Esterase mutation is a mechanism of resistance to antimalarial compounds

Pepstatin is a known inhibitor of malarial proteases, but its activity varies between sources. Here, Istvanet al. identify a pepstatin ester as the active component of pepstatin preparations and show that this prodrug is activated by a Plasmodiumesterase, mutation of which can confer resistance to p...

Full description

Bibliographic Details
Main Authors:	Eva S. Istvan, Jeremy P. Mallari, Victoria C. Corey, Neekesh V. Dharia, Garland R. Marshall, Elizabeth A. Winzeler, Daniel E. Goldberg
Format:	Article
Language:	English
Published:	Nature Publishing Group 2017-01-01
Series:	Nature Communications
Online Access:	https://doi.org/10.1038/ncomms14240

id	doaj-1d38f9612f4048a39eb045aecf7bcf36
record_format	Article
spelling	doaj-1d38f9612f4048a39eb045aecf7bcf362021-05-11T07:09:06ZengNature Publishing GroupNature Communications2041-17232017-01-01811810.1038/ncomms14240Esterase mutation is a mechanism of resistance to antimalarial compoundsEva S. Istvan0Jeremy P. Mallari1Victoria C. Corey2Neekesh V. Dharia3Garland R. Marshall4Elizabeth A. Winzeler5Daniel E. Goldberg6Department of Medicine, Division of Infectious Diseases, Washington University School of MedicineDepartment of Medicine, Division of Infectious Diseases, Washington University School of MedicineDepartment of Pediatrics, School of Medicine, University of California San Diego School of MedicineDepartment of Pediatrics, School of Medicine, University of California San Diego School of MedicineDepartment of Biochemistry and Molecular Biophysics, Washington University School of MedicineDepartment of Pediatrics, School of Medicine, University of California San Diego School of MedicineDepartment of Medicine, Division of Infectious Diseases, Washington University School of MedicinePepstatin is a known inhibitor of malarial proteases, but its activity varies between sources. Here, Istvanet al. identify a pepstatin ester as the active component of pepstatin preparations and show that this prodrug is activated by a Plasmodiumesterase, mutation of which can confer resistance to pepstatin and other compounds.https://doi.org/10.1038/ncomms14240
collection	DOAJ
language	English
format	Article
sources	DOAJ
author	Eva S. Istvan Jeremy P. Mallari Victoria C. Corey Neekesh V. Dharia Garland R. Marshall Elizabeth A. Winzeler Daniel E. Goldberg
spellingShingle	Eva S. Istvan Jeremy P. Mallari Victoria C. Corey Neekesh V. Dharia Garland R. Marshall Elizabeth A. Winzeler Daniel E. Goldberg Esterase mutation is a mechanism of resistance to antimalarial compounds Nature Communications
author_facet	Eva S. Istvan Jeremy P. Mallari Victoria C. Corey Neekesh V. Dharia Garland R. Marshall Elizabeth A. Winzeler Daniel E. Goldberg
author_sort	Eva S. Istvan
title	Esterase mutation is a mechanism of resistance to antimalarial compounds
title_short	Esterase mutation is a mechanism of resistance to antimalarial compounds
title_full	Esterase mutation is a mechanism of resistance to antimalarial compounds
title_fullStr	Esterase mutation is a mechanism of resistance to antimalarial compounds
title_full_unstemmed	Esterase mutation is a mechanism of resistance to antimalarial compounds
title_sort	esterase mutation is a mechanism of resistance to antimalarial compounds
publisher	Nature Publishing Group
series	Nature Communications
issn	2041-1723
publishDate	2017-01-01
description	Pepstatin is a known inhibitor of malarial proteases, but its activity varies between sources. Here, Istvanet al. identify a pepstatin ester as the active component of pepstatin preparations and show that this prodrug is activated by a Plasmodiumesterase, mutation of which can confer resistance to pepstatin and other compounds.
url	https://doi.org/10.1038/ncomms14240
work_keys_str_mv	AT evasistvan esterasemutationisamechanismofresistancetoantimalarialcompounds AT jeremypmallari esterasemutationisamechanismofresistancetoantimalarialcompounds AT victoriaccorey esterasemutationisamechanismofresistancetoantimalarialcompounds AT neekeshvdharia esterasemutationisamechanismofresistancetoantimalarialcompounds AT garlandrmarshall esterasemutationisamechanismofresistancetoantimalarialcompounds AT elizabethawinzeler esterasemutationisamechanismofresistancetoantimalarialcompounds AT danielegoldberg esterasemutationisamechanismofresistancetoantimalarialcompounds
_version_	1721452733260627968

Esterase mutation is a mechanism of resistance to antimalarial compounds

Similar Items