Molecular Target Synopsis
Overview
Domains and Structures
Drugs and Clinical Candidates
Druggability
Chemistry
Ligand Efficiency Plot
Pathways
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
RNAi
Mutations
Germline Genetics

RPS6KA2 (Q15349) - Overview - Molecular Target Synopsis

Protein


RPS6KA2, Ribosomal protein S6 kinase alpha-2
Enzyme Classification 2.7.11.1
UniProt Q15349

Also Known as KS6A2_HUMAN, RPS6KA2, MAPKAPK1C, RSK3

Serine/threonine-protein kinase that acts downstream of ERK (MAPK1/ERK2 and MAPK3/ERK1) signaling and mediates mitogenic and stress-induced activation of transcription factors, regulates translation, and mediates cellular proliferation, survival, and differentiation. May function as tumor suppressor in epithelial ovarian cancer cells. Forms a complex with either MAPK1/ERK2 or MAPK3/ERK1 in quiescent cells. Transiently dissociates following mitogenic stimulation (By similarity). Interacts with FBXO5; cooperate to induce the metaphase arrest of early blastomeres; increases and stabilizes interaction of FBXO5 with CDC20.

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: RPS6KA2 is active in the following subcellular-locations: cytoplasm, nucleus.
GO terms: RPS6KA2 is active in the following subcellular-locations: cytoplasm, cytosol, nucleoplasm, nucleus.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project RPS6KA2 has gain in 0 cell-lines, loss in 6 cell-lines and no signal in 999 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: M14, HS578T, OVCAR_3

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: SK-N-FI, MeWo, M059K

In Array Express (RNA-seq of long poly adenylated RNA and long non poly adenylated RNA from ENCODE cell lines), the highest expressing cell lines are: SK-N-SH, NHLF, HSMM

(see details)

RNA Interference


RPS6KA2 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: HS578T, MDAMB231. (see details)

3D Structures


At greater than 90% identity similarity to RPS6KA2 there are:
9 structures (10 chains) solved
9 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


RPS6KA2 has been screened with 1068 compounds (1882 bioactivities), 237 compounds have bioactivities that show binding affinity of <= 500nM (252 bioactivities). (see details)