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First-in-human Study of AZD5153, A Small-molecule Inhibitor of Bromodomain Protein 4, in Patients with Relapsed/Refractory Malignant Solid Tumors and Lymphoma.
Hamilton EP, Wang JS, Oza AM, Patel MR, Ulahannan SV, Bauer T, Karlix JL, Zeron-Medina J, Fabbri G, Marco-Casanova P, Moorthy G, Hattersley MM, Littlewood GM, Mitchell P, Saeh J, Pouliot GP, Moore KN. Hamilton EP, et al. Mol Cancer Ther. 2023 Oct 2;22(10):1154-1165. doi: 10.1158/1535-7163.MCT-23-0065. Mol Cancer Ther. 2023. PMID: 37486983 Free PMC article. Clinical Trial.
AZD5153, a reversible, bivalent inhibitor of the bromodomain and extraterminal family protein BRD4, has preclinical activity in multiple tumors. ...One patient with metastatic pancreatic cancer receiving combination treatment had a partial response lasting 4.2 month …
AZD5153, a reversible, bivalent inhibitor of the bromodomain and extraterminal family protein BRD4, has preclinical activity in multi …
BRD4 inhibition impairs DNA mismatch repair, induces mismatch repair mutation signatures and creates therapeutic vulnerability to immune checkpoint blockade in MMR-proficient tumors.
Fu Y, Yang B, Cui Y, Hu X, Li X, Lu F, Qin T, Zhang L, Hu Z, Guo E, Fan J, Xiao R, Li W, Qin X, Hu D, Peng W, Liu J, Wang B, Mills GB, Chen G, Sun C. Fu Y, et al. J Immunother Cancer. 2023 Apr;11(4):e006070. doi: 10.1136/jitc-2022-006070. J Immunother Cancer. 2023. PMID: 37072347 Free PMC article.
Here, we identify that BRD4 inhibition induces a persistent dMMR phenotype in cancers. METHODS: We confirmed the correlation between BRD4 and mismatch repair (MMR) by the bioinformatic analysis on The Cancer Genome Atlas and Clinical Proteomic Tumor Analysis Consort …
Here, we identify that BRD4 inhibition induces a persistent dMMR phenotype in cancers. METHODS: We confirmed the correlation between …
Synergistic effect of PARP inhibitor and BRD4 inhibitor in multiple models of ovarian cancer.
Huang Y, Liu C, You L, Li X, Chen G, Fan J. Huang Y, et al. J Cell Mol Med. 2023 Mar;27(5):634-649. doi: 10.1111/jcmm.17683. Epub 2023 Feb 8. J Cell Mol Med. 2023. PMID: 36753396 Free PMC article.
Ovarian cancer has the highest facility rate among gynaecological tumours. ...In this study, we used the following multiple ovarian cancer models PDX, PDO and 3D/2D cell lines to elucidate the co-effect of AZD5153 and olaparib in vivo and in vitro. ...
Ovarian cancer has the highest facility rate among gynaecological tumours. ...In this study, we used the following multiple ovarian …
Evaluation of the Synergistic Potential of Simultaneous Pan- or Isoform-Specific BET and SYK Inhibition in B-Cell Lymphoma: An In Vitro Approach.
Sender S, Sultan AW, Palmer D, Koczan D, Sekora A, Beck J, Schuetz E, Taher L, Brenig B, Fuellen G, Junghanss C, Murua Escobar H. Sender S, et al. Cancers (Basel). 2022 Sep 27;14(19):4691. doi: 10.3390/cancers14194691. Cancers (Basel). 2022. PMID: 36230614 Free PMC article.
We evaluated the anti-lymphoma activity of the isoform-specific bivalent BET inhibitor AZD5153 (AZD) and the pan-BET inhibitor I-BET151 (I-BET) as single agents and in combination with SYK inhibitor Entospletinib (Ento) in vitro. ...
We evaluated the anti-lymphoma activity of the isoform-specific bivalent BET inhibitor AZD5153 (AZD) and the pan-BET inhibitor I-BET1 …
MUS81 Inhibition Enhances the Anticancer Efficacy of Talazoparib by Impairing ATR/CHK1 Signaling Pathway in Gastric Cancer.
Wang T, Zhang P, Li C, Liu W, Shen Q, Yang L, Xie G, Bai J, Li R, Tao K, Yin Y. Wang T, et al. Front Oncol. 2022 Apr 11;12:844135. doi: 10.3389/fonc.2022.844135. eCollection 2022. Front Oncol. 2022. PMID: 35480096 Free PMC article.
Therefore, in this study, the Cancer Genome Atlas (TCGA) data were analyzed and showed that MUS81 is a key regulator of cell cycle distribution and DNA damage repair in gastric cancer. ...Moreover, addition of the bromodomain-containing protein 4 inhibitor AZD515 …
Therefore, in this study, the Cancer Genome Atlas (TCGA) data were analyzed and showed that MUS81 is a key regulator of cell cycle di …
AZD5153, a Bivalent BRD4 Inhibitor, Suppresses Hepatocarcinogenesis by Altering BRD4 Chromosomal Landscape and Modulating the Transcriptome of HCC Cells.
Lin CH, Kuo JC, Li D, Koenig AB, Pan A, Yan P, Bai XF, Lee RJ, Ghoshal K. Lin CH, et al. Front Cell Dev Biol. 2022 Mar 24;10:853652. doi: 10.3389/fcell.2022.853652. eCollection 2022. Front Cell Dev Biol. 2022. PMID: 35399501 Free PMC article.
BRD4, a chromatin modifier frequently upregulated in a variety of neoplasms including hepatocellular cancer (HCC), promotes cancer cell growth by activating oncogenes through its interaction with acetylated histone tails of nucleosomes. ...AZD5153 trea …
BRD4, a chromatin modifier frequently upregulated in a variety of neoplasms including hepatocellular cancer (HCC), promotes …
AZD5153 reverses palbociclib resistance in ovarian cancer by inhibiting cell cycle-related proteins and the MAPK/PI3K-AKT pathway.
Liu C, Huang Y, Qin T, You L, Lu F, Hu D, Xiao R, Qin X, Guo E, Yang B, Li X, Fan J, Li X, Fu Y, Liu S, Wang Z, Dou Y, Wang W, Li W, Yang X, Liu J, Peng W, Zhang L, Cui Y, Sun C, Chen G. Liu C, et al. Cancer Lett. 2022 Mar 1;528:31-44. doi: 10.1016/j.canlet.2021.12.021. Epub 2021 Dec 20. Cancer Lett. 2022. PMID: 34942306
The CDK4/6 inhibitor, palbociclib has recently entered clinic-trial stage for breast cancer treatment. However, translating its efficacy to other solid tumors has been challenging, especially for aggressive solid tumors. ...In preclinical models, this study demonstrated th …
The CDK4/6 inhibitor, palbociclib has recently entered clinic-trial stage for breast cancer treatment. However, translating its effic …
Bromodomain 4 inhibition leads to MYCN downregulation in Wilms tumor.
Woods AD, Berlow NE, Ortiz MV, Dela Cruz F, Siddiquee A, Coutinho DF, Purohit R, Freier KET, Michalek JE, Lathara M, Matlock K, Srivivasa G, Royer-Pokora B, Veselska R, Kung AL, Keller C. Woods AD, et al. Pediatr Blood Cancer. 2022 Feb;69(2):e29401. doi: 10.1002/pbc.29401. Epub 2021 Oct 24. Pediatr Blood Cancer. 2022. PMID: 34693628 Free PMC article.
BACKGROUND: Wilms tumor is the most common childhood kidney cancer. Two distinct histological subtypes of Wilms tumor have been described: tumors lacking anaplasia (the favorable subtype) and tumors displaying anaplastic features (the unfavorable subtype). ...MYCN dysregul …
BACKGROUND: Wilms tumor is the most common childhood kidney cancer. Two distinct histological subtypes of Wilms tumor have been descr …
Combining inhibitors of Brd4 and cyclin-dependent kinase can decrease tumor growth in neuroblastoma with MYCN amplification.
Wood L, Huang M, Zeki J, Gong M, Taylor J, Shimada H, Chiu B. Wood L, et al. J Pediatr Surg. 2021 Jul;56(7):1199-1202. doi: 10.1016/j.jpedsurg.2021.03.037. Epub 2021 Mar 26. J Pediatr Surg. 2021. PMID: 33838899 Free PMC article.
Several genes were potential Bromodomain-containing protein 4 (Brd4) targets, making Brd4 inhibitors - JQ1, AZD5153 - and cyclin-dependent kinase (Brd4's binding partner) inhibitors - dinaciclib - potential therapeutic agents. JQ1 and dinaciclib were synergistic in inducin …
Several genes were potential Bromodomain-containing protein 4 (Brd4) targets, making Brd4 inhibitors - JQ1, AZD5153 - and cyclin-depe …
29 results