disease Cellline: HT29
Disease Info:
Drug: AZD2014
Drug Info: AZD2014 (Vistusertib) is an ATP-competitive mTOR inhibitor targeting both mTORC1 and mTORC2 complexes with an IC50 of 2.81 nM.
Effect: modulate
Effect Info: "AZD-2014 inhibits the phosphorylation of S6K and S6, thereby preventing the activation of mTORC1, and inhibits the phosphorylation of Akt (Ser 473), thereby preventing the activation of mTORC2, which in turn activates autophagy in colorectal cancer cells."
Note:
Score: 4.0
Pubmed(PMID): 24309100
Sentence Index:
Sentence:

Sequence & Structure:

MRRRRRRDGFYPAPDFRDREAEDMAGVFDIDLDQPEDAGSEDELEEGGQLNESMDHGGVGPYELGMEHCEKFEISETSVNRGPEKIRPECFELLRVLGKGGYGKVFQVRKVTGANTGKIFAMKVLKKAMIVRNAKDTAHTKAERNILEEVKHPFIVDLIYAFQTGGKLYLILEYLSGGELFMQLEREGIFMEDTACFYLAEISMALGHLHQKGIIYRDLKPENIMLNHQGHVKLTDFGLCKESIHDGTVTHTFCGTIEYMAPEILMRSGHNRAVDWWSLGALMYDMLTGAPPFTGENRKKTIDKILKCKLNLPPYLTQEARDLLKKLLKRNAASRLGAGPGDAGEVQAHPFFRHINWEELLARKVEPPFKPLLQSEEDVSQFDSKFTRQTPVDSPDDSTLSESANQVFLGFTYVAPSVLESVKEKFSFEPKIRSPRRFIGSPRTPVSPVKFSPGDFWGRGASASTANPQTPVEYPMETSGIEQMDVTMSGEASAPLPIRQPNSGPYKKQAFPMISKRPEHLRMNL

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

Target Drug name MOA Phase Status Disease Source
RPS6KB1 TAS0612 Ribosomal protein S6 kinase (P70S6K) inhibitor 1 Recruiting neoplasm ClinicalTrials
RPS6KB1 MSC-2363318A Ribosomal protein S6 kinase (P70S6K) inhibitor 1 Completed neoplasm ClinicalTrials
RPS6KB1 LY-2780301 Ribosomal protein S6 kinase (P70S6K) inhibitor 1 Completed lymphoma ClinicalTrials
RPS6KB1 XL-418 Ribosomal protein S6 kinase (P70S6K) inhibitor 1 Suspended neoplasm ClinicalTrials
RPS6KB1 LY-2584702 Ribosomal protein S6 kinase 1 inhibitor 1 Terminated renal cell carcinoma ClinicalTrials
RPS6KB1 LY-2584702 Ribosomal protein S6 kinase 1 inhibitor 1 Terminated non-small cell lung carcinoma ClinicalTrials
RPS6KB1 LY-2584702 Ribosomal protein S6 kinase 1 inhibitor 1 Terminated metastasis ClinicalTrials
RPS6KB1 LY-2780301 Ribosomal protein S6 kinase (P70S6K) inhibitor 1 Completed metastasis ClinicalTrials
RPS6KB1 LY-2584702 Ribosomal protein S6 kinase 1 inhibitor 1 Terminated neuroendocrine neoplasm ClinicalTrials
RPS6KB1 LY-2584702 Ribosomal protein S6 kinase 1 inhibitor 1 Completed cancer ClinicalTrials
RPS6KB1 LY-2584702 Ribosomal protein S6 kinase 1 inhibitor 1 Terminated cancer ClinicalTrials
RPS6KB1 XL-418 Ribosomal protein S6 kinase (P70S6K) inhibitor 1 Suspended cancer 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
RPS6KB1-Thr389
Cancer Intensity
BRCA
COAD
HGSC
ccRCC 0.707
GBM -0.707
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
T 389 P Liver cancer Phosphorylation 23537100

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

No data.

Function score:

source: funscoR

No data.

Cross Links: