Lanyon-Hogg, Thomas; Ritzefeld, Markus; Zhang, Leran; Andrei, Sebastian A.; Pogranyi, Balazs; Mondal, Milon; Sefer, Lea; Johnston, Callum D.; Coupland, Claire E.; Greenfield, Jake L.; Newington, Joshua; Fuchter, Matthew J.; Magee, Anthony I.; Siebold, Christian; Tate, Edward W. published an article in 2021. The article was titled 《Photochemical Probe Identification of a Small-Molecule Inhibitor Binding Site in Hedgehog Acyltransferase (HHAT)》, and you may find the article in Angewandte Chemie, International Edition.Synthetic Route of C9H9BrO2 The information in the text is summarized as follows:
The mammalian membrane-bound O-acyltransferase (MBOAT) superfamily is involved in biol. processes including growth, development and appetite sensing. MBOATs are attractive drug targets in cancer and obesity; however, information on the binding site and mol. mechanisms underlying small-mol. inhibition is elusive. This study reports rational development of a photochem. probe to interrogate a novel small-mol. inhibitor binding site in the human MBOAT Hedgehog acyltransferase (HHAT). Structure-activity relationship investigation identified single enantiomer IMP-1575, the most potent HHAT inhibitor reported to-date, and guided design of photocrosslinking probes that maintained HHAT-inhibitory potency. Photocrosslinking and proteomic sequencing of HHAT delivered identification of the first small-mol. binding site in a mammalian MBOAT. Topol. and homol. data suggested a potential mechanism for HHAT inhibition which was confirmed by kinetic anal. Our results provide an optimal HHAT tool inhibitor IMP-1575 (Ki=38 nM) and a strategy for mapping small mol. interaction sites in MBOATs.Benzyl 2-bromoacetate(cas: 5437-45-6Synthetic Route of C9H9BrO2) was used in this study.
Benzyl 2-bromoacetate(cas: 5437-45-6) belongs to benzyl acetate. Benzyl acetate is an aromatic chemical, usually appearing as a clear liquid with a moderate sweet-jasmine fragrance. This compound appears as a component of some of our fragrance blends.Synthetic Route of C9H9BrO2
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary