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

PLK2 (Q9NYY3) - Overview - Molecular Target Synopsis

Protein


PLK2, Serine/threonine-protein kinase PLK2
Enzyme Classification 2.7.11.21
UniProt Q9NYY3

Also Known as PLK2_HUMAN, PLK2, SNK

Tumor suppressor serine/threonine-protein kinase involved in synaptic plasticity, centriole duplication and G1/S phase transition. Polo-like kinases act by binding and phosphorylating proteins are that already phosphorylated on a specific motif recognized by the POLO box domains. Phosphorylates CENPJ, NPM1, RAPGEF2, RASGRF1, SNCA, SIPA1L1 and SYNGAP1. Plays a key role in synaptic plasticity and memory by regulating the Ras and Rap protein signaling: required for overactivity-dependent spine remodeling by phosphorylating the Ras activator RASGRF1 and the Rap inhibitor SIPA1L1 leading to their degradation by the proteasome. Conversely, phosphorylates the Rap activator RAPGEF2 and the Ras inhibitor SYNGAP1, promoting their activity. Also regulates synaptic plasticity independently of kinase activity, via its interaction with NSF that disrupts the interaction between NSF and the GRIA2 subunit of AMPARs, leading to a rapid rundown of AMPAR-mediated current that occludes long term depression. Required for procentriole formation and centriole duplication by phosphorylating CENPJ and NPM1, respectively. Its induction by p53/TP53 suggests that it may participate in the mitotic checkpoint following stress. Interacts with NSF; causing NSF dissociation from GRIA2. Interacts with CIB1.

4XB0
STRUCTURE OF THE PLK2 POLO-BOX DOMAIN
RCSB/PDB
Inspect Structure
See all 3D Structures for PLK2

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
685ENSG00000145632ENST00000274289ENSP00000274289Q9NYY3-1

Sub-cellular localization


UniProt: PLK2 is active in the following subcellular-locations: cell projection, centriole, centrosome, cytoplasm, cytoskeleton, dendrite, microtubule organizing center.
GO terms: PLK2 is active in the following subcellular-locations: centriole, centrosome, chromatin, cytoplasm, cytosol, dendrite, intracellular.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project PLK2 has gain in 1 cell-lines, loss in 2 cell-lines and no signal in 1001 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: TK_10, ACHN, A498

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: OVCAR-8, HEY, NCI-H2373

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, HSMM, AG445

(see details)

RNA Interference


PLK2 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: MDAMB134VI, CAL51. (see details)

3D Structures


For PLK2 there are:
7 structures (9 chains) solved
5 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


PLK2 has been screened with 484 compounds (718 bioactivities), 59 compounds have bioactivities that show binding affinity of <= 500nM (70 bioactivities). (see details)