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

STK10 (O94804) - Overview - Molecular Target Synopsis

Protein


STK10, Serine/threonine-protein kinase 10
Enzyme Classification 2.7.11.1
UniProt O94804

Also Known as STK10_HUMAN, STK10, LOK

Serine/threonine-protein kinase involved in regulation of lymphocyte migration. Phosphorylates MSN, and possibly PLK1. Involved in regulation of lymphocyte migration by mediating phosphorylation of ERM proteins such as MSN. Acts as a negative regulator of MAP3K1/MEKK1. May also act as a cell cycle regulator by acting as a polo kinase kinase: mediates phosphorylation of PLK1 in vitro; however such data require additional evidences in vivo. Homodimer; homodimerization is required for activation segment autophosphorylation.

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
968ENSG00000072786ENST00000176763ENSP00000176763O94804-1
278ENSG00000072786ENST00000520476ENSP00000428806

Sub-cellular localization


UniProt: STK10 is active in the following subcellular-locations: cell membrane.
GO terms: STK10 is active in the following subcellular-locations: cytoplasm, extracellular exosome, plasma membrane, specific granule membrane.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project STK10 has gain in 2 cell-lines, loss in 4 cell-lines and no signal in 998 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: HL_60, SK_MEL_28, M14

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: WM-115, HNT-34, HEL

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, HMEC, CD14-positive monocyte

(see details)

RNA Interference


STK10 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: PCI30, BEN. (see details)

3D Structures


There are 11 structures (18 chains) solved for STK10
11 are solved in complex with at least one small molecule ligand
2 are solved with an approved drug

STK10 is solved in complex with the approved drug(s):

EUI/COBIMETINIB (4AN2_A),
DB8/BOSUTINIB (4QMN_A, 5AJQ_A, 5AJQ_B),
1N1/DASATINIB (4QMS_A, 5OWR_A),
B49/SUNITINIB (4KS8_A, 4QMZ_A).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


STK10 has been screened with 774 compounds (1450 bioactivities), 35 compounds have bioactivities that show binding affinity of <= 500nM (62 bioactivities). (see details)