Details of the Target

General Information of Target

Target ID LDTP05529
Target Name Bcl-2-like protein 1 (BCL2L1)
Gene Name BCL2L1
Gene ID 598
Synonyms
BCL2L; BCLX; Bcl-2-like protein 1; Bcl2-L-1; Apoptosis regulator Bcl-X
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSQSNRELVVDFLSYKLSQKGYSWSQFSDVEENRTEAPEGTESEMETPSAINGNPSWHLA
DSPAVNGATGHSSSLDAREVIPMAAVKQALREAGDEFELRYRRAFSDLTSQLHITPGTAY
QSFEQVVNELFRDGVNWGRIVAFFSFGGALCVESVDKEMQVLVSRIAAWMATYLNDHLEP
WIQENGGWDTFVELYGNNAAAESRKGQERFNRWFLTGMTVAGVVLLGSLFSRK
Target Type
Clinical trial
Target Bioclass
Transporter and channel
Family
Bcl-2 family
Subcellular location
Mitochondrion inner membrane
Function
Potent inhibitor of cell death. Inhibits activation of caspases. Appears to regulate cell death by blocking the voltage-dependent anion channel (VDAC) by binding to it and preventing the release of the caspase activator, CYC1, from the mitochondrial membrane. Also acts as a regulator of G2 checkpoint and progression to cytokinesis during mitosis.; Isoform Bcl-X(L) also regulates presynaptic plasticity, including neurotransmitter release and recovery, number of axonal mitochondria as well as size and number of synaptic vesicle clusters. During synaptic stimulation, increases ATP availability from mitochondria through regulation of mitochondrial membrane ATP synthase F(1)F(0) activity and regulates endocytic vesicle retrieval in hippocampal neurons through association with DMN1L and stimulation of its GTPase activity in synaptic vesicles. May attenuate inflammation impairing NLRP1-inflammasome activation, hence CASP1 activation and IL1B release.; Isoform Bcl-X(S) promotes apoptosis.
TTD ID
T56510
Uniprot ID
Q07817
DrugMap ID
TTU1E82
Ensemble ID
ENST00000307677.5
HGNC ID
HGNC:992
ChEMBL ID
CHEMBL4625

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
BT549 SNV: p.G227A .
DOTC24510 SNV: p.A84E .
HT115 SNV: p.E32D .
HUH28 SNV: p.E32Q .
L428 SNV: p.N136K .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
STPyne
 Probe Info  		K87(10.00)  LDD0277  [1]
Jackson_14
 Probe Info  		2.00  LDD0123  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0016  Ranjitkar_cp1 MDA-MB-231 2.00  LDD0123  [2]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Very long chain fatty acid elongase 4 (ELOVL4) ELO family Q9GZR5
NACHT, LRR and PYD domains-containing protein 1 (NLRP1) NLRP family Q9C000
Serine/threonine-protein kinase mTOR (MTOR) PI3/PI4-kinase family P42345
E3 ubiquitin-protein ligase RNF4 (RNF4) . P78317
Transporter and channel
Click To Hide/Show 10 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Apoptosis regulator BAX (BAX) Bcl-2 family Q07812
Bcl-2 homologous antagonist/killer (BAK1) Bcl-2 family Q16611
Bcl-2-like protein 1 (BCL2L1) Bcl-2 family Q07817
Bcl-2-like protein 11 (BCL2L11) Bcl-2 family O43521
Beclin-1 (BECN1) Beclin family Q14457
Protein spinster homolog 1 (SPNS1) Spinster (TC 2.A.1.49) family Q9H2V7
Cellular tumor antigen p53 (TP53) P53 family P04637
Alpha-synuclein (SNCA) Synuclein family P37840
Transmembrane protein 50B (TMEM50B) UPF0220 family P56557
Granulysin (GNLY) . P22749
Other
Click To Hide/Show 16 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Apoptosis-stimulating of p53 protein 2 (TP53BP2) ASPP family Q13625
Bcl-2-binding component 3, isoforms 1/2 (BBC3) Bcl-2 family Q9BXH1
Bcl-2-modifying factor (BMF) Bcl-2 family Q96LC9
Bcl2-associated agonist of cell death (BAD) Bcl-2 family Q92934
Receptor expression-enhancing protein 4 (REEP4) DP1 family Q9H6H4
Endoplasmic reticulum-Golgi intermediate compartment protein 3 (ERGIC3) ERGIC family Q9Y282
Golgi membrane protein 1 (GOLM1) GOLM family Q8NBJ4
RAB6-interacting golgin (GORAB) GORAB family Q5T7V8
Translation initiation factor IF-3, mitochondrial (MTIF3) IF-3 family Q9H2K0
Activator of apoptosis harakiri (HRK) . O00198
Apoptosis regulatory protein Siva (SIVA1) . O15304
Bcl-2-interacting killer (BIK) . Q13323
BH3-interacting domain death agonist (BID) . P55957
G0/G1 switch protein 2 (G0S2) . P27469
Protein BNIP5 (BNIP5) . P0C671
Protein Bop (RTL10) . Q7L3V2

The Drug(s) Related To This Target

Phase 3
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Abt-263 Small molecular drug D06ETI
Phase 2
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Apg-1252 Small molecular drug D4WN2M
Azd0466 Small molecular drug DQ1P6X
Obatoclax Small molecular drug D02OZK
Investigative
Click To Hide/Show 6 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
4'-fluoro-1,1'-biphenyl-4-carboxylic Acid Small molecular drug D0T3VP
4'-fluoro-11'-biphenyl-4-carboxylic Acid Small molecular drug DB07108
Eapb0203 Small molecular drug D2SJZ9
Gossypol Small molecular drug DB13044
E-003 . D09FWK
Wehi-0103122 . D04IPX
Patented
Click To Hide/Show 7 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Indole-based Analog 2 Small molecular drug D0C2DV
Indole-based Analog 3 Small molecular drug D0MZ7I
Pmid27744724-compound-10 Small molecular drug D0IS8R
Pmid27744724-compound-18 Small molecular drug D0TU3N
Pmid27744724-compound-21 Small molecular drug D0J9FN
Pmid27744724-compound-26 Small molecular drug D09XWR
Pmid27744724-compound-27 Small molecular drug D0F9QC

References

1 A Paal-Knorr agent for chemoproteomic profiling of targets of isoketals in cells. Chem Sci. 2021 Oct 15;12(43):14557-14563. doi: 10.1039/d1sc02230j. eCollection 2021 Nov 10.
Mass spectrometry data entry: PXD028270
2 Appendage and Scaffold Diverse Fully Functionalized Small-Molecule Probes via a Minimalist Terminal Alkyne-Aliphatic Diazirine Isocyanide. J Org Chem. 2018 Sep 21;83(18):11245-11253. doi: 10.1021/acs.joc.8b01831. Epub 2018 Aug 31.