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

RACGAP1 (Q9H0H5) - Overview - Molecular Target Synopsis

Protein


RACGAP1, Rac GTPase-activating protein 1
UniProt Q9H0H5

Also Known as RGAP1_HUMAN, RACGAP1, KIAA1478, MGCRACGAP

Component of the centralspindlin complex that serves as a microtubule-dependent and Rho-mediated signaling required for the myosin contractile ring formation during the cell cycle cytokinesis. Required for proper attachment of the midbody to the cell membrane during cytokinesis. Plays key roles in controlling cell growth and differentiation of hematopoietic cells through mechanisms other than regulating Rac GTPase activity. Also involved in the regulation of growth-related processes in adipocytes and myoblasts. May be involved in regulating spermatogenesis and in the RACGAP1 pathway in neuronal proliferation. Shows strong GAP (GTPase activation) activity towards CDC42 and RAC1 and less towards RHOA. Essential for the early stages of embryogenesis. May play a role in regulating cortical activity through RHOA during cytokinesis. May participate in the regulation of sulfate transport in male germ cells. Heterotetramer of two molecules each of RACGAP1 and KIF23. Found in the centralspindlin complex composed of RACGAP1 and KIF23. Associates with alpha-, beta- and gamma-tubulin and microtubules. Interacts via its Rho-GAP domain with RND2. Associates with AURKB during M phase. Interacts via its Rho-GAP domain and basic region with PRC1. The interaction with PRC1 inhibits its GAP activity towards CDC42 in vitro, which may be required for maintaining normal spindle morphology. Interacts with SLC26A8 via its N-terminus. Interacts with RAB11FIP3. Interacts with ECT2; the interaction is direct, occurs at anaphase and during cytokinesis in a microtubule-dependent manner and is enhanced by phosphorylation by PLK1. Interacts with KIF23; the interaction is direct.

5C2J
COMPLEX STRUCTURE OF THE GAP DOMAIN OF MGCRACGAP AND CDC42
RCSB/PDB
Inspect Structure
See all 3D Structures for RACGAP1

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: RACGAP1 is active in the following subcellular-locations: acrosome, cell membrane, cleavage furrow, cytoplasm, cytoplasmic vesicle, cytoskeleton, midbody, midbody ring, nucleus, secretory vesicle, spindle.
GO terms: RACGAP1 is active in the following subcellular-locations: acrosomal vesicle, centralspindlin complex, cleavage furrow, cytosol, extracellular exosome, extrinsic component of cytoplasmic side of plasma membrane, Flemming body, microtubule, midbody, mitotic spindle, nucleoplasm, nucleus, spindle midzone.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project RACGAP1 has gain in 0 cell-lines, loss in 0 cell-lines and no signal in 1005 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: SF_268, HS578T, T47D

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: UM-UC-3, HEY, OVCAR-8

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: HeLa-S3, HMEC, MCF-7

(see details)

3D Structures


For RACGAP1 there are:
7 structures (14 chains) solved
1 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


RACGAP1 has been screened with compounds ( bioactivities). (see details)