Structural basis of malaria parasite phenylalanine tRNA-synthetase inhibition by bicyclic azetidines

Bicyclic azetidine inhibitors are promising antimalarials that target the Plasmodium cytosolic phenylalanine tRNAsynthetase (cFRS). Here, Sharma et al. provide the biochemical and structural basis of its mechanism using co-crystal structure of PvcFRS with BRD1389.

Bibliographic Details
Main Authors:	Manmohan Sharma, Nipun Malhotra, Manickam Yogavel, Karl Harlos, Bruno Melillo, Eamon Comer, Arthur Gonse, Suhel Parvez, Branko Mitasev, Francis G. Fang, Stuart L. Schreiber, Amit Sharma
Format:	Article
Language:	English
Published:	Nature Publishing Group 2021-01-01
Series:	Nature Communications
Online Access:	https://doi.org/10.1038/s41467-020-20478-5

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spelling	doaj-96b3e407ffe647c5b54ac432fe843d792021-01-17T12:12:05ZengNature Publishing GroupNature Communications2041-17232021-01-0112111010.1038/s41467-020-20478-5Structural basis of malaria parasite phenylalanine tRNA-synthetase inhibition by bicyclic azetidinesManmohan Sharma0Nipun Malhotra1Manickam Yogavel2Karl Harlos3Bruno Melillo4Eamon Comer5Arthur Gonse6Suhel Parvez7Branko Mitasev8Francis G. Fang9Stuart L. Schreiber10Amit Sharma11Molecular Medicine, Structural Parasitology Group, International Centre for Genetic Engineering and BiotechnologyMolecular Medicine, Structural Parasitology Group, International Centre for Genetic Engineering and BiotechnologyMolecular Medicine, Structural Parasitology Group, International Centre for Genetic Engineering and BiotechnologyDivision of Structural Biology, Welcome Centre for Human Genetics, University of OxfordChemical Biology and Therapeutics Science Program, Broad Institute of Harvard and MITChemical Biology and Therapeutics Science Program, Broad Institute of Harvard and MITChemical Biology and Therapeutics Science Program, Broad Institute of Harvard and MITDepartment of Medical Elementology and Toxicology, School of Chemical and Life Sciences, Jamia HamdardEisai Inc.Eisai Inc.Chemical Biology and Therapeutics Science Program, Broad Institute of Harvard and MITMolecular Medicine, Structural Parasitology Group, International Centre for Genetic Engineering and BiotechnologyBicyclic azetidine inhibitors are promising antimalarials that target the Plasmodium cytosolic phenylalanine tRNAsynthetase (cFRS). Here, Sharma et al. provide the biochemical and structural basis of its mechanism using co-crystal structure of PvcFRS with BRD1389.https://doi.org/10.1038/s41467-020-20478-5
collection	DOAJ
language	English
format	Article
sources	DOAJ
author	Manmohan Sharma Nipun Malhotra Manickam Yogavel Karl Harlos Bruno Melillo Eamon Comer Arthur Gonse Suhel Parvez Branko Mitasev Francis G. Fang Stuart L. Schreiber Amit Sharma
spellingShingle	Manmohan Sharma Nipun Malhotra Manickam Yogavel Karl Harlos Bruno Melillo Eamon Comer Arthur Gonse Suhel Parvez Branko Mitasev Francis G. Fang Stuart L. Schreiber Amit Sharma Structural basis of malaria parasite phenylalanine tRNA-synthetase inhibition by bicyclic azetidines Nature Communications
author_facet	Manmohan Sharma Nipun Malhotra Manickam Yogavel Karl Harlos Bruno Melillo Eamon Comer Arthur Gonse Suhel Parvez Branko Mitasev Francis G. Fang Stuart L. Schreiber Amit Sharma
author_sort	Manmohan Sharma
title	Structural basis of malaria parasite phenylalanine tRNA-synthetase inhibition by bicyclic azetidines
title_short	Structural basis of malaria parasite phenylalanine tRNA-synthetase inhibition by bicyclic azetidines
title_full	Structural basis of malaria parasite phenylalanine tRNA-synthetase inhibition by bicyclic azetidines
title_fullStr	Structural basis of malaria parasite phenylalanine tRNA-synthetase inhibition by bicyclic azetidines
title_full_unstemmed	Structural basis of malaria parasite phenylalanine tRNA-synthetase inhibition by bicyclic azetidines
title_sort	structural basis of malaria parasite phenylalanine trna-synthetase inhibition by bicyclic azetidines
publisher	Nature Publishing Group
series	Nature Communications
issn	2041-1723
publishDate	2021-01-01
description	Bicyclic azetidine inhibitors are promising antimalarials that target the Plasmodium cytosolic phenylalanine tRNAsynthetase (cFRS). Here, Sharma et al. provide the biochemical and structural basis of its mechanism using co-crystal structure of PvcFRS with BRD1389.
url	https://doi.org/10.1038/s41467-020-20478-5
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Structural basis of malaria parasite phenylalanine tRNA-synthetase inhibition by bicyclic azetidines

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