The Invention of WM382, a Highly Potent PMIX/X Dual Inhibitor toward the Treatment of Malaria-Reference-Cited by-同舟云学术

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The Invention of WM382, a Highly Potent PMIX/X Dual Inhibitor toward the Treatment of Malaria

Published:2022-10-12 Issue:11 Volume:13 Page:1745-1754
ISSN:1948-5875
Container-title:ACS Medicinal Chemistry Letters
language:en
Short-container-title:ACS Med. Chem. Lett.

Author:

de Lera Ruiz Manuel¹^ORCID,Favuzza Paola²³,Guo Zhuyan¹,Zhao Lianyun¹,Hu Bin⁴,Lei Zhiyu⁴,Zhan Dongmei⁴,Murgolo Nicholas¹,Boyce Christopher W.¹,Vavrek Marissa¹,Thompson Jennifer²,Ngo Anna²,Jarman Kate E.²,Robbins Johnathan¹,Boddey Justin²³,Sleebs Brad E.²³^ORCID,Lowes Kym N.²³,Cowman Alan F.²³,Olsen David B.¹,McCauley John A.¹

Affiliation:

1. Merck & Co., Inc., 770 Sumneytown Pike, West Point, Pennsylvania 19486, United States

2. The Walter and Eliza Hall Institute of Medical Research, Parkville, VIC3052, Australia

3. University of Melbourne, Melbourne, VIC3010, Australia

4. WuXi AppTec, 288 Fute Zhong Lu, Shanghai200131, China

Funder

Wellcome Trust

Publisher

American Chemical Society (ACS)

Subject

Organic Chemistry,Drug Discovery,Biochemistry

Link

https://pubs.acs.org/doi/pdf/10.1021/acsmedchemlett.2c00355

Reference18 articles.

1. World Malaria Report 2021; World Health Organization, 2021.

2. The spread of artemisinin-resistant Plasmodium falciparum in the Greater Mekong subregion: a molecular epidemiology observational study

3. Drug-Resistant Malaria Detected in Africa Will Require Monitoring

4. Malaria parasite plasmepsins: More than just plain old degradative pepsins

5. Dual Plasmepsin-Targeting Antimalarial Agents Disrupt Multiple Stages of the Malaria Parasite Life Cycle

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1. Assessing the interplay between off-target promiscuity, cytotoxicity, and tolerability in rodents to improve the safety profile of novel anti-malarial plasmepsin X inhibitors;Toxicological Sciences;2024-07-08

2. Advances in protease inhibition-based chemotherapy: A decade of insights from Malaria Research;Advances in Parasitology;2024

3. Design of Novel Series of Antimalarial PMX Inhibitors with Increased Half-Life via Molecular Property Optimization;ACS Medicinal Chemistry Letters;2023-10-20

4. Antimalarial drug discovery: progress and approaches;Nature Reviews Drug Discovery;2023-08-31

5. Plasmepsin X activates the PCRCR complex of Plasmodium falciparum by processing PfRh5 for erythrocyte invasion;Nature Communications;2023-04-19

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