8042-97-5Relevant articles and documents
Assessing and utilizing esterase specificity in antimicrobial prodrug development
Hetrick, Kenton J.,Raines, Ronald T.
, (2021/12/30)
As a class of enzymes, esterases have been investigated for decades and have found use in industrial processes, synthetic organic chemistry, and elsewhere. Esters are functional groups composed of an alcohol moiety and a carboxylic acid moiety. Although much work has explored the influence of the carboxyl moiety of an ester on its susceptibility to esterases, little work has explored the influence of the alcohol moiety. Here, we describe an in vitro methodology to explore the influence of changing the alcohol moiety of an ester on its enzymatic hydrolysis, including strategies for analyzing such data. We then describe leveraging data from these assays to develop targeted antimicrobial prodrugs that activate in certain species due to the discriminatory activity of species-specific esterases. We envisage the potential of genomics and machine learning to further these efforts. Finally, we anticipate the potential future uses of these ideas, including developing targeted anti-cancer compounds.
Oxygen Vacancy-Engineered PEGylated MoO3 ?x Nanoparticles with Superior Sulfite Oxidase Mimetic Activity for Vitamin B1 Detection
Chen, Yuan,Chen, Tongming,Wu, Xiaoju,Yang, Guowei
, (2019/11/03)
Sulfite oxidase (SuOx) is a molybdenum-dependent enzyme that catalyzes the oxidation of sulfite to sulfate to maintain the intracellular levels of sulfite at an appropriate low level. The deficiency of SuOx would cause severe neurological damage and infant diseases, which makes SuOx of tremendous biomedical importance. Herein, a SuOx mimic nanozyme of PEGylated (polyethylene glycol)-MoO3 ?x nanoparticles (P-MoO3 ?x NPs) with abundant oxygen vacancies created by vacancy-engineering is reported. Their level of SuOx-like activity is 12 times higher than that of bulk-MoO3. It is also established that the superior increased enzyme mimetic activity is due to the introduction of the oxygen vacancies acting as catalytic hotspots, which allows better sulfite capture ability. It is found that vitamin B1 (VB1) inhibits the SuOx mimic activity of P-MoO3 ?x NPs through the irreversible cleavage by sulfite and the electrostatic interaction with P-MoO3 ?x NPs. A colorimetric platform is developed for the detection of VB1 with high sensitivity (the low detection limit is 0.46 μg mL?1) and good selectivity. These findings pave the way for further investigating the nanozyme which possess intrinsic SuOx mimicing activity and is thus a promising candidate for biomedical detection.
Biosynthesis of a thiamin antivitamin in clostridium botulinum
Cooper, Lisa E.,O'Leary, Seán E.,Begley, Tadhg P.
, p. 2215 - 2217 (2014/05/06)
Bacimethrin-derived 2′-methoxythiamin pyrophosphate inhibits microbial growth by disrupting metabolic pathways dependent on thiamin-utilizing enzymes. This study describes the discovery of the bacimethrin biosynthetic gene cluster of Clostridium botulinum A ATCC 19397 and in vitro reconstitution of bacimethrin biosynthesis from cytidine 5′-monophosphate.