Antimalarial Inhibitors Targeting Serine Hydroxymethyltransferase (SHMT) with in Vivo Efficacy and Analysis of their Binding Mode Based on X-ray Cocrystal Structures-Reference-Cited by-同舟云学术

Antimalarial Inhibitors Targeting Serine Hydroxymethyltransferase (SHMT) with in Vivo Efficacy and Analysis of their Binding Mode Based on X-ray Cocrystal Structures

Published:2017-06-13 Issue:12 Volume:60 Page:4840-4860
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Schwertz Geoffrey¹,Witschel Matthias C.²,Rottmann Matthias³⁴,Bonnert Roger⁵,Leartsakulpanich Ubolsree⁶,Chitnumsub Penchit⁶,Jaruwat Aritsara⁶,Ittarat Wanwipa⁶,Schäfer Anja³⁴,Aponte Raphael A.²,Charman Susan A.⁷,White Karen L.⁷,Kundu Abhijit⁸,Sadhukhan Surajit⁸,Lloyd Mel⁹,Freiberg Gail M.¹⁰,Srikumaran Myron¹⁰,Siggel Marc¹,Zwyssig Adrian¹,Chaiyen Pimchai¹¹,Diederich François¹^ORCID

Affiliation:

1. Laboratorium für Organische Chemie, ETH Zurich, Vladimir-Prelog-Weg 3, 8093 Zurich, Switzerland

2. BASF SE, Carl-Bosch-Strasse 38, 67056 Ludwigshafen, Germany

3. Swiss Tropical and Public Health Institute (SwissTPH), Socinstrasse 57, 4051 Basel, Switzerland

4. Universität Basel, Petersplatz 1, 4003 Basel, Switzerland

5. Medicines for Malaria Venture, Route de Pré-Bois 20, CH-1215 Geneva, Switzerland

6. National Center for Genetic Engineering and Biotechnology, 113 Thailand Science Park, Phahonyothin Road, Pathumthni 12120, Thailand

7. Centre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, 381 Royal Parade, Parkville, Victoria 3052, Australia

8. TCG Lifesciences Private Limited, Block BN, Plot 7, Saltlake Electronics Complex, Sector V, Kolkata 700091, West Bengal India

9. Covance Laboratories Ltd., Otley Road, Harrogate HG3 1PY, United Kingdom

10. Molecular Characterization, Department R4AE, AbbVie, 1 North Waukegan Road, North Chicago, Illinois 60064-6217, United States

11. Department of Biochemistry and Center for Excellence in Protein and Enzyme Technology, Faculty of Science Mahidol University, 272 Rama VI Road, Bangkok 10400, Thailand

Funder

Eidgenössische Technische Hochschule Zürich

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.7b00008

Reference62 articles.

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4. Artemisinin and Artemisinin-Based Combination Therapy Resistance;Status Report Global Malaria Programme;World Health Organization:Geneva, October 2016.

5. A molecular mechanism of artemisinin resistance in Plasmodium falciparum malaria

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