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MCL1 apoptosis regulator, BCL2 family member

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Target not currently curated in GtoImmuPdb

Target id: 2847

Nomenclature: MCL1 apoptosis regulator, BCL2 family member

Abbreviated Name: Mcl-1

Family: B-cell lymphoma 2 (Bcl-2) protein family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 350 1q21.2 MCL1 MCL1 apoptosis regulator, BCL2 family member
Mouse 1 331 3 40.74 cM Mcl1 myeloid cell leukemia sequence 1
Rat 1 330 2q34 Mcl1 MCL1 apoptosis regulator, BCL2 family member
Previous and Unofficial Names Click here for help
MCL1 apoptosis regulator | BCL2 family apoptosis regulator | MCL1 | MCL1, BCL2 family apoptosis regulator | myeloid cell leukemia 1
Database Links Click here for help
Alphafold Q07820 (Hs), P97287 (Mm), Q9Z1P3 (Rn)
ChEMBL Target CHEMBL4361 (Hs), CHEMBL5768 (Mm)
Ensembl Gene ENSG00000143384 (Hs), ENSMUSG00000038612 (Mm), ENSRNOG00000063678 (Rn)
Entrez Gene 4170 (Hs), 17210 (Mm), 60430 (Rn)
Human Protein Atlas ENSG00000143384 (Hs)
KEGG Gene hsa:4170 (Hs), mmu:17210 (Mm), rno:60430 (Rn)
OMIM 159552 (Hs)
Pharos Q07820 (Hs)
RefSeq Nucleotide NM_021960 (Hs), NM_008562 (Mm), NM_021846 (Rn)
RefSeq Protein NP_068779 (Hs), NP_032588 (Mm), NP_068618 (Rn)
UniProtKB Q07820 (Hs), P97287 (Mm), Q9Z1P3 (Rn)
Wikipedia MCL1 (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  INDUCED MYELOID LEUKEMIA CELL DIFFERENTIATION PROTEIN FABCOMPLEX IN COMPLEX WITH AZD5991
PDB Id:  6FS0
Ligand:  AZD5991
Resolution:  2.25Å
Species:  Human
References:  3

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Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
AZD5991 Small molecule or natural product Ligand has a PDB structure Hs Antagonist 9.7 pKi 1
⤷ pKi 9.7 (Ki 2x10-10 M) [1]
venetoclax Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Antagonist <6.3 pKi 2
⤷ pKi <6.3 (Ki >4.44x10-7 M) [2]
obatoclax Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Antagonist 5.5 pKi 4
⤷ pKi 5.5 (Ki 2.9x10-6 M) [4]
Description: In vitro antagonism determined in a fluorescence polarisation assay.
Immuno Process Associations
Immuno Process:  Cytokine production & signalling

References

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1. Denis C, Sopková-de Oliveira Santos J, Bureau R, Voisin-Chiret AS. (2020) Hot-Spots of Mcl-1 Protein. J Med Chem, 63 (3): 928-943. [PMID:31580668]

2. Souers AJ, Leverson JD, Boghaert ER, Ackler SL, Catron ND, Chen J, Dayton BD, Ding H, Enschede SH, Fairbrother WJ et al.. (2013) ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets. Nat Med, 19 (2): 202-8. [PMID:23291630]

3. Tron AE, Belmonte MA, Adam A, Aquila BM, Boise LH, Chiarparin E, Cidado J, Embrey KJ, Gangl E, Gibbons FD et al.. (2018) Discovery of Mcl-1-specific inhibitor AZD5991 and preclinical activity in multiple myeloma and acute myeloid leukemia. Nat Commun, 9 (1): 5341. [PMID:30559424]

4. Wan Y, Dai N, Tang Z, Fang H. (2018) Small-molecule Mcl-1 inhibitors: Emerging anti-tumor agents. Eur J Med Chem, 146: 471-482. [PMID:29407973]

How to cite this page

B-cell lymphoma 2 (Bcl-2) protein family: MCL1 apoptosis regulator, BCL2 family member. Last modified on 04/01/2024. Accessed on 18/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2847.