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

RHOH (Q15669) - Overview - Molecular Target Synopsis

Protein


RHOH, Rho-related GTP-binding protein RhoH
UniProt Q15669

Also Known as RHOH_HUMAN, RHOH, ARHH, TTF

Negative regulator of hematopoietic progenitor cell proliferation, survival and migration. Critical regulator of thymocyte development and T-cell antigen receptor (TCR) signaling by mediating recruitment and activation of ZAP70. Required for phosphorylation of CD3Z, membrane translocation of ZAP70 and subsequent activation of the ZAP70-mediated pathways. Essential for efficient beta-selection and positive selection by promoting the ZAP70-dependent phosphorylation of the LAT signalosome during pre-TCR and TCR signaling. Crucial for thymocyte maturation during DN3 to DN4 transition and during positive selection. Plays critical roles in mast cell function by facilitating phosphorylation of SYK in Fc epsilon RI-mediated signal transduction. Essential for the phosphorylation of LAT, LCP2, PLCG1 and PLCG2 and for Ca(2+) mobilization in mast cells (By similarity). Binds GTP but lacks intrinsic GTPase activity and is resistant to Rho-specific GTPase-activating proteins. Inhibits the activation of NF-kappa-B by TNF and IKKB and the activation of CRK/p38 by TNF. Inhibits activities of RAC1, RHOA and CDC42. Negatively regulates leukotriene production in neutrophils. Interacts with ZAP70 (via SH2 domains) and the interaction is enhanced by its phosphorylation by LCK. Interacts with SYK and the interaction is enhanced by its phosphorylation by FYN (By similarity). Interacts with GDI1 and GDI2. Interacts with PAK5.

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: RHOH is active in the following subcellular-locations: cell membrane, cytoplasm.
GO terms: RHOH is active in the following subcellular-locations: cell cortex, cell projection, cytoplasm, cytosol, immunological synapse, plasma membrane.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project RHOH has gain in 1 cell-lines, loss in 2 cell-lines and no signal in 1002 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: CCRF_CEM, MOLT_4, RPMI_8226

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: Daudi, TK, Pfeiffer

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: GM12878, CD20-positive B cell, SK-N-SH

(see details)

3D Structures


At greater than 35% identity similarity to RHOH there are:
146 structures (250 chains) solved
114 are solved in complex with at least one small molecule ligand
4 are solved with an approved drug

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

FMN/RIBOFLAVIN 5'-PHOSPHATE (2WKP_A, 2WKQ_A, 2WKR_A),
AMP/ADENOSINE PHOSPHATE (4ITR_C, 4ITR_D).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


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