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

MASTL (Q96GX5) - Overview - Molecular Target Synopsis

Protein


MASTL, Serine/threonine-protein kinase greatwall
Enzyme Classification 2.7.11.1
UniProt Q96GX5

Also Known as GWL_HUMAN, MASTL, GW, GWL, THC2

Serine/threonine kinase that plays a key role in M phase by acting as a regulator of mitosis entry and maintenance. Acts by promoting the inactivation of protein phosphatase 2A (PP2A) during M phase: does not directly inhibit PP2A but acts by mediating phosphorylation and subsequent activation of ARPP19 and ENSA at 'Ser-62' and 'Ser-67', respectively. ARPP19 and ENSA are phosphatase inhibitors that specifically inhibit the PPP2R2D (PR55-delta) subunit of PP2A. Inactivation of PP2A during M phase is essential to keep cyclin-B1-CDK1 activity high. Following DNA damage, it is also involved in checkpoint recovery by being inhibited. Phosphorylates histone protein in vitro; however such activity is unsure in vivo. May be involved in megakaryocyte differentiation.

5LOH
KINASE DOMAIN OF HUMAN GREATWALL
RCSB/PDB
Inspect Structure
See all 3D Structures for MASTL

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: MASTL is active in the following subcellular-locations: centrosome, cleavage furrow, cytoplasm, cytoskeleton, microtubule organizing center, nucleus.
GO terms: MASTL is active in the following subcellular-locations: centrosome, cleavage furrow, cytoplasm, nucleoplasm, nucleus.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project MASTL has gain in 4 cell-lines, loss in 8 cell-lines and no signal in 993 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: MDA_MB_231, OVCAR_4, RXF_393

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: NCI-H196, HCC38, MHH-NB-11

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: MCF-7, SK-N-SH, K562

(see details)

RNA Interference


MASTL was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: HCH1, MDAMB453. (see details)

3D Structures


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



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


MASTL has been screened with compounds ( bioactivities). (see details)