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RSC Medicinal Chemistry
Article . 2023
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The war on hTG2: warhead optimization in small molecule human tissue transglutaminase inhibitors

Authors: Lavleen Mader; Sarah K. I. Watt; Harish R. Iyer; Linh Nguyen; Harpreet Kaur; Jeffrey W. Keillor;
Lavleen Mader; Sarah K. I. Watt; Harish R. Iyer; Linh Nguyen; Harpreet Kaur; Jeffrey W. Keillor;
doi: 10.1039/d2md00378c
The war on hTG2: warhead optimization in small molecule human tissue transglutaminase inhibitors
Abstract
This systematic structure–activity relationship study provides key insights into warhead design and application for optimizing efficiency, selectivity, and pharmacokinetic stability of hTG2 inhibitors.
Keywords
Pharmacology, Organic Chemistry, Drug Discovery, Pharmaceutical Science, Molecular Medicine, Biochemistry
Pharmacology, Organic Chemistry, Drug Discovery, Pharmaceutical Science, Molecular Medicine, Biochemistry
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This systematic structure–activity relationship study provides key insights into warhead design and application for optimizing efficiency, selectivity, and pharmacokinetic stability of hTG2 inhibitors.