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

MCL1 (Q07820) - Overview - Molecular Target Synopsis

Protein


MCL1, Induced myeloid leukemia cell differentiation protein Mcl-1
UniProt Q07820

Also Known as MCL1_HUMAN, MCL1, BCL2L3

Involved in the regulation of apoptosis versus cell survival, and in the maintenance of viability but not of proliferation. Mediates its effects by interactions with a number of other regulators of apoptosis. Isoform 1 inhibits apoptosis. Isoform 2 promotes apoptosis. Interacts with HIF3A (via C-terminus domain) (By similarity). Interacts with BAD, BOK, BIK and BMF (By similarity). Interacts with PMAIP1 (PubMed:17389404). Interacts with BBC3 (By similarity). Isoform 1 interacts with BAX, BAK1 and TPT1 (PubMed:10837489, PubMed:12149273, PubMed:15077116). Heterodimer of isoform 1 and isoform 2. Homodimers of isoform 1 or isoform 2 are not detected. Isoform 2 does not interact with pro-apoptotic BCL2-related proteins (PubMed:10837489). Interacts with RTL10/BOP (PubMed:23055042). Interacts with BCL2L11; may sequester BCL2L11 to prevent its pro-apoptotic activity (PubMed:10837489, PubMed:27013495, PubMed:17389404, PubMed:20562877). Interacts with GIMAP5 and HSPA8/HSC70; the interaction between HSPA8 and MCL1 is impaired in the absence of GIMAP5 (By similarity).

6QZ5
STRUCTURE OF MCL-1 IN COMPLEX WITH COMPOUND 8A
RCSB/PDB
Inspect Structure
See all 3D Structures for MCL1

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
350ENSG00000143384ENST00000369026ENSP00000358022Q07820-1
271ENSG00000143384ENST00000307940ENSP00000309973Q07820-2

Sub-cellular localization


UniProt: MCL1 is active in the following subcellular-locations: cytoplasm, membrane, mitochondrion, nucleoplasm, nucleus.
GO terms: MCL1 is active in the following subcellular-locations: Bcl-2 family protein complex, cytoplasm, cytosol, integral component of membrane, membrane, mitochondrial outer membrane, mitochondrion, nucleoplasm, nucleus.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project MCL1 has gain in 23 cell-lines, loss in 0 cell-lines and no signal in 982 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: SR, SF_539, KM12

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: HCC1599, NCI-H2135, NCI-H929

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)

3D Structures


For MCL1 there are:
83 structures (185 chains) solved
57 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


MCL1 has been screened with 2297 compounds (2919 bioactivities), 361 compounds have bioactivities that show binding affinity of <= 500nM (603 bioactivities). (see details)