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

CIT (O14578) - Overview - Molecular Target Synopsis

Protein


CIT, Citron Rho-interacting kinase
Enzyme Classification 2.7.11.1
UniProt O14578

Also Known as CTRO_HUMAN, CIT, CRIK, KIAA0949, STK21

Plays a role in cytokinesis. Required for KIF14 localization to the central spindle and midbody. Putative RHO/RAC effector that binds to the GTP-bound forms of RHO and RAC1. It probably binds p21 with a tighter specificity in vivo. Displays serine/threonine protein kinase activity. Plays an important role in the regulation of cytokinesis and the development of the central nervous system. Phosphorylates MYL9/MLC2. Directly interacts with KIF14 depending on the activation state (stronger interaction with the kinase-dead form). Homodimer (By similarity). Interacts with TTC3.

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: CIT is active in the following subcellular-locations: cytoplasm.
GO terms: CIT is active in the following subcellular-locations: cleavage furrow, cytosol, Golgi cisterna, membrane, midbody, neuronal cell body, nucleus.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project CIT has gain in 2 cell-lines, loss in 0 cell-lines and no signal in 1003 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: M14, ACHN, SK_MEL_28

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: G96, G44, COLO-818

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, HeLa-S3, SK-N-SH

(see details)

RNA Interference


CIT was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: SUM44, CAL120. (see details)

3D Structures


At greater than 35% identity similarity to CIT there are:
44 structures (103 chains) solved
42 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


CIT has been screened with 104 compounds (143 bioactivities), 13 compounds have bioactivities that show binding affinity of <= 500nM (21 bioactivities). (see details)