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

SIK3 (Q9Y2K2) - Overview - Molecular Target Synopsis

Protein


SIK3, Serine/threonine-protein kinase SIK3
Enzyme Classification 2.7.11.1
UniProt Q9Y2K2

Also Known as SIK3_HUMAN, SIK3, KIAA0999, QSK

Inhibits CREB activity by phosphorylating and inhibiting activity of TORCs, the CREB-specific coactivators, like CRTC2/TORC2 and CRTC3/TORC3 in response to cAMP signaling. Binds to and is activated by YWHAZ when phosphorylated on Thr-221 (PubMed:16306228). Interacts (when phosphorylated at Thr-469 and/or Ser-551) with 14-3-3 proteins; the interaction inhibits kinase activity towards TORCs (PubMed:29211348).

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: SIK3 is active in the following subcellular-locations: cytoplasm.
GO terms: SIK3 is active in the following subcellular-locations: cytoplasm.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project SIK3 has gain in 1 cell-lines, loss in 5 cell-lines and no signal in 999 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are:

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: MHH-ES-1, MKN-74, A-673

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: CD20-positive B cell, CD14-positive monocyte, HMEC

(see details)

RNA Interference


SIK3 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: SUM149, MIAPACA2. (see details)

3D Structures


At greater than 50% identity similarity to SIK3 there are:
15 structures (41 chains) solved
4 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


SIK3 has been screened with 91 compounds (99 bioactivities), 7 compounds have bioactivities that show binding affinity of <= 500nM (9 bioactivities). (see details)