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

CDC42 (P60953) - Overview - Molecular Target Synopsis

Protein


CDC42, Cell division control protein 42 homolog
UniProt P60953

Also Known as CDC42_HUMAN, CDC42

Plasma membrane-associated small GTPase which cycles between an active GTP-bound and an inactive GDP-bound state. In active state binds to a variety of effector proteins to regulate cellular responses. Involved in epithelial cell polarization processes. Regulates the bipolar attachment of spindle microtubules to kinetochores before chromosome congression in metaphase. Plays a role in the extension and maintenance of the formation of thin, actin-rich surface projections called filopodia. Mediates CDC42-dependent cell migration. Required for DOCK10-mediated spine formation in Purkinje cells and hippocampal neurons. Facilitates filopodia formation upon DOCK11-activation (By similarity). Also plays a role in phagocytosis through organization of the F-actin cytoskeleton associated with forming phagocytic cups. Interacts with CDC42EP1, CDC42EP2, CDC42EP3, CDC42EP4, CDC42EP5, CDC42SE1, CDC42SE2, PARD6A, PARD6B and PARD6G (in a GTP-dependent manner) (PubMed:10490598, PubMed:10816584, PubMed:10954424, PubMed:11260256). Interacts with activated CSPG4 and with BAIAP2 (PubMed:10587647, PubMed:11130076). Interacts with activated CSPG4 and with BAIAP2 (By similarity). Interacts with DOCK11/Zizimin2; the interaction activates CDC42 by exchanging GDP for GTP (By similarity). Interacts with DOCK9; the interaction activates CDC42 by exchanging GDP for GTP (PubMed:12172552, PubMed:19745154). Interacts with DOCK8 (via DHR-2 domain); the interaction activates CDC42 by exchanging GDP for GTP (PubMed:12172552). Interacts with IQGAP1 (By similarity). Interacts with NET1 and ARHGAP33/TCGAP (By similarity). Part of a complex with PARD3, PARD6A or PARD6B and PRKCI or PRKCZ (PubMed:11260256). The GTP-bound form interacts with CCPG1 (By similarity). Interacts with USP6 (PubMed:12612085). Interacts with NEK6 (PubMed:20873783). Part of a collagen stimulated complex involved in cell migration composed of CDC42, CRK, TNK2 and BCAR1/p130cas (PubMed:17038317). Interacts with ITGB1BP1 (PubMed:11807099). Interacts with ARHGDIA; this interaction inactivates and stabilizes CDC42 (PubMed:23434736). Interacts with ARHGDIB; this maintains CDC42 in the inactive, GDP-bound form (PubMed:7512369). Interacts (in GTP-bound form) with FNBP1L and ABI1, but only in the presence of FNBP1L (PubMed:19798448). May interact with ARHGEF16; responsible for the activation of CDC42 by the viral protein HPV16 E6 (PubMed:21139582).

2WMO
STRUCTURE OF THE COMPLEX BETWEEN DOCK9 AND CDC42.
RCSB/PDB
Inspect Structure
See all 3D Structures for CDC42

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: CDC42 is active in the following subcellular-locations: cell membrane, centrosome, cytoplasm, cytoskeleton, microtubule organizing center, midbody, spindle.
GO terms: CDC42 is active in the following subcellular-locations: cell cortex, cell projection, cytoplasm, cytoplasmic ribonucleoprotein granule, cytosol, dendritic spine, endoplasmic reticulum membrane, extracellular exosome, filopodium, focal adhesion, Golgi membrane, Golgi transport complex, membrane, microtubule organizing center, midbody, mitotic spindle, neuron projection, neuronal cell body, plasma membrane, protein-containing complex, spindle midzone.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project CDC42 has gain in 1 cell-lines, loss in 0 cell-lines and no signal in 1004 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: 786_0, RXF_393, U251

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: Okajima, Hs 746T, AGS

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, HSMM, HMEC

(see details)

3D Structures


For CDC42 there are:
40 structures (64 chains) solved
24 are solved in complex with at least one small molecule ligand
1 are solved with an approved drug

CDC42 is solved in complex with the approved drug(s):

AMP/ADENOSINE PHOSPHATE (4ITR_C, 4ITR_D).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


CDC42 has been screened with 57 compounds (87 bioactivities), 1 compounds have bioactivities that show binding affinity of <= 500nM (1 bioactivities). (see details)