Target Information
| Target General Information | Top | |||||
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| Target ID |
T35809
(Former ID: TTDI03063)
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| Target Name |
Bromodomain-containing protein 1 (BRD1)
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| Synonyms |
Bromodomain and PHD finger-containing protein 2; BRPF2; BRL; BR140-like protein
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| Gene Name |
BRD1
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| Target Type |
Literature-reported target
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[1] | ||||
| Function |
Component of the MOZ/MORF complex which has a histone H3 acetyltransferase activity.
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| BioChemical Class |
Bromodomain
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| UniProt ID | ||||||
| Sequence |
MRRKGRCHRGSAARHPSSPCSVKHSPTRETLTYAQAQRMVEIEIEGRLHRISIFDPLEII
LEDDLTAQEMSECNSNKENSERPPVCLRTKRHKNNRVKKKNEALPSAHGTPASASALPEP KVRIVEYSPPSAPRRPPVYYKFIEKSAEELDNEVEYDMDEEDYAWLEIVNEKRKGDCVPA VSQSMFEFLMDRFEKESHCENQKQGEQQSLIDEDAVCCICMDGECQNSNVILFCDMCNLA VHQECYGVPYIPEGQWLCRHCLQSRARPADCVLCPNKGGAFKKTDDDRWGHVVCALWIPE VGFANTVFIEPIDGVRNIPPARWKLTCYLCKQKGVGACIQCHKANCYTAFHVTCAQKAGL YMKMEPVKELTGGGTTFSVRKTAYCDVHTPPGCTRRPLNIYGDVEMKNGVCRKESSVKTV RSTSKVRKKAKKAKKALAEPCAVLPTVCAPYIPPQRLNRIANQVAIQRKKQFVERAHSYW LLKRLSRNGAPLLRRLQSSLQSQRSSQQRENDEEMKAAKEKLKYWQRLRHDLERARLLIE LLRKREKLKREQVKVEQVAMELRLTPLTVLLRSVLDQLQDKDPARIFAQPVSLKEVPDYL DHIKHPMDFATMRKRLEAQGYKNLHEFEEDFDLIIDNCMKYNARDTVFYRAAVRLRDQGG VVLRQARREVDSIGLEEASGMHLPERPAAAPRRPFSWEDVDRLLDPANRAHLGLEEQLRE LLDMLDLTCAMKSSGSRSKRAKLLKKEIALLRNKLSQQHSQPLPTGPGLEGFEEDGAALG PEAGEEVLPRLETLLQPRKRSRSTCGDSEVEEESPGKRLDAGLTNGFGGARSEQEPGGGL GRKATPRRRCASESSISSSNSPLCDSSFNAPKCGRGKPALVRRHTLEDRSELISCIENGN YAKAARIAAEVGQSSMWISTDAAASVLEPLKVVWAKCSGYPSYPALIIDPKMPRVPGHHN GVTIPAPPLDVLKIGEHMQTKSDEKLFLVLFFDNKRSWQWLPKSKMVPLGIDETIDKLKM MEGRNSSIRKAVRIAFDRAMNHLSRVHGEPTSDLSDID Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| Cell-based Target Expression Variations | Top | |||||
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| Cell-based Target Expression Variations | ||||||
| Drug Binding Sites of Target | Top | |||||
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| Ligand Name: OF-1 | Ligand Info | |||||
| Structure Description | Crystal structure of the bromodomain of human BRD1 (BRPF2) in complex with OF-1 chemical probe | PDB:5FG6 | ||||
| Method | X-ray diffraction | Resolution | 1.10 Å | Mutation | No | [2] |
| PDB Sequence |
RLTPLTVLLR
572 SVLDQLQDKD582 PARIFAQPVS592 LKEVPDYLDH602 IKHPMDFATM612 RKRLEAQGYK 622 NLHEFEEDFD632 LIIDNCMKYN642 ARDTVFYRAA652 VRLRDQGGVV662 LRQARREVDS 672 IGLEEASG
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| Ligand Name: Cysteinesulfonic Acid | Ligand Info | |||||
| Structure Description | PWWP Domain of Human Bromodomain-Containing Protein 1 | PDB:3LYI | ||||
| Method | X-ray diffraction | Resolution | 2.10 Å | Mutation | No | [3] |
| PDB Sequence |
EPLKVVWAKC
937 SGYPSYPALI947 IDPKMPRVPG957 HHNGVTIPAP967 PLDVLKIGEH977 MQTKSDEKLF 987 LVLFFDNKRS997 WQWLPKSKMV1007 PLGIDETIDK1017 LKMMEGRNSS1027 IRKAVRIAFD 1037 RAMNHLSRVH1047
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| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| Different Human System Profiles of Target | Top |
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Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Tissue Distribution
of target is determined from a proteomics study that quantified more than 12,000 genes across 32 normal human tissues. Tissue Specificity (TS) score was used to define the enrichment of target across tissues.
The distribution of targets among different tissues or organs need to be taken into consideration when assessing the target druggability, as it is generally accepted that the wider the target distribution, the greater the concern over potential adverse effects
(Nat Rev Drug Discov, 20: 64-81, 2021).
Biological Network Descriptors
of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database.
The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information
(Front Pharmacol, 9, 1245, 2018;
Curr Opin Struct Biol. 44:134-142, 2017).
Human Similarity Proteins
Human Tissue Distribution
Biological Network Descriptors
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Note:
If a protein has TS (tissue specficity) scores at least in one tissue >= 2.5, this protein is called tissue-enriched (including tissue-enriched-but-not-specific and tissue-specific). In the plots, the vertical lines are at thresholds 2.5 and 4.
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| Degree | 5 | Degree centrality | 5.37E-04 | Betweenness centrality | 5.63E-06 |
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| Closeness centrality | 1.94E-01 | Radiality | 1.33E+01 | Clustering coefficient | 3.00E-01 |
| Neighborhood connectivity | 1.32E+01 | Topological coefficient | 2.95E-01 | Eccentricity | 12 |
| Download | Click to Download the Full PPI Network of This Target | ||||
| Chemical Structure based Activity Landscape of Target | Top |
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| Target Poor or Non Binders | Top | |||||
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| Target Poor or Non Binders | ||||||
| Target Regulators | Top | |||||
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| Target-interacting Proteins | ||||||
| References | Top | |||||
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| REF 1 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2724). | |||||
| REF 2 | Crystal structure of the bromodomain of human BRD1 (BRPF2) in complex with OF-1 chemical probe | |||||
| REF 3 | Structural and histone binding ability characterizations of human PWWP domains. PLoS One. 2011;6(6):e18919. | |||||
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