The war on hTG2: warhead optimization in small molecule human tissue transglutaminase inhibitors-Reference-Cited by-同舟云学术

The war on hTG2: warhead optimization in small molecule human tissue transglutaminase inhibitors

Published:2023 Issue:2 Volume:14 Page:277-298
ISSN:2632-8682
Container-title:RSC Medicinal Chemistry
language:en
Short-container-title:RSC Med. Chem.

Author:

Mader Lavleen¹^ORCID,Watt Sarah K. I.¹,Iyer Harish R.²,Nguyen Linh²,Kaur Harpreet²,Keillor Jeffrey W.¹^ORCID

Affiliation:

1. Department of Chemistry and Biomolecular Sciences, University of Ottawa, Ottawa, Ontario K1N 6N5, Canada

2. Dalriada Drug Discovery, Mississauga, Ontario L5N 8G4, Canada

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.

Funder

Natural Sciences and Engineering Research Council of Canada

Canadian Institutes of Health Research

Publisher

Royal Society of Chemistry (RSC)

Subject

Organic Chemistry,Drug Discovery,Pharmaceutical Science,Pharmacology,Molecular Medicine,Biochemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2023/MD/D2MD00378C

Reference59 articles.

1. Transglutaminase 2: A molecular Swiss army knife

2. Transglutaminase Regulation of Cell Function

3. Acyl transfer mechanisms of tissue transglutaminase

4. The diamond anniversary of tissue transglutaminase: a protein of many talents

5. Tissue transglutaminase: an enzyme with a split personality

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