Results 171 to 180 of about 27,094 (219)
Discovery of molecular glues that bind FKBP12 and structurally distinct targets using DNA-encoded libraries. [PDF]
Nat CommunZandi TA +9 more
europepmc +1 more source
Perturbation of BRD4 and p300 activity suppresses super enhancer‑driven <i>KLF6</i> expression in renal carcinoma. [PDF]
Oncol RepZamberi NNM +5 more
europepmc +1 more source
Discovery of BAZ2A bromodomain ligands [PDF]
European Journal of Medicinal Chemistry, 2017 The bromodomain adjacent to zinc finger domain protein 2A (BAZ2A) is implicated in aggressive prostate cancer. The BAZ2A bromodomain is a challenging target because of the shallow pocket of its natural ligand, the acetylated side chain of lysine. Here, we report the successful screening of a library of nearly 1500 small molecules by high-throughput ...
Christoph Rademacher +2 more
exaly +9 more sources
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Current Opinion in Chemical Biology, 2022
Lysine acetylation creates docking sites for epigenetic reader domains of BET bromodomain proteins that have emerged as principal regulators of linage specific gene transcription. The development of potent and highly selective inhibitors, that have been soon widely available, enabled mechanistic studies in a diversity of disease models leading to a ...
Martin P. Schwalm, Stefan Knapp
openaire +2 more sources
Lysine acetylation creates docking sites for epigenetic reader domains of BET bromodomain proteins that have emerged as principal regulators of linage specific gene transcription. The development of potent and highly selective inhibitors, that have been soon widely available, enabled mechanistic studies in a diversity of disease models leading to a ...
Martin P. Schwalm, Stefan Knapp
openaire +2 more sources
Bromodomain inhibitors and therapeutic applications
Current Opinion in Chemical Biology, 2023The bromodomain acts to recognize acetylated lysine in histones and transcription proteins and plays a fundamental role in chromatin-based cellular processes including gene transcription and chromatin remodeling. Many bromodomain proteins, particularly the bromodomain and extra terminal domain (BET) protein BRD4 have been implicated in cancers and ...
Ming-Ming Zhou
exaly +3 more sources
Bromodomains and Their Pharmacological Inhibitors
ChemMedChem, 2014AbstractOver 60 bromodomains belonging to proteins with very different functions have been identified in humans. Several of them interact with acetylated lysine residues, leading to the recruitment and stabilization of protein complexes. The bromodomain and extra‐terminal domain (BET) proteins contain tandem bromodomains which bind to acetylated ...
Daniel, Gallenkamp +3 more
openaire +2 more sources
Bromodomain and extraterminal domain protein bromodomain inhibitor based cancer therapeutics
Current Opinion in Oncology, 2021Purpose of review Bromodomain and extraterminal domain (BET) proteins are evolutionarily conserved, multifunctional super-regulators that specifically recognize acetyl-lysine on histones and other proteins controlling gene transcription.
Tithi Ghosh, Halder +2 more
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Cancer and the bromodomains of BAF180
Biochemical Society Transactions, 2012Chromatin remodelling complexes alter the structure of chromatin and have central roles in all DNA-templated activities, including regulation of gene expression and DNA repair. Mutations in subunits of the PBAF (polybromo/Brg1-associated factor) or SWI/SNF-B remodelling complex, including BAF180, are frequently associated with cancer.
Brownlee, Peter M +3 more
openaire +3 more sources