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Drug Discovery
The Medicinal Chemist's Guide to Solving ADMET ChallengesCheck Access
Edited by
Patrick Schnider
Patrick Schnider
Bottmingen, Switzerland
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Hardback ISBN:
978-1-78801-227-0
PDF ISBN:
978-1-78801-641-4
EPUB ISBN:
978-1-83916-049-3
Special Collection:
2021 ebook collection
Series:
Drug Discovery Series
No. of Pages:
518
Published online:
20 Aug 2021
Published in print:
27 Aug 2021
Book Chapter
CHAPTER 13: Glucuronidation Check Access
By
Yue Pan
Yue Pan
Global Discovery Chemistry, Novartis Institutes for BioMedical Research
22 Windsor Street
Cambridge
Massachusetts 02139
USA
[email protected]
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Published:20 Aug 2021
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Special Collection: 2021 ebook collectionSeries: Drug Discovery Series
Page range:
278 - 302
Citation
Y. Pan, in The Medicinal Chemist's Guide to Solving ADMET Challenges, ed. P. Schnider, The Royal Society of Chemistry, 2021, pp. 278-302.
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Glucuronidation catalyzed by uridine 5′-diphospho-glucuronosyltransferase (UGT) is the most common phase II metabolism. The UGTs can severely limit a drug's exposure and generate reactive metabolites, leading to toxicity. This chapter provides a brief overview of the current understanding of the UGT enzyme family, followed by various medicinal chemistry strategies to address this metabolic liability and select examples from the literature.
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