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Non-CYP Enzymes

While Cytochrome P450 (CYP) enzymes are well-known and profiled for their role in metabolism of many small molecule drugs, other enzymes can play critical roles in a drug compound’s metabolism and overall disposition in a similar way. Here we offer resources which explore research involving drug interactions with non-CYP enzymes such as UGTs, SULTs, MAO-A, MAO-B, AO, XO, and others.

 

Scientific Posters

An assessment of in vitro inhibition of CYPs, UGTs and transporters by phosphodiester- or phosphorothioate-linked oligonucleotides

Presented at the 2019 Marbach Castle Drug-Drug Interaction Workshop in Germany by Dr. Brian W. Ogilvie. Based on the publication: Kazmi F, Yerino P, McCoy...
Blog

Cypex Expands Portfolio of Recombinant Enzymes

As the exclusive distributor for Cypex in the US and Canada, SEKISUI XenoTech is proud to offer this portfolio of products based...

Publications

An assessment of the in vitro inhibition of cytochrome P450 enzymes (CYP), UDP-glucuronsyltransferases (UGT) and transporters by phosphodiester- or phosphorothioate-linked oligonucleotides

Faraz Kazmi, Phyllis Yerino, Chase McCoy, Andrew Parkinson, David B Buckley and Brian W Ogilvie Oligonucleotides represent an expanding class of pharmacotherapeutics in development for...
Scientific Posters

Evaluation of interspecies metabolic activities for Non-CYP enzymes, suitable incubation conditions

Recently, lead compound screenings has become widely used in drug development. This has led to the development of increasing range of lead compound structures with...
Scientific Posters

Effects of organ preservation solution on aldehyde oxidase and xanthine oxidase activity in pooled human liver S9

Non-transplant quality human livers donated for research are a common source of both cellular and subcellular material utilized in in vitro drug metabolism studies. At...
Blog

UGT Activities, Concomitant Drugs, and DDI

If you have concerns about how your compound may affect UDP-glucuronosyltransferase (UGT) induction and/or inhibition when combined with other therapeutic...

Scientific Posters

In Vitro Evaluation of Ketoconazole and its Alternatives as Non-CYP Inhibitors

The In Vitro Evaluation of Ketoconazole and its Alternative Clinical CYP3A4/5 Inhibitors (Ritonavir, Clarithromycin and Itraconazole) as Inhibitors of Non-CYP Enzymes ABSTRACT Ketoconazole is a...
Scientific Posters

Evaluation of Chemical Inhibitors for UDP-glucuronosyltransferase UGT Reaction Phenotyping Assays

Evaluation of Chemical Inhibitors for UDP-glucuronosyltransferase (UGT) Reaction Phenotyping Assays in Human Liver Microsomes In the development of a new chemical entity (NCE) reaction phenotyping studies...
Scientific Posters

UGT Inhibition Studies in the Presence or Absence of Alamethicin Evaluation of UGT1A1 and UGT2B7

UGT Inhibition Studies in the Presence or Absence of Alamethicin: Evaluation of UGT1A1 and UGT2B7 Inhibition in Human Liver Microsomes and Recombinant Enzymes The importance...
Publications

A long-standing mystery solved: The formation of 3-hydroxydesloratadine is catalyzed by CYP2C8 but prior glucuronidation of desloratadine by UGT2B10 is an obligatory requirement

Faraz Kazmi, Joanna E. Barbara, Phyllis Yerino and Andrew Parkinson Desloratadine (Clarinex®), the major active metabolite of loratadine (Claritin®), is a non-sedating long-lasting antihistamine widely used for...
Scientific Posters

Induction of UDP-Glucuronosyltransferases in Cultures of Fresh and Immortalized Human Hepatocytes

Induction of UDP-Glucuronosyltransferases in Primary Cultures of Fresh and ImmortalizedHuman Hepatocytes Abstract We have examined the induction of UDP-glucuronosyltransferases (UGTs) in primary cultures ofHuman hepatocytes...
Publications

In vitro inhibition of human liver cytochrome P450 (CYP) and UDP-glucuronosyltransferase (UGT) enzymes by rose bengal: system-dependent effects on inhibitory potential

Faraz Kazmi, Lois J. Haupt, Jennifer R. Horkman, Brian D. Smith, David B. Buckley, Eric A. Wachter, and Jamie M. Singer 1. Rose bengal (4,5,6,7-tetrachloro-2′,4′,5′,7′-tetraiodofluorescein)...
Scientific Posters

ISSX 2013 – Aldehyde Oxidase

Selection of human liver S9 and cytosol fractions for evaluating clearance by aldehyde oxidase (AO): The impact of low versus high AO activity lots. Aldehyde oxidase (AO) is a...
Publications

Catechol and aldehyde moieties of 3,4-dihydroxyphenylacetaldehyde contribute to tyrosine hydroxylase inhibition and neurotoxicity

Lydia M. Vermeer , Virginia R. Florang , Jonathan A. Doorn Parkinson’s disease (PD) is a progressive neurodegenerative disorder which leads to the selective loss...
Publications

Activator Protein-1 Regulation of Murine Aldehyde Dehydrogenase 1a1

Previously we demonstrated that aldehyde dehydrogenase (ALDH) 1a1 is the major ALDH expressed in mouse liver and is an effective catalyst in metabolism of lipid aldehydes...
Scientific Posters

Microsomes and S9 Prepared from Renal Tissue Yield High CYP, FMO and UGT Activities that are Stable…

Microsomes and S9 Prepared from Renal Tissue Yield High CYP, FMO and UGT Activities that are Stable over Multiple Freeze/Thaw Cycles Abstract We have developed...
Scientific Posters

Microsomes Prepared from Eluted Enterocytes Yield High Cytochrome P450 and UGT Activities that are…

Microsomes Prepared from Eluted Enterocytes Yield High Cytochrome P450 and UGT Activities that are Stable over Multiple Freeze/Thaw Cycles Abstract Enterocytes in the upper region...