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Crystal Structure of the first bromodomain of human BRD4 in complex with a 5-methyl-triazolopyrimidine ligand

Functional Information from PDB Data
site_idAC1
Number of Residues7
DetailsBINDING SITE FOR RESIDUE EDO A 201
ChainResidue
AILE100
AILE101
ALYS102
ATHR103
AASN135
AHOH481
AHOH482

site_idAC2
Number of Residues10
DetailsBINDING SITE FOR RESIDUE 25K A 202
ChainResidue
APHE83
ALEU92
ALEU94
ALYS99
AASN140
AILE146
AMET149
AHOH316
ATRP81
APRO82

Functional Information from PROSITE/UniProt
site_idPS00633
Number of Residues60
DetailsBROMODOMAIN_1 Bromodomain signature. AwpFqqpvDavklnlpDYYkiIktpMdmgtIkkrlenny..Ywnaqeciqdfnt.MftNCyiY
ChainResidueDetails
AALA80-TYR139

Functional Information from SwissProt/UniProt
site_idSWS_FT_FI1
Number of Residues106
DetailsDomain: {"description":"Bromo 1","evidences":[{"source":"PROSITE-ProRule","id":"PRU00035","evidenceCode":"ECO:0000255"}]}
ChainResidueDetails

site_idSWS_FT_FI2
Number of Residues1
DetailsSite: {"description":"Acetylated histone binding","evidences":[{"source":"PubMed","id":"22464331","evidenceCode":"ECO:0000269"}]}
ChainResidueDetails

site_idSWS_FT_FI3
Number of Residues2
DetailsCross-link: {"description":"Glycyl lysine isopeptide (Lys-Gly) (interchain with G-Cter in SUMO2)","evidences":[{"source":"PubMed","id":"28112733","evidenceCode":"ECO:0007744"}]}
ChainResidueDetails

246905

PDB entries from 2025-12-31

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