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

MARK1 (Q9P0L2) - Overview - Molecular Target Synopsis

Protein


MARK1, Serine/threonine-protein kinase MARK1
Enzyme Classification 2.7.11.1
UniProt Q9P0L2

Also Known as MARK1_HUMAN, MARK1, KIAA1477, MARK

Serine/threonine-protein kinase (PubMed:23666762). Involved in cell polarity and microtubule dynamics regulation. Phosphorylates DCX, MAP2 and MAP4. Phosphorylates the microtubule-associated protein MAPT/TAU (PubMed:23666762). Involved in cell polarity by phosphorylating the microtubule-associated proteins MAP2, MAP4 and MAPT/TAU at KXGS motifs, causing detachment from microtubules, and their disassembly. Involved in the regulation of neuronal migration through its dual activities in regulating cellular polarity and microtubule dynamics, possibly by phosphorylating and regulating DCX. Also acts as a positive regulator of the Wnt signaling pathway, probably by mediating phosphorylation of dishevelled proteins (DVL1, DVL2 and/or DVL3). Interacts with MAPT/TAU.

6C9D
CRYSTAL STRUCTURE OF KA1-AUTOINHIBITED MARK1 KINASE
RCSB/PDB
Inspect Structure
See all 3D Structures for MARK1

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: MARK1 is active in the following subcellular-locations: cell membrane, cell projection, cytoplasm, cytoskeleton, dendrite.
GO terms: MARK1 is active in the following subcellular-locations: cytoplasm, cytoskeleton, dendrite, microtubule cytoskeleton, plasma membrane.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project MARK1 has gain in 2 cell-lines, loss in 1 cell-lines and no signal in 1002 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: SF_268, NCI_H322M, HOP_62

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: KYSE-70, NCI-H209, NCI-H2106

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: HSMM, NHLF, A549

(see details)

RNA Interference


MARK1 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: RMGI, MCF12A. (see details)

3D Structures


For MARK1 there are:
3 structures (11 chains) solved
0 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


MARK1 has been screened with 782 compounds (1391 bioactivities), 9 compounds have bioactivities that show binding affinity of <= 500nM (13 bioactivities). (see details)