Molecular Glue Degraders Redefining Targeted Therapies From Discovery to Therapeutic Applications
MedComm – Oncology, Volume 5, Issue 1, March 2026.Molecular glue degraders (MGDs) constitute an emerging class of therapeutic agents poised to revolutionize the paradigm of targeted drug discovery. By reprogramming E3 ubiquitin ligases to degrade proteins of interest (POI) via a transient formation of a ternary complex mediated by protein–protein interactions, MGDs surpass the intrinsic limitations of
Jinfeng Wen +3 more
wiley +1 more source
A Novel BD2-Selective Inhibitor of BRDs Mitigates ROS Production and OA Pathogenesis
AntioxidantsBromodomain and extra-terminal domain (BET) family proteins regulate transcription and recognize lysine residues in histones. Selective BET inhibitors targeting one domain have attracted attention because they maintain normal physiological activities ...
Hyemi Lee +6 more
doaj +1 more source
A chalcone derivative reactivates latent HIV-1 transcription through activating P-TEFb and promoting Tat-SEC interaction on viral promoter. [PDF]
, 2017 The principal barrier to the eradication of HIV/AIDS is the existence of latent viral reservoirs. One strategy to overcome this barrier is to use latency-reversing agents (LRAs) to reactivate the latent proviruses, which can then be eliminated by ...
Ao, Ming-Tao +9 more
core +2 more sources
Breaking barriers: transitioning from X‐ray crystallography to cryo‐EM for structural studies
Acta Crystallographica Section D, Volume 82, Issue 3, Page 253-273, March 2026.This article describes the transition of the Glass laboratory from X‐ray crystallography to single‐particle cryo‐electron microscopy (cryo‐EM) for structural studies of ATAD2B, a large AAA+ ATPase‐ and bromodomain‐containing protein involved in chromatin regulation.
Hassan Zafar +4 more
wiley +1 more source
Selective BET bromodomain inhibition as an antifungal therapeutic strategy
Nature Communications, 2017 BET proteins bind chromatin through their bromodomains (BDs) to regulate transcription and chromatin remodelling. Here, the authors show that the BET protein Bdf1 is essential for the fungal pathogenCandida albicans, and report compounds that inhibit the
Flore Mietton +17 more
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iScienceSummary: Combinatorial signaling by proinflammatory cytokines synergizes to exacerbate toxicity to cells and tissue injury during acute infections. To explore synergism at the gene-regulatory level, we investigated the dynamics of transcription and ...
Ronan C. Bracken +9 more
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Metabolic rewiring in MYC-driven medulloblastoma by BET-bromodomain inhibition. [PDF]
Sci Rep, 2023 Graziani V +5 more
europepmc +1 more source
The Development and Evaluation of a Novel Highly Selective PET Radiotracer for Targeting BET BD1
PharmaceuticalsBackground/Objectives: Small molecules that interfere with the interaction between acetylated protein tails and the tandem bromodomains of BET (bromodomain and extra-terminal) family proteins are pivotal in modulating immune/inflammatory and neoplastic ...
Yanli Wang +5 more
doaj +1 more source
Bromodomain inhibitors and cancer therapy: From structures to applications
Epigenetics, 2017 Aberrations in the epigenetic landscape are a hallmark of cancer. Alterations in enzymes that are “writers,” “erasers,” or “readers” of histone modification marks are common. Bromodomains are “readers” that bind acetylated lysines in histone tails. Their
Montserrat Pérez-Salvia, Manel Esteller
doaj +1 more source