Details of the Target

General Information of Target

Target ID LDTP03714
Target Name Polycomb complex protein BMI-1 (BMI1)
Gene Name BMI1
Gene ID 100532731
Synonyms
PCGF4; RNF51; Polycomb complex protein BMI-1; Polycomb group RING finger protein 4; RING finger protein 51
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MHRTTRIKITELNPHLMCVLCGGYFIDATTIIECLHSFCKTCIVRYLETSKYCPICDVQV
HKTRPLLNIRSDKTLQDIVYKLVPGLFKNEMKRRRDFYAAHPSADAANGSNEDRGEVADE
DKRIITDDEIISLSIEFFDQNRLDRKVNKDKEKSKEEVNDKRYLRCPAAMTVMHLRKFLR
SKMDIPNTFQIDVMYEEEPLKDYYTLMDIAYIYTWRRNGPLPLKYRVRPTCKRMKISHQR
DGLTNAGELESDSGSDKANSPAGGIPSTSSCLPSPSTPVQSPHPQFPHISSTMNGTSNSP
SGNHQSSFANRPRKSSVNGSSATSSG
Target Type
Clinical trial
Target Bioclass
Enzyme
Subcellular location
Nucleus
Function
Component of a Polycomb group (PcG) multiprotein PRC1-like complex, a complex class required to maintain the transcriptionally repressive state of many genes, including Hox genes, throughout development. PcG PRC1 complex acts via chromatin remodeling and modification of histones; it mediates monoubiquitination of histone H2A 'Lys-119', rendering chromatin heritably changed in its expressibility. The complex composed of RNF2, UB2D3 and BMI1 binds nucleosomes, and has activity only with nucleosomal histone H2A. In the PRC1-like complex, regulates the E3 ubiquitin-protein ligase activity of RNF2/RING2.
TTD ID
T74066
Uniprot ID
P35226
DrugMap ID
TTIPNSR
Ensemble ID
ENST00000376663.8
HGNC ID
HGNC:1066
ChEMBL ID
CHEMBL4295749

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 12 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		15.00  LDD0402  [1]
STPyne
 Probe Info  		K235(2.27)  LDD0277  [2]
Probe 1
 Probe Info  		Y80(12.31)  LDD3495  [3]
DBIA
 Probe Info  		C53(2.94); C56(2.94)  LDD0080  [4]
4-Iodoacetamidophenylacetylene
 Probe Info  		N.A.  LDD0038  [5]
IA-alkyne
 Probe Info  		N.A.  LDD0036  [5]
Lodoacetamide azide
 Probe Info  		N.A.  LDD0037  [5]
IPM
 Probe Info  		N.A.  LDD0005  [6]
TFBX
 Probe Info  		N.A.  LDD0148  [7]
Phosphinate-6
 Probe Info  		N.A.  LDD0018  [8]
AOyne
 Probe Info  		14.90  LDD0443  [9]
NAIA_5
 Probe Info  		N.A.  LDD2223  [10]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0632  CL-Sc Hep-G2 C166(1.47)  LDD2227  [10]
 LDCM0625  F8 Ramos C166(1.88)  LDD2187  [11]
 LDCM0576  Fragment14 Ramos C166(0.62)  LDD2193  [11]
 LDCM0569  Fragment7 Ramos C166(0.65)  LDD2186  [11]
 LDCM0022  KB02 HCT 116 C53(2.94); C56(2.94)  LDD0080  [4]
 LDCM0023  KB03 HCT 116 C53(7.32); C56(7.32)  LDD0081  [4]
 LDCM0024  KB05 HCT 116 C53(2.33); C56(2.33)  LDD0082  [4]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 8 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Helicase MOV-10 (MOV10) DNA2/NAM7 helicase family Q9HCE1
Ubiquitin carboxyl-terminal hydrolase 11 (USP11) Peptidase C19 family P51784
Ubiquitin carboxyl-terminal hydrolase 7 (USP7) Peptidase C19 family Q93009
Casein kinase II subunit alpha (CSNK2A1) Ser/Thr protein kinase family P68400
Phosphatidylinositol 3,4,5-trisphosphate 3-phosphatase and dual-specificity protein phosphatase PTEN (PTEN) PTEN phosphatase protein family P60484
E3 SUMO-protein ligase CBX4 (CBX4) . O00257
E3 ubiquitin-protein ligase RING1 (RING1) . Q06587
E3 ubiquitin-protein ligase RING2 (RNF2) . Q99496
Other
Click To Hide/Show 11 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Nuclear distribution protein nudE-like 1 (NDEL1) NudE family Q9GZM8
Polyubiquitin-C (UBC) Ubiquitin family P0CG48
Vacuolar protein sorting-associated protein 11 homolog (VPS11) VPS11 family Q9H270
Chromobox protein homolog 6 (CBX6) . O95503
Chromobox protein homolog 7 (CBX7) . O95931
Chromobox protein homolog 8 (CBX8) . Q9HC52
Heat shock factor 2-binding protein (HSF2BP) . O75031
Polyhomeotic-like protein 1 (PHC1) . P78364
Polyhomeotic-like protein 2 (PHC2) . Q8IXK0
Pre-mRNA-processing factor 6 (PRPF6) . O94906
Whirlin (WHRN) . Q9P202

