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

CDC42BPB (Q9Y5S2) - Overview - Molecular Target Synopsis

Protein


CDC42BPB, Serine/threonine-protein kinase MRCK beta
Enzyme Classification 2.7.11.1
UniProt Q9Y5S2

Also Known as MRCKB_HUMAN, CDC42BPB, KIAA1124

Serine/threonine-protein kinase which is an important downstream effector of CDC42 and plays a role in the regulation of cytoskeleton reorganization and cell migration. Regulates actin cytoskeletal reorganization via phosphorylation of PPP1R12C and MYL9/MLC2 (PubMed:21457715, PubMed:21949762). In concert with MYO18A and LURAP1, is involved in modulating lamellar actomyosin retrograde flow that is crucial to cell protrusion and migration (PubMed:18854160). Phosphorylates PPP1R12A (PubMed:21457715). In concert with FAM89B/LRAP25 mediates the targeting of LIMK1 to the lamellipodium resulting in its activation and subsequent phosphorylation of CFL1 which is important for lamellipodial F-actin regulation. Homodimer and homotetramer via the coiled coil regions (PubMed:21949762). Interacts tightly with GTP-bound but not GDP-bound CDC42. Interacts with TJP1, when in the presence of catalytically active CDC42 (By similarity). Forms a tripartite complex with MYO18A and LURAP1 with the latter acting as an adapter connecting CDC42BPB and MYO18A. LURAP1 binding results in activation of CDC42BPB by abolition of its negative autoregulation (PubMed:18854160). Interacts with STRIP1, STRN3 and SIKE1 (PubMed:25743393). Interacts with CPNE4 (via VWFA domain). Interacts with LURAP1. Interacts (via AGC-kinase C-terminal domain) with FAM89B/LRAP25 (via LRR repeat). Forms a tripartite complex with FAM89B/LRAP25 and LIMK1.

5OTE
MRCK BETA IN COMPLEX WITH BDP-00008900
RCSB/PDB
Inspect Structure
See all 3D Structures for CDC42BPB

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: CDC42BPB is active in the following subcellular-locations: cell junction, cell membrane, cell projection, cytoplasm, lamellipodium.
GO terms: CDC42BPB is active in the following subcellular-locations: actomyosin, cell leading edge, cell-cell junction, cytoplasm, cytoskeleton, extracellular exosome, lamellipodium, plasma membrane.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project CDC42BPB has gain in 5 cell-lines, loss in 3 cell-lines and no signal in 997 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: SK_OV_3, PC_3, OVCAR_5

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: HCC2302, NIH:OVCAR-3, OCUM-1

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, A549, NHLF

(see details)

RNA Interference


CDC42BPB was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: COV504, PL5. (see details)

3D Structures


For CDC42BPB there are:
6 structures (8 chains) solved
6 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


CDC42BPB has been screened with 663 compounds (1244 bioactivities), 5 compounds have bioactivities that show binding affinity of <= 500nM (6 bioactivities). (see details)