GNE-064: A Potent, Selective, and Orally Bioavailable Chemical Probe for the Bromodomains of SMARCA2 and SMARCA4 and the Fifth Bromodomain of PBRM1.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c00662
Abstract: Bromodomains are acetyllysine recognition domains present in a variety of human proteins. Bromodomains also bind small molecules that compete with acetyllysine, and therefore bromodomains have been targets for drug discovery efforts. Highly potent and selective… read more here.
Keywords: bromodomains smarca2; smarca4; gne 064; pbrm1 ... See more keywords
Selective and Cell-Active PBRM1 Bromodomain Inhibitors Discovered through NMR Fragment Screening.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c00864
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… read more here.
Keywords: pbrm1 bromodomain; cell active; selective cell; pbrm1 ... See more keywords
Immune microenvironment in clear cell type renal cell carcinoma with loss of PBRM1 protein expression
Sign Up to like & getrecommendations! Published in 2019 at "Annals of Oncology"
DOI: 10.1093/annonc/mdz338.016
Abstract: Abstract Background Polybromo-1 (PBRM1) is a chromatin-modifying gene and its mutation is detected in approximately 40% of clear cell type renal cell carcinoma (ccRCC). It has been recently reported that PBRM1 mutation was positively associated… read more here.
Keywords: protein expression; pbrm1 protein; pbrm1; cell ... See more keywords
A cytoskeletal function for PBRM1 reading methylated microtubules
Sign Up to like & getrecommendations! Published in 2021 at "Science Advances"
DOI: 10.1126/sciadv.abf2866
Abstract: Methyl marks made by the epigenetic writer SETD2 recruit the epigenetic reader PBRM1 to spindle microtubules during mitosis. Epigenetic effectors “read” marks “written” on chromatin to regulate function and fidelity of the genome. Here, we… read more here.
Keywords: pbrm1; methyl marks; chromatin; reading ... See more keywords
A Pan-Cancer Analysis of the Role of PBRM1 in Human Tumors
Sign Up to like & getrecommendations! Published in 2022 at "Stem Cells International"
DOI: 10.1155/2022/7676541
Abstract: To understand common but distinctive systems to drive oncogenic stages in human tumors is critical for understanding disease programme and developing novel therapeutic strategies. PBRM1 is a critical gene in oncogenesis. We found that PBRM1… read more here.
Keywords: hnsc kirc; human tumors; pan cancer; analysis ... See more keywords
PBRM1 Deficiency Confers Synthetic Lethality to DNA Repair Inhibitors in Cancer
Sign Up to like & getrecommendations! Published in 2021 at "Cancer Research"
DOI: 10.1158/0008-5472.can-21-0628
Abstract: This study demonstrates that PARP and ATR inhibitors are synthetic lethal with the loss of PBRM1, a PBAF-specific subunit, thus providing the rationale for assessing these inhibitors in patients with PBRM1-defective cancer. Inactivation of Polybromo… read more here.
Keywords: pbrm1; parp atr; pbrm1 defective; cancer ... See more keywords
Abstract 1058: Targeting chromatin remodeling-associated genetic vulnerabilities in cancer: PBRM1 defects are synthetic lethal with PARP and ATR inhibitors
Sign Up to like & getrecommendations! Published in 2020 at "Cancer Research"
DOI: 10.1158/1538-7445.am2020-1058
Abstract: Aim: Polybromo-1 (PBRM1), a specific subunit of the pBAF chromatin remodeling complex, is frequently inactivated in cancer. For example, 40% of clear cell Renal Cell Carcinoma (ccRCC) and 15% of cholangiocarcinoma present deleterious PBRM1 mutations.… read more here.
Keywords: pbrm1; pbrm1 defects; cancer; cell ... See more keywords
Abstract 6147: MCL1 inhibitor PRT1419 demonstrates anti-tumor activity in PBRM1-altered clear cell renal cancer and synergizes with standard of care agents
Sign Up to like & getrecommendations! Published in 2023 at "Cancer Research"
DOI: 10.1158/1538-7445.am2023-6147
Abstract: Induced myeloid leukemia cell differentiation protein (MCL1) is a member of the B-cell lymphoma-2 (BCL2) family of apoptosis regulators, which plays a critical role in maintaining cellular homeostasis and promoting cancer cell survival. Increased expression… read more here.
Keywords: cell; mcl1; pbrm1; prt1419 ... See more keywords
BAP1 and PBRM1 in metastatic clear cell renal cell carcinoma: tumor heterogeneity and concordance with paired primary tumor
Sign Up to like & getrecommendations! Published in 2017 at "BMC Urology"
DOI: 10.1186/s12894-017-0209-3
Abstract: BackgroundBAP1 and PBRM1 are frequently mutated in primary clear cell renal cell carcinoma (ccRCC) tumors; however, the frequency and clinical relevance of these mutations in metastatic ccRCC tumors is unknown. Additionally, while intra-tumor heterogeneity has… read more here.
Keywords: pbrm1; expression; bap1 pbrm1; cell ... See more keywords