Vantourout, Julien C.; Mason, Andrew M.; Yuen, Josephine; Simpson, Graham L.; Evindar, Ghotas; Kuai, Letian; Hobbs, Michael; Edgar, Emma; Needle, Saul; Bai, Xiaopeng; Wilson, Steve; Scott-Stevens, Paul; Traylen, William; Lambert, Kim; Young, Neil; Bunally, Shenaz; Summerfield, Scott G.; Snell, Richard; Lad, Rakesh; Shi, Eric; Skinner, Steven; Shewchuk, Lisa; Watson, Allan J. B.; Chung, Chun-wa; Pal, Sandeep; Holt, Dennis A.; Kallander, Lara S.; Prendergast, Joanne; Rivera, Katrina; Washburn, David G.; Harpel, Mark R.; Arico-Muendel, Christopher; Isidro-Llobet, Albert published their research in Bioconjugate Chemistry in 2021. The article was titled 《In Vivo Half-Life Extension of BMP1/TLL Metalloproteinase Inhibitors Using Small-Molecule Human Serum Albumin Binders》.Quality Control of Benzyl 2-bromoacetate The article contains the following contents:
Reducing the required frequence of drug dosing can improve the adherence of patients to chronic treatments. Hence, drugs with longer in vivo half-lives are highly desirable. One of the most promising approaches to extend the in vivo half-life of drugs is conjugation to human serum albumin (HSA). In this work, we describe the use of AlbuBinder 1, a small-mol. noncovalent HSA binder, to extend the in vivo half-life and pharmacol. of small-mol. BMP1/TLL inhibitors in humanized mice (HSA KI/KI). A series of conjugates of AlbuBinder 1 with BMP1/TLL inhibitors were prepared In particular, conjugate c showed good solubility and a half-life extension of >20-fold vs. the parent mol. in the HSA KI/KI mice, reaching half-lives of >48 h with maintained maximal inhibition of plasma BMP1/TLL. The same conjugate showed a half-life of only 3 h in the wild-type mice, suggesting that the half-life extension was principally due to specific interactions with HSA. It is envisioned that conjugation to AlbuBinder 1 should be applicable to a wide range of small mol. or peptide drugs with short half-lives. In this context, AlbuBinders represent a viable alternative to existing half-life extension technologies. The results came from multiple reactions, including the reaction of Benzyl 2-bromoacetate(cas: 5437-45-6Quality Control of Benzyl 2-bromoacetate)
Benzyl 2-bromoacetate(cas: 5437-45-6) belongs to benzyl acetate. Benzyl acetate is a synthetic chemical produced for industry from benzyl alcohol and acetic acid, but is also naturally present in the essential oils of many plants, including jasmine and ylang ylang.Quality Control of Benzyl 2-bromoacetate
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary