Hu, Rong; Wang, Wan-Li; Yang, Ying-Yue; Hu, Xia-Tong; Wang, Qi-Wei; Zuo, Wei-Qiong; Xu, Ying; Feng, Qiang; Wang, Ning-Yu published an article in 2022. The article was titled 《Identification of a selective BRD4 PROTAC with potent antiproliferative effects in AR-positive prostate cancer based on a dual BET/PLK1 inhibitor》, and you may find the article in European Journal of Medicinal Chemistry.Electric Literature of C4H7BrO2 The information in the text is summarized as follows:
BRD4-targeted proteolysis targeting chimera (PROTAC) have exhibited promising in vitro and in vivo anticancer activity in a number of cancer models. However, the clin. development of current reported BRD4-PROTACs have stagnated, largely due to the safety risks caused by their poor degradation selectivity. In this study, we designed and synthesized a series of PROTACs based on our recently reported dual BET/PLK1 inhibitor WNY0824, which led to the discovery of an isoform-selective and potent BRD4-PROTAC 12a (WWL0245). WWL0245 exhibited excellent selective cytotoxicity in the BETi sensitive cancer cell lines, including AR-pos. prostate cancer cell lines. It could also efficiently induce ubiquitin-proteasomal degradation of BRD4 in AR-pos. prostate cancer cell lines, with sub-nanomolar half-maximal degrading concentration (DC50) and maximum degradation (Dmax) > 99%. Moreover, WWL0245 induced cell cycle arrest at the G0/G1 phase and apoptosis in AR-pos. prostate cancer by downregulation of the protein levels of AR, PSA and c-Myc as well as transcriptionally suppressed AR-regulated genes. WWL0245 was thus expected to be developed as a promising drug candidate for AR-pos. prostate cancer and a valuable tool compound to study the biol. function of BRD4. In addition to this study using 4-Bromobutanoic acid, there are many other studies that have used 4-Bromobutanoic acid(cas: 2623-87-2Electric Literature of C4H7BrO2) was used in this study.
4-Bromobutanoic acid(cas: 2623-87-2) belongs to carboxylic acids. The chief chemical characteristic of the carboxylic acids is their acidity. They are generally more acidic than other organic compounds containing hydroxyl groups but are generally weaker than the familiar mineral acids (e.g., hydrochloric acid, HCl, sulfuric acid, H2SO4, etc.).Electric Literature of C4H7BrO2
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary