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

SRMS (Q9H3Y6) - Overview - Molecular Target Synopsis

Protein


SRMS, Tyrosine-protein kinase Srms
Enzyme Classification 2.7.10.2
UniProt Q9H3Y6

Also Known as SRMS_HUMAN, SRMS, C20orf148

Non-receptor tyrosine-protein kinase which phosphorylates DOK1 on tyrosine residues (PubMed:23822091). Also phosphorylates KHDRBS1/SAM68 and VIM on tyrosine residues (PubMed:29496907). Phosphorylation of KHDRBS1 is EGF-dependent (PubMed:29496907). Interacts (via the SH2 and SH3 domains) with DOK1 (PubMed:23822091). Interacts with KHDRBS1/SAM68 and VIM (PubMed:29496907).

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
488ENSG00000125508ENST00000217188ENSP00000217188Q9H3Y6-1

Drugs


SRMS is targeted by Approved Drugs Dasatinib, Vandetanib. (see details)
Dasatinib
Vandetanib

Sub-cellular localization


UniProt: SRMS is active in the following subcellular-locations: cytoplasm.
GO terms: SRMS is active in the following subcellular-locations: cytoplasm, cytosol, extrinsic component of cytoplasmic side of plasma membrane.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project SRMS has gain in 7 cell-lines, loss in 1 cell-lines and no signal in 997 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: HCT_116, SN12C, HS578T

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: SUM 52PE, CAL-12T, KATO III

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, NHLF, HSMM

(see details)

RNA Interference


SRMS was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: SKGT4, HCC1954. (see details)

3D Structures


At greater than 50% identity similarity to SRMS there are:
112 structures (188 chains) solved
104 are solved in complex with at least one small molecule ligand
12 are solved with an approved drug

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

AMP/ADENOSINE PHOSPHATE (3DQX_A, 3DQX_B),
1N1/DASATINIB (3G5D_A, 3G5D_B, 3QLG_A, 3QLG_B, 5H2U_A, 5H2U_B, 5H2U_C, 5H2U_D),
DB8/BOSUTINIB (4MXO_A, 4MXO_B, 4MXX_A, 4MXX_B, 4MXY_A, 4MXY_B, 4MXZ_A, 4MXZ_B),
RXT/RUXOLITINIB (4U5J_A, 4U5J_B),
STI/IMATINIB (2OIQ_A, 3OEZ_A, 3OEZ_B, 4CSV_A).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


SRMS has been screened with 490 compounds (905 bioactivities), 8 compounds have bioactivities that show binding affinity of <= 500nM (11 bioactivities). (see details)