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

MARK3 (P27448) - Overview - Molecular Target Synopsis

Protein


MARK3, MAP/microtubule affinity-regulating kinase 3
Enzyme Classification 2.7.11.1
UniProt P27448

Also Known as MARK3_HUMAN, MARK3, CTAK1, EMK2

Serine/threonine-protein kinase (PubMed:23666762). Involved in the specific phosphorylation of microtubule-associated proteins for MAP2 and MAP4. Phosphorylates the microtubule-associated protein MAPT/TAU (PubMed:23666762). Phosphorylates CDC25C on 'Ser-216'. Regulates localization and activity of some histone deacetylases by mediating phosphorylation of HDAC7, promoting subsequent interaction between HDAC7 and 14-3-3 and export from the nucleus (PubMed:16980613). Negatively regulates the Hippo signaling pathway and antagonizes the phosphorylation of LATS1. Cooperates with DLG5 to inhibit the kinase activity of STK3/MST2 toward LATS1 (PubMed:28087714). Interacts with MAPT/TAU (PubMed:23666762). Interacts with DLG5 (via coiled-coil domain). Interacts with STK3/MST2 and STK4/MST1 in the presence of DLG5 (PubMed:28087714).

3FE3
CRYSTAL STRUCTURE OF THE KINASE MARK3/PAR-1: T211A-S215A DOUBLE MUTANT
RCSB/PDB
Inspect Structure
See all 3D Structures for MARK3

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: MARK3 is active in the following subcellular-locations: cell membrane, cell projection, cytoplasm, dendrite.
GO terms: MARK3 is active in the following subcellular-locations: cytoplasm, cytosol, dendrite, extracellular exosome, plasma membrane.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project MARK3 has gain in 5 cell-lines, loss in 2 cell-lines and no signal in 998 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: SF_268, CCRF_CEM, PC_3

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: Hs 746T, SNU-398, NCI-H209

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, NHLF, HMEC

(see details)

RNA Interference


MARK3 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: CAL51, SCC47. (see details)

3D Structures


For MARK3 there are:
2 structures (4 chains) solved
0 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


MARK3 has been screened with 679 compounds (1130 bioactivities), 14 compounds have bioactivities that show binding affinity of <= 500nM (20 bioactivities). (see details)