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

KRAS (P01116) - Overview - Molecular Target Synopsis

Protein


KRAS, GTPase KRas
UniProt P01116

Also Known as RASK_HUMAN, KRAS, KRAS2, RASK2

Ras proteins bind GDP/GTP and possess intrinsic GTPase activity. Plays an important role in the regulation of cell proliferation (PubMed:23698361, PubMed:22711838). Plays a role in promoting oncogenic events by inducing transcriptional silencing of tumor suppressor genes (TSGs) in colorectal cancer (CRC) cells in a ZNF304-dependent manner (PubMed:24623306). Interacts with PHLPP. Interacts (active GTP-bound form preferentially) with RGS14 (By similarity). Interacts (when farnesylated) with PDE6D; this promotes dissociation from the cell membrane (PubMed:23698361). Interacts with SOS1 (PubMed:22431598).

6EPN
RAS GUANINE EXCHANGE FACTOR SOS1 (REM-CDC25) IN COMPLEX WITH KRAS(G12C) AND FRAGMENT SCREENING HIT F2
RCSB/PDB
Inspect Structure
See all 3D Structures for KRAS

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: KRAS is active in the following subcellular-locations: cell membrane, cytoplasm, cytosol.
GO terms: KRAS is active in the following subcellular-locations: cytoplasm, cytosol, extrinsic component of cytoplasmic side of plasma membrane, focal adhesion, membrane, membrane raft, mitochondrion, plasma membrane.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project KRAS has gain in 36 cell-lines, loss in 3 cell-lines and no signal in 966 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: OVCAR_5, SW_620, DU_145

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: A4/Fuk, HCC630, BEN

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: NHLF, AG445, NHEK

(see details)

3D Structures


For KRAS there are:
119 structures (284 chains) solved
112 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


KRAS has been screened with 15 compounds (20 bioactivities). (see details)