Covalent-fragment screening of BRD4 identifies a ligandable site orthogonal to the acetyl-lysine binding sites.
Sign Up to like & getrecommendations! Published in 2020 at "ACS chemical biology"
DOI: 10.1021/acschembio.0c00058
Abstract: BRD4, a member of the bromodomain and extraterminal domain (BET) family, has emerged as a promising epigenetic target in cancer and inflammatory disorders. All reported BET family ligands bind within the bromodomain acetyl-lysine binding sites… read more here.
Keywords: acetyl lysine; site; brd4; binding sites ... See more keywords
High resolution structure of human apolipoprotein (a) kringle IV type 2: beyond the lysine binding site
Sign Up to like & getrecommendations! Published in 2020 at "Journal of Lipid Research"
DOI: 10.1194/jlr.ra120001023
Abstract: Lipoprotein (a) [Lp(a)] is characterized by an LDL-like composition in terms of lipids and apoB100, and by one copy of a unique glycoprotein, apo(a). The apo(a) structure is mainly based on the repetition of tandem… read more here.
Keywords: high resolution; kringle type; binding site; structure ... See more keywords
Inactivation of the lysine binding sites of human plasminogen (hPg) reveals novel structural requirements for the tight hPg conformation, M-protein binding, and rapid activation
Sign Up to like & getrecommendations! Published in 2023 at "Frontiers in Molecular Biosciences"
DOI: 10.3389/fmolb.2023.1166155
Abstract: Accelerated activation of the human plasminogen zymogen (hPg) to two-chain active plasmin (hPm) is achieved following conformational changes induced by ligand-binding at the lysine-binding sites (LBSs) in four of the five hPg kringle domains. In… read more here.
Keywords: lysine binding; hpg; human plasminogen; inactivation ... See more keywords