Molecular Target Synopsis
Domains and Structures
Drugs and Clinical Candidates
Ligand Efficiency Plot
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
Germline Genetics

SIK3 (Q9Y2K2) - Overview - Molecular Target Synopsis


SIK3, Serine/threonine-protein kinase SIK3
Enzyme Classification
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.

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)