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

WEE1 (P30291) - Overview - Molecular Target Synopsis

Protein


WEE1, Wee1-like protein kinase
Enzyme Classification 2.7.10.2
UniProt P30291

Also Known as WEE1_HUMAN, WEE1

Acts as a negative regulator of entry into mitosis (G2 to M transition) by protecting the nucleus from cytoplasmically activated cyclin B1-complexed CDK1 before the onset of mitosis by mediating phosphorylation of CDK1 on 'Tyr-15'. Specifically phosphorylates and inactivates cyclin B1-complexed CDK1 reaching a maximum during G2 phase and a minimum as cells enter M phase. Phosphorylation of cyclin B1-CDK1 occurs exclusively on 'Tyr-15' and phosphorylation of monomeric CDK1 does not occur. Its activity increases during S and G2 phases and decreases at M phase when it is hyperphosphorylated. A correlated decrease in protein level occurs at M/G1 phase, probably due to its degradation.

5VD9
CRYSTAL STRUCTURE OF HUMAN WEE1 KINASE DOMAIN IN COMPLEX WITH RAC-IV- 097, A MK1775 ANALOGUE
RCSB/PDB
Inspect Structure
See all 3D Structures for WEE1

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: WEE1 is active in the following subcellular-locations: nucleus.
GO terms: WEE1 is active in the following subcellular-locations: cytoplasm, nucleolus, nucleoplasm, nucleus.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project WEE1 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: K_562, SF_268, HS578T

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: SU-DHL-6, RI-1, HT

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: NHLF, K562, SK-N-SH

(see details)

RNA Interference


WEE1 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: ZR7530, H727. (see details)

3D Structures


For WEE1 there are:
20 structures (20 chains) solved
20 are solved in complex with at least one small molecule ligand
1 are solved with an approved drug

WEE1 is solved in complex with the approved drug(s):

DB8/BOSUTINIB (5VC3_A).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


WEE1 has been screened with 446 compounds (816 bioactivities), 227 compounds have bioactivities that show binding affinity of <= 500nM (484 bioactivities). (see details)