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

CDK16 (Q00536) - Overview - Molecular Target Synopsis

Protein


CDK16, Cyclin-dependent kinase 16
Enzyme Classification 2.7.11.22
UniProt Q00536

Also Known as CDK16_HUMAN, CDK16, PCTAIRE1, PCTK1

Protein kinase that plays a role in vesicle-mediated transport processes and exocytosis. Regulates GH1 release by brain neurons. Phosphorylates NSF, and thereby regulates NSF oligomerization. Required for normal spermatogenesis. Regulates neuron differentiation and dendrite development (By similarity). Plays a role in the regulation of insulin secretion in response to changes in blood glucose levels. Can phosphorylate CCNY at 'Ser-336' (in vitro). Found in a complex containing CABLES1, CDK17 and TDRD7. Interacts with YWHAH, YWHAQ and YWHAZ. Interacts with NSF. Identified in a complex with NSF, syntaxin-1, synaptotagmin, SYN1, SYP and CDK5R1 (By similarity). Interacts with BRSK2. Interacts with CCNY; this increases the CDK16 kinase activity.

5G6V
CRYSTAL STRUCTURE OF THE PCTAIRE1 KINASE IN COMPLEX WITH INHIBITOR
RCSB/PDB
Inspect Structure
See all 3D Structures for CDK16

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: CDK16 is active in the following subcellular-locations: cell junction, cell membrane, cytoplasm, cytoplasmic vesicle, secretory vesicle, synapse, synaptosome.
GO terms: CDK16 is active in the following subcellular-locations: cell junction, cytoplasm, cytosol, extrinsic component of cytoplasmic side of plasma membrane, microtubule cytoskeleton, neuron projection, nucleus, plasma membrane, synaptic vesicle.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project CDK16 has gain in 1 cell-lines, loss in 61 cell-lines and no signal in 943 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: HCC12, COV318, SiHa

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, HeLa-S3, HMEC

(see details)

RNA Interference


CDK16 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: OAW42, HUO3N1. (see details)

3D Structures


For CDK16 there are:
2 structures (3 chains) solved
2 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


CDK16 has been screened with 322 compounds (441 bioactivities), 14 compounds have bioactivities that show binding affinity of <= 500nM (27 bioactivities). (see details)