Literature DB >> 22284359

Global phenotypic screening for antimalarials.

W Armand Guiguemde1, Anang A Shelat, Jose F Garcia-Bustos, Thierry T Diagana, Francisco-Javier Gamo, R Kiplin Guy.   

Abstract

Malaria, a devastating infectious disease caused by Plasmodium spp., leads to roughly 655,000 deaths per year, mostly of African children. To compound the problem, drug resistance has emerged to all classical antimalarials and may be emerging for artemisinin-based combination therapies. To address the need for new antimalarials with novel mechanisms, several groups carried out phenotypic screening campaigns to identify compounds inhibiting growth of the blood stages of Plasmodium falciparum. In this review, we describe the characterization of these compounds, explore currently ongoing strategies to develop lead molecules, and endorse the concept of a "malaria box" of publicly accessible active compounds.
Copyright © 2012 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID: 22284359      PMCID: PMC3269778          DOI: 10.1016/j.chembiol.2012.01.004

Source DB:  PubMed          Journal:  Chem Biol        ISSN: 1074-5521


  84 in total

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2.  Conversion of dihydroorotate to orotate in parasitic protozoa.

Authors:  W E Gutteridge; D Dave; W H Richards
Journal:  Biochim Biophys Acta       Date:  1979-02-01

3.  Genome-scale protein expression and structural biology of Plasmodium falciparum and related Apicomplexan organisms.

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Journal:  Mol Biochem Parasitol       Date:  2006-11-13       Impact factor: 1.759

4.  Identification and activity of a series of azole-based compounds with lactate dehydrogenase-directed anti-malarial activity.

Authors:  Angus Cameron; Jon Read; Rebecca Tranter; Victoria J Winter; Richard B Sessions; R Leo Brady; Livia Vivas; Anna Easton; Howard Kendrick; Simon L Croft; David Barros; Jose Luis Lavandera; José Julio Martin; Felix Risco; Silvestre García-Ochoa; Fracisco Javier Gamo; Laura Sanz; Luisa Leon; Jose R Ruiz; Raquel Gabarró; Araceli Mallo; Federico Gómez de las Heras
Journal:  J Biol Chem       Date:  2004-04-26       Impact factor: 5.157

5.  In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen.

Authors:  David Plouffe; Achim Brinker; Case McNamara; Kerstin Henson; Nobutaka Kato; Kelli Kuhen; Advait Nagle; Francisco Adrián; Jason T Matzen; Paul Anderson; Tae-Gyu Nam; Nathanael S Gray; Arnab Chatterjee; Jeff Janes; S Frank Yan; Richard Trager; Jeremy S Caldwell; Peter G Schultz; Yingyao Zhou; Elizabeth A Winzeler
Journal:  Proc Natl Acad Sci U S A       Date:  2008-06-25       Impact factor: 11.205

6.  Artemisinin resistance in Plasmodium falciparum malaria.

Authors:  Arjen M Dondorp; François Nosten; Poravuth Yi; Debashish Das; Aung Phae Phyo; Joel Tarning; Khin Maung Lwin; Frederic Ariey; Warunee Hanpithakpong; Sue J Lee; Pascal Ringwald; Kamolrat Silamut; Mallika Imwong; Kesinee Chotivanich; Pharath Lim; Trent Herdman; Sen Sam An; Shunmay Yeung; Pratap Singhasivanon; Nicholas P J Day; Niklas Lindegardh; Duong Socheat; Nicholas J White
Journal:  N Engl J Med       Date:  2009-07-30       Impact factor: 91.245

7.  Towards an in vitro model of Plasmodium hypnozoites suitable for drug discovery.

Authors:  Laurent Dembele; Audrey Gego; Anne-Marie Zeeman; Jean-François Franetich; Olivier Silvie; Armelle Rametti; Roger Le Grand; Nathalie Dereuddre-Bosquet; Robert Sauerwein; Geert-Jan van Gemert; Jean-Christophe Vaillant; Alan W Thomas; Georges Snounou; Clemens H M Kocken; Dominique Mazier
Journal:  PLoS One       Date:  2011-03-31       Impact factor: 3.240

8.  A high-throughput screen targeting malaria transmission stages opens new avenues for drug development.

Authors:  Kathrin Buchholz; Thomas A Burke; Kim C Williamson; Roger C Wiegand; Dyann F Wirth; Matthias Marti
Journal:  J Infect Dis       Date:  2011-05-15       Impact factor: 5.226

9.  Novