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

PKMYT1 (Q99640) - Overview - Molecular Target Synopsis

Protein


PKMYT1, Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase
Enzyme Classification 2.7.11.1
UniProt Q99640

Also Known as PMYT1_HUMAN, PKMYT1, MYT1

Acts as a negative regulator of entry into mitosis (G2 to M transition) by phosphorylation of the CDK1 kinase specifically when CDK1 is complexed to cyclins. Mediates phosphorylation of CDK1 predominantly on 'Thr-14'. Also involved in Golgi fragmentation. May be involved in phosphorylation of CDK1 on 'Tyr-15' to a lesser degree, however tyrosine kinase activity is unclear and may be indirect. May be a downstream target of Notch signaling pathway during eye development. Interacts with CDC2-CCNB1 complex. Can also interact with PIN1 when phosphorylated by CDC2-CCNB1.

5VCX
CRYSTAL STRUCTURE OF HUMAN MYT1 KINASE DOMAIN (UNTREATED) IN COMPLEX WITH SARACATINIB
RCSB/PDB
Inspect Structure
See all 3D Structures for PKMYT1

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: PKMYT1 is active in the following subcellular-locations: endoplasmic reticulum membrane, golgi apparatus membrane.
GO terms: PKMYT1 is active in the following subcellular-locations: cytosol, endoplasmic reticulum, endoplasmic reticulum membrane, Golgi apparatus, Golgi membrane, membrane, nucleolus, nucleoplasm, nucleus.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project PKMYT1 has gain in 0 cell-lines, loss in 0 cell-lines and no signal in 1005 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: NCI_ADR_RES, SK_OV_3, K_562

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: SK23, SiHa, LN-229

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: K562, A549, SK-N-SH

(see details)

RNA Interference


PKMYT1 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: MIAPACA2, TE10. (see details)

3D Structures


For PKMYT1 there are:
9 structures (10 chains) solved
8 are solved in complex with at least one small molecule ligand
2 are solved with an approved drug

PKMYT1 is solved in complex with the approved drug(s):

1N1/DASATINIB (5VCV_A),
DB8/BOSUTINIB (5VCY_A).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


PKMYT1 has been screened with 129 compounds (205 bioactivities), 5 compounds have bioactivities that show binding affinity of <= 500nM (6 bioactivities). (see details)