ArticleJournal of medicinal chemistry2022
Selective and Cell-Active PBRM1 Bromodomain Inhibitors Discovered through NMR Fragment Screening.
Article in Journal of medicinal chemistry, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 20 citations in OpenAlex.
- Chemical inhibition of INO1 reduces phytic acid in rice and wheat grains for enhanced micronutrient bioavailability.Nature food · 2026Article
- Structural Genomics Defines PBRM1 Bromodomain Variant Function in ccRCC.Human mutation · 2026Article
- Polybromo‑1 Bromodomain Inhibitor Selectivity Is Mediated by a Unique Ligand-Binding Pocket.ACS medicinal chemistry letters · 2025Article
- Discovery of Pyrimidoindolones as Novel Family VIII Bromodomain Binders.ACS medicinal chemistry letters · 2025Article
- Affinity Ultrafiltration Mass Spectrometry for Screening Active Ingredients in Traditional Chinese Medicine: A Review of the Past Decade (2014-2024).Molecules (Basel, Switzerland) · 2025Review
- The TRIM33 Bromodomain Recognizes Histone Lysine Lactylation.ACS chemical biology · 2024Article
- Chromatin accessibility: biological functions, molecular mechanisms and therapeutic application.Signal transduction and targeted therapy · 2024Review
- Epigenetics-targeted drugs: current paradigms and future challenges.Signal transduction and targeted therapy · 2024Review
- Chromatin remodellers as therapeutic targets.Nature reviews. Drug discovery · 2024Review
- Context-specific functions of chromatin remodellers in development and disease.Nature reviews. Genetics · 2024Review
- Cancer-associated polybromo-1 bromodomain 4 missense variants variably impact bromodomain ligand binding and cell growth suppression.The Journal of biological chemistry · 2024Article
- Targeting SWI/SNF Complexes in Cancer: Pharmacological Approaches and Implications.Epigenomes · 2024Review
- Rational Design and Development of Selective BRD7 Bromodomain Inhibitors and Their Activity in Prostate Cancer.Journal of medicinal chemistry · 2023Article
- Fragment-based drug discovery of small molecule ligands for the human chemokine CCL28.SLAS discovery : advancing life sciences R & D · 2023Article
- Fragment-based screening by protein-detected NMR spectroscopy.Methods in enzymology · 2023Article
Corrections and comments
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Authors and funding
15 authors at 2 institutions in 1 country.
Funding
Abstract
PBRM1 is a subunit of the PBAF chromatin remodeling complex that uniquely contains six bromodomains. PBRM1 can operate as a tumor suppressor or tumor promoter. PBRM1 is a tumor promoter in prostate cancer, contributing to migratory and immunosuppressive phenotypes. Selective chemical probes targeting PBRM1 bromodomains are desired to elucidate the association between aberrant PBRM1 chromatin binding and cancer pathogenesis and the contributions of PBRM1 to immunotherapy. Previous PBRM1 inhibitors unselectively bind SMARCA2 and SMARCA4 bromodomains with nanomolar potency. We used our protein-detected NMR screening pipeline to screen 1968 fragments against the second PBRM1 bromodomain, identifying 17 hits with
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.