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

STK36 (Q9NRP7) - Overview - Molecular Target Synopsis

Protein


STK36, Serine/threonine-protein kinase 36
Enzyme Classification 2.7.11.1
UniProt Q9NRP7

Also Known as STK36_HUMAN, STK36, KIAA1278

Serine/threonine protein kinase which plays an important role in the sonic hedgehog (Shh) pathway by regulating the activity of GLI transcription factors (PubMed:10806483). Controls the activity of the transcriptional regulators GLI1, GLI2 and GLI3 by opposing the effect of SUFU and promoting their nuclear localization (PubMed:10806483). GLI2 requires an additional function of STK36 to become transcriptionally active, but the enzyme does not need to possess an active kinase catalytic site for this to occur (PubMed:10806483). Required for postnatal development, possibly by regulating the homeostasis of cerebral spinal fluid or ciliary function (By similarity). Essential for construction of the central pair apparatus of motile cilia. Interacts with GLI1, GLI2 and GLI3 (PubMed:10806483). Interacts with SPAG16 and KIF27.

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: STK36 is active in the following subcellular-locations: cytoplasm, nucleus.
GO terms: STK36 is active in the following subcellular-locations: cytoplasm, cytosol, extracellular region, nucleus.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project STK36 has gain in 0 cell-lines, loss in 2 cell-lines and no signal in 1003 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: SK_MEL_28, NCI_H522, SR

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: MDA-MB-134-VI, OvCA 432, SNU-398

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, K562, IMR-90

(see details)

RNA Interference


STK36 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, MDAMB231. (see details)

3D Structures


At greater than 35% identity similarity to STK36 there are:
50 structures (75 chains) solved
36 are solved in complex with at least one small molecule ligand
3 are solved with an approved drug

STK36 is solved in complex with the approved drug(s):

DB8/BOSUTINIB (5AJQ_A, 5AJQ_B, 6FDY_U),
1N1/DASATINIB (5OWR_A).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


STK36 has been screened with 107 compounds (177 bioactivities), 7 compounds have bioactivities that show binding affinity of <= 500nM (10 bioactivities). (see details)