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Corning® Supersomes? Human UDP-glucuronosyltransferases Portfolio

Corning® Supersomes? Human UDP-glucuronosyltransferases Portfolio
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Corning® Supersomes? Human UDP-glucuronosyltransferases Portfolio - 1

Corning® Supersomes™ Human UDP-glucuronosyltransferases Portfolio UDP-glucuronosyltransferases (UGTs) belong to a membranebound superfamily of Phase II enzymes which conjugate glucuronic acid to substrates to make them more water soluble. UGTs are expressed in many mammalian tissues, with highest expression level in liver and intestine. UGTs are the most important Phase II drug metabolizing enzymes in humans, as well as being the major contributor to “non-CYP” drug elimination pathways. Corning has expanded its portfolio to include human UGT2B10; abundant in liver, and important for the glucuronidation of several tricyclic antidepressant drugs such as amitriptyline. Features w Facilitates efficient metabolite formation with long linear time course; ideal for slow metabolizing drug compounds w Ensures glucuronidation activity of recombinant enzymes is similar to UGTs expressed in human liver and other organs w Delivers high catalytic activity; ideal for high-throughput screening assays w Supports essential assays such as reaction phenotyping w Provides researchers with the most comprehensive set of UGT enzyme products available w Manufactured using baculovirus/insect cell expression system w Newly added UGT2B10, like Corning’s long standing product UGT1A4, contributes to quaternary N-glucuronidation of xenobiotics such as tricyclic antidepressants and nicotine High Enzymatic Activity Corning Supersomes are engineered to provide efficient metabolite production with long linear metabolite formation times of 60 minutes or greater, making the products highly suited to identifying metabolites for slowly metabolized compounds (shown in Figure 1). Engineered for Native Activity Corning Supersomes UGT cDNA matches the published sequence from the US National Library of Medicine native DNA sequence. Corning’s UGTs behave like native UGTs expressed in human liver and other organs as demonstrated by measured glucuronidation activity where the Km of recombinant UGTs are similar to those of human liver microsomes (HLMs) (shown in Table 1). Extensive Portfolio of Phase I and Phase II Recombinant Enzymes Corning Supersomes are recognized worldwide as the “industry gold standard”, with the most extensive portfolio of CYPs, UGTs, FMOs, MAOs, NATs, and CESs.

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Corning® Supersomes? Human UDP-glucuronosyltransferases Portfolio - 2

Time Course of Product Formation 70 Michaelis-Menten Kinetic Parameters Km (µM) Corning® Supersomes™ Figure 1. The time course of product formation for UGT1A1, UGT1A4, UGT2B17 was shown to be linear out to 60 minutes. Estradiol, Trifluoperazine, and Eugenol were used as the substrate of UGT1A1, UGT1A4, and UGT2B17, respectively. HLM: Human Liver Microsomes Table 1. Michaelis-Menten kinetic parameters of UGTs compared to HLM. Km values obtained using recombinant UGTs were found to be similar to those obtained using HLM (Pooled). HLM is Corning UltraPool™ HLM 150; Cat. No. 452117. Corning...

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