Compounds > 2-4-Di(3-pyridyl)-1-3-thiazole

2-4-Di(3-pyridyl)-1-3-thiazole and Prostatic-Neoplasms

2-4-Di(3-pyridyl)-1-3-thiazole has been researched along with Prostatic-Neoplasms* in 1 studies

Other Studies

1 other study(ies) available for 2-4-Di(3-pyridyl)-1-3-thiazole and Prostatic-Neoplasms

Article	Year
Selective and Cell-Active PBRM1 Bromodomain Inhibitors Discovered through NMR Fragment Screening. Journal of medicinal chemistry, 2022, 10-27, Volume: 65, Issue:20 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 Topics: Carcinogens; Chromatin; DNA Helicases; DNA-Binding Proteins; Histones; Humans; Male; Nuclear Proteins; Prostatic Neoplasms; Protein Domains; Transcription Factors	2022

Article

Year

Selective and Cell-Active PBRM1 Bromodomain Inhibitors Discovered through NMR Fragment Screening.

Journal of medicinal chemistry, 2022, 10-27, Volume: 65, Issue:20

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

Topics: Carcinogens; Chromatin; DNA Helicases; DNA-Binding Proteins; Histones; Humans; Male; Nuclear Proteins; Prostatic Neoplasms; Protein Domains; Transcription Factors

2022