Bcl-2-like 1

Target id: 2845

Nomenclature: Bcl-2-like 1

Abbreviated Name: Bcl-xL

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

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

   GtoImmuPdb view: OFF :     Bcl-2-like 1 has curated GtoImmuPdb data

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 233 20q11.21 BCL2L1 BCL2 like 1
Mouse - 233 2 H1 Bcl2l1 BCL2-like 1
Rat - 233 3q41.2 Bcl2l1 Bcl2-like 1
Gene and Protein Information Comments
A shorter human isoform, Bcl-xS, is produced from transcript variant NM_001191 (170 aa). A longer mouse isoform Bcl-x gamma, is produced from transcript variant NM_001289739 (235 aa). For the rat gene we represent the isoform analoghous to the human and mouse in the table above. Note that both a longer rat isoform (284 aa) and a shorter isoform (170 aa) have been reported.
Previous and Unofficial Names
Bcl-X | BCLX | BCL2-like 1
Database Links
ChEMBL Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of Bcl-xL in complex with ABT-737.
PDB Id:  2YXJ
Ligand:  ABT-737
Resolution:  2.2Å
Species:  Human
References:  2

Download all structure-activity data for this target as a CSV file

Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
ABT-737 Hs Antagonist >9.3 pKi 1
pKi >9.3 (Ki <5x10-10 M) [1]
navitoclax Hs Antagonist >9.0 pKi 3
pKi >9.0 (Ki <1x10-9 M) [3]
venetoclax Hs Antagonist 7.3 pKi 4
pKi 7.3 (Ki 4.8x10-8 M) [4]
Immunopharmacology Comments
The role of Bcl-2 family members in immunity and disease is reviewed in [5]. Pharmacological inhibition of Bcl-2 family proteins reduces disease severity in several animal models of autoimmunity; see ligand ABT-737 [1].
Immuno Process Associations
Immuno Process:  Cytokine production & signalling
Immuno Process ID:  9
Comment: 
GO Annotation:  Associated to GO processes
GO Processes:  response to cytokine (GO:0034097) IDA
References: 
Immuno Process:  Antigen presentation
Immuno Process ID:  3
Comment: 
GO Annotation:  Associated to GO processes, IEA only
GO Processes:  endocytosis (GO:0006897) IEA
References: 

References

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1. Bruncko M, Oost TK, Belli BA, Ding H, Joseph MK, Kunzer A, Martineau D, McClellan WJ, Mitten M, Ng SC et al.. (2007) Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL. J. Med. Chem.50 (4): 641-62. [PMID:17256834]

2. Lee EF, Czabotar PE, Smith BJ, Deshayes K, Zobel K, Colman PM, Fairlie WD. (2007) Crystal structure of ABT-737 complexed with Bcl-xL: implications for selectivity of antagonists of the Bcl-2 family. Cell Death Differ.14 (9): 1711-3. [PMID:17572662]

3. Park CM, Bruncko M, Adickes J, Bauch J, Ding H, Kunzer A, Marsh KC, Nimmer P, Shoemaker AR, Song X et al.. (2008) Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins. J. Med. Chem.51 (21): 6902-15. [PMID:18841882]

4. 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]

How to cite this page

B-cell lymphoma 2 (Bcl-2) protein family: Bcl-2-like 1. Last modified on 31/01/2017. Accessed on 19/10/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2845.