References

1 Quantitative and Site-Specific Chemoproteomic Profiling of Targets of Acrolein. Chem Res Toxicol. 2019 Mar 18;32(3):467-473. doi: 10.1021/acs.chemrestox.8b00343. Epub 2019 Jan 15.
2 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
3 An Azo Coupling-Based Chemoproteomic Approach to Systematically Profile the Tyrosine Reactivity in the Human Proteome. Anal Chem. 2021 Jul 27;93(29):10334-10342. doi: 10.1021/acs.analchem.1c01935. Epub 2021 Jul 12.
4 Reimagining high-throughput profiling of reactive cysteines for cell-based screening of large electrophile libraries. Nat Biotechnol. 2021 May;39(5):630-641. doi: 10.1038/s41587-020-00778-3. Epub 2021 Jan 4.
5 Enhancing Cysteine Chemoproteomic Coverage through Systematic Assessment of Click Chemistry Product Fragmentation. Anal Chem. 2022 Mar 8;94(9):3800-3810. doi: 10.1021/acs.analchem.1c04402. Epub 2022 Feb 23.
Mass spectrometry data entry: PXD028853
6 A modification-centric assessment tool for the performance of chemoproteomic probes. Nat Chem Biol. 2022 Aug;18(8):904-912. doi: 10.1038/s41589-022-01074-8. Epub 2022 Jul 21.
Mass spectrometry data entry: PXD027758 , PXD027755 , PXD027760 , PXD027762 , PXD027756 , PXD027591 , PXD007149 , PXD030064 , PXD032392 , PXD027789 , PXD027767 , PXD027764
7 Chemoproteomic Profiling by Cysteine Fluoroalkylation Reveals Myrocin G as an Inhibitor of the Nonhomologous End Joining DNA Repair Pathway. J Am Chem Soc. 2021 Dec 8;143(48):20332-20342. doi: 10.1021/jacs.1c09724. Epub 2021 Nov 24.
Mass spectrometry data entry: PXD029255
8 DFT-Guided Discovery of Ethynyl-Triazolyl-Phosphinates as Modular Electrophiles for Chemoselective Cysteine Bioconjugation and Profiling. Angew Chem Int Ed Engl. 2022 Oct 10;61(41):e202205348. doi: 10.1002/anie.202205348. Epub 2022 Aug 22.
Mass spectrometry data entry: PXD033004
9 Chemoproteomic profiling of targets of lipid-derived electrophiles by bioorthogonal aminooxy probe. Redox Biol. 2017 Aug;12:712-718. doi: 10.1016/j.redox.2017.04.001. Epub 2017 Apr 5.
10 N-Acryloylindole-alkyne (NAIA) enables imaging and profiling new ligandable cysteines and oxidized thiols by chemoproteomics. Nat Commun. 2023 Jun 15;14(1):3564. doi: 10.1038/s41467-023-39268-w.
Mass spectrometry data entry: PXD041264
11 Site-specific quantitative cysteine profiling with data-independent acquisition-based mass spectrometry. Methods Enzymol. 2023;679:295-322. doi: 10.1016/bs.mie.2022.07.037. Epub 2022 Sep 7.
Mass spectrometry data entry: PXD027578