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

KSR1 (Q8IVT5) - Overview - Molecular Target Synopsis

Protein


KSR1, Kinase suppressor of Ras 1
UniProt Q8IVT5

Also Known as KSR1_HUMAN, KSR1, KSR

Scaffolding protein that is part of a multiprotein signaling complex. Promotes phosphorylation of Raf family members and activation of downstream MAP kinases. Promotes activation of MAPK1 and/or MAPK3, both in response to EGF and to cAMP. Does not have kinase activity by itself. Interacts with HSP90AA1/HSP90, YWHAE/14-3-3, CDC37, MAP2K1/MEK-1 and MAP2K2/MEK-2 (PubMed:10409742). Interacts with MARK3, PPP2R1A and PPP2CA. Also interacts with RAF and MAPK/ERK, in a Ras-dependent manner. The binding of 14-3-3 proteins to phosphorylated KSR prevents the membrane localization (By similarity). Interacts with isoform 1 of VRK2 (PubMed:20679487). Interacts with AKAP13 and BRAF (PubMed:21102438). Identified in a complex with AKAP13, MAP2K1 and BRAF.

5VYK
CRYSTAL STRUCTURE OF THE BRS DOMAIN OF BRAF IN COMPLEX WITH THE CC-SAM DOMAIN OF KSR1
RCSB/PDB
Inspect Structure
See all 3D Structures for KSR1

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: KSR1 is active in the following subcellular-locations: cell membrane, cell projection, cytoplasm, endoplasmic reticulum membrane, membrane, ruffle membrane.
GO terms: KSR1 is active in the following subcellular-locations: cytosol, endoplasmic reticulum, endoplasmic reticulum membrane, membrane, protein-containing complex, ruffle membrane.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project KSR1 has gain in 3 cell-lines, loss in 3 cell-lines and no signal in 999 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: SR, K_562, OVCAR_3

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: HEL, SNU-182, OCI-M1

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: K562, GM12878, HUVEC

(see details)

RNA Interference


KSR1 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: SCC47, PL5. (see details)

3D Structures


For KSR1 there are:
1 structures (2 chains) solved
0 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


KSR1 has been screened with compounds ( bioactivities). (see details)