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Carboxylesterase Inhibitors: Relevance for Pharmaceutical Applications
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2019
Trifluoroketones are potent inhibitors of a variety of hydrolases, such as juvenile hormone esterase (Prestwich et al., 1984), AchE (Gelb et al., 2002; Wadkins et al., 2007), chymotrypsin (Brady and Abeles, 1990), angiotensin converting enzyme (Ojima et al., 1994) and fatty acid amidohydrolase (Boger et al., 1999). Trifluoroketones also displayed strong inhibitory effects on human CES with Ki values at nanomolar level, and mostly demonstrated poor specificity toward CES1 or CES2 (Table 9.4) (Wadkins et al., 2007). The trifluoro moiety of these compounds could be easily hydrated to form the gem-diol (Gelb et al., 2002; Wadkins et al., 2007). However, the equilibrium between the ketone and gem-diol forms must be sufficiently dynamic such that adequate concentrations of the ketone are available for enzyme inhibition (Rosell et al., 1996). Thus the rates of the ketone/gem-diol equilibrium would affect the interactions between trifluoroketones and the amino acid residues within the CES active site, and thus affect their inhibition potency. However, this process was poorly understood and would require further investigation to explore the mechanism of trifluoroketones as CES inhibitors. In most cases, thioether-containing compounds were more potent inhibitors than sulfinyl or sulfonyl analogs, and these compounds containing longer, more hydrophobic alkyl chains were more potent inhibitors of CES (Table 9.4).
Comparative transcriptome analysis reveals the impact of the daily rhythm on the hemolymph of the Chinese mitten crab (Eriocheir sinensis)
Published in Chronobiology International, 2022
Changyue Yu, Baoli Zhang, Zhiyuan Zhang, Simiao Wang, Tingyu Wei, Lisong Li, Yingying Zhao, Hua Wei, Yingdong Li
A total of 3,659 DEGs were identified between the 06:00 and 18:00 h groups; of these, 1,521 were upregulated and 2,138 were downregulated. The upregulated DEGs at 18:00 h were associated with the molting process, such as the expression of genes encoding cryptocyanin, juvenile hormone esterase, JHE-like carboxylesterase, and chitin deacetylase (Table S3). The downregulated DEGs at 18:00 h were associated with immune processes, such as genes encoding crustin, dicer, and cytochrome c oxidase (Table S4). The results demonstrate the effect of the daily rhythm on molt and immunity in E. sinensis.