Inhibitors of Plasmepsin II – Potential Antimalarial Agents

Malaria is a very serious infectious disease affecting over two billion people worldwide. Currently available antimalarial drugs are losing effectiveness due to the emergence and the spread of resistant parasite strains. In order to regain control over the disease, new treatments are urgen...

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Main Authors: Christoph Boss, Reto Brun, Walter Fischli, Christoph Binkert, Solange Meyer, Lars Prade, Luke Harris, Lionel Coppex, Corinna Grisostomi, Olivier Corminboeuf, Jean-Marc Bourgeois, Rocco Furnari, Sylvia Richard-Bildstein, Thomas Weller
Format: Article
Language:deu
Published: Swiss Chemical Society 2004-09-01
Series:CHIMIA
Subjects:
Online Access:https://chimia.ch/chimia/article/view/3880
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author Christoph Boss
Reto Brun
Walter Fischli
Christoph Binkert
Solange Meyer
Lars Prade
Luke Harris
Lionel Coppex
Corinna Grisostomi
Olivier Corminboeuf
Jean-Marc Bourgeois
Rocco Furnari
Sylvia Richard-Bildstein
Thomas Weller
author_facet Christoph Boss
Reto Brun
Walter Fischli
Christoph Binkert
Solange Meyer
Lars Prade
Luke Harris
Lionel Coppex
Corinna Grisostomi
Olivier Corminboeuf
Jean-Marc Bourgeois
Rocco Furnari
Sylvia Richard-Bildstein
Thomas Weller
author_sort Christoph Boss
collection DOAJ
description Malaria is a very serious infectious disease affecting over two billion people worldwide. Currently available antimalarial drugs are losing effectiveness due to the emergence and the spread of resistant parasite strains. In order to regain control over the disease, new treatments are urgently needed. Drug discovery efforts in this direction are most likely to be successful if they target a novel mechanism of action. Such approaches will lead to antimalarial medicines that are functionally and structurally different from the existing drugs and therefore will have the potential to overcome existing resistances. Our own efforts are focused on the aspartic protease plasmepsin II (PMII) which is a promising new drug target for future antimalarial therapies. We have found structurally simple, moderately active, non-peptide inhibitors of plasmepsin II which offer ample opportunity for further optimization efforts.
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spelling doaj.art-fd58db8601ee4bc29579ec1db0929e932022-12-22T02:46:09ZdeuSwiss Chemical SocietyCHIMIA0009-42932673-24242004-09-0158910.2533/000942904777677524Inhibitors of Plasmepsin II – Potential Antimalarial AgentsChristoph BossReto BrunWalter FischliChristoph BinkertSolange MeyerLars PradeLuke HarrisLionel CoppexCorinna GrisostomiOlivier CorminboeufJean-Marc BourgeoisRocco FurnariSylvia Richard-BildsteinThomas Weller Malaria is a very serious infectious disease affecting over two billion people worldwide. Currently available antimalarial drugs are losing effectiveness due to the emergence and the spread of resistant parasite strains. In order to regain control over the disease, new treatments are urgently needed. Drug discovery efforts in this direction are most likely to be successful if they target a novel mechanism of action. Such approaches will lead to antimalarial medicines that are functionally and structurally different from the existing drugs and therefore will have the potential to overcome existing resistances. Our own efforts are focused on the aspartic protease plasmepsin II (PMII) which is a promising new drug target for future antimalarial therapies. We have found structurally simple, moderately active, non-peptide inhibitors of plasmepsin II which offer ample opportunity for further optimization efforts. https://chimia.ch/chimia/article/view/3880Aspartic proteasesEnzyme inhibitorsMalariaMedicinal chemistryPlasmepsin ii (pmii)
spellingShingle Christoph Boss
Reto Brun
Walter Fischli
Christoph Binkert
Solange Meyer
Lars Prade
Luke Harris
Lionel Coppex
Corinna Grisostomi
Olivier Corminboeuf
Jean-Marc Bourgeois
Rocco Furnari
Sylvia Richard-Bildstein
Thomas Weller
Inhibitors of Plasmepsin II – Potential Antimalarial Agents
CHIMIA
Aspartic proteases
Enzyme inhibitors
Malaria
Medicinal chemistry
Plasmepsin ii (pmii)
title Inhibitors of Plasmepsin II – Potential Antimalarial Agents
title_full Inhibitors of Plasmepsin II – Potential Antimalarial Agents
title_fullStr Inhibitors of Plasmepsin II – Potential Antimalarial Agents
title_full_unstemmed Inhibitors of Plasmepsin II – Potential Antimalarial Agents
title_short Inhibitors of Plasmepsin II – Potential Antimalarial Agents
title_sort inhibitors of plasmepsin ii potential antimalarial agents
topic Aspartic proteases
Enzyme inhibitors
Malaria
Medicinal chemistry
Plasmepsin ii (pmii)
url https://chimia.ch/chimia/article/view/3880
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