High-throughput screening technologies for drug glucuronidation profiling.

High-throughput screening technologies for drug glucuronidation profiling. Research Abstract Details 

Research Abstract Table of Contents

Jump to the:

High-throughput screening technologies for drug glucuronidation profiling. Abstract Text:

A significant number of endogenous and exogenous compounds, including many therapeutic agents, are metabolized in humans via glucuronidation, catalysed by uridine diphosphoglucuronosyltransferases (UGTs). The study of the UGTs is a growing field of research, with constantly accumulated and updated information regarding UGT structure, purification, substrate specificity and inhibition, including clinically relevant drug interactions. Development of reliable UGT assays for the assessment of individual isoform substrate specificity and for the discovery of novel isoform-specific substrates and inhibitors is crucial for understanding the function and regulation of the UGT enzyme family and its clinical and pharmacological relevance. High-throughput screening (HTS) is a powerful technology used to search for novel substrates and inhibitors for a wide variety of targets. However, application of HTS in the context of UGTs is complicated because of the poor stability, low levels of expression, low affinity and broad substrate specificity of the enzymes, combined with difficulties in obtaining individual UGT isoforms in purified format, and insufficient information regarding isoform-specific substrates and inhibitors. This review examines the current status of HTS assays used in the search for novel UGT substrates and inhibitors, emphasizing advancements and challenges in HTS technologies for drug glucuronidation profiling, and discusses possible avenues for future advancement of the field.

High-throughput screening technologies for drug glucuronidation profiling. Publishing Authors By Initials

For similar abstracts research abstracts see: abstracts research

PUBMED ID PMID:

MEDLINE DATE:

High-throughput screening technologies for drug glucuronidation profiling. Journal Published:

PUBLICATION TYPE: Journal Article

Journal: The Journal of pharmacy and pharmacology

VOLUME: 60

Page Numbers: 1061-7

Journal Abbreviation: J. Pharm. Pharmacol.

ISSN: 0022-3573

DAY: 22

MONTH: Aug

YEAR: 2008

High-throughput screening technologies for drug glucuronidation profiling. Information

Number of References:

LANGUAGE: eng

NlmUniqueID: 376363

High-throughput screening technologies for drug glucuronidation profiling. Keywords Mesh Terms:

KEYWORDS:

MESH TERMS:

Chemical & Substance for Abstract: High-throughput screening technologies for drug glucuronidation profiling. Information

Substance Name:

Registry Number:

Grant and Affiliation Information for High-throughput screening technologies for drug glucuronidation profiling.

AFFILIATION: School of Pharmacy, University of Wisconsin, Madison, Wisconsin, USA.

Country: England

AGENCY:

GRANT:

ACRONYM:

MEDLINETA: J Pharm Pharmacol

REFSOURCE:

DATABASENAME:

ACCESSION NUMBER:

Number Hits: 0

High-throughput screening technologies for drug glucuronidation profiling Related Publications

• Evaluation of synthetic polymeric micelles as a stabilization medium for the handling of membrane proteins in pharmaceutical drug discovery.
• High throughput screening assay for UDP-glucuronosyltransferase 1A1 glucuronidation profiling.
• High-throughput screening technologies for drug glucuronidation profiling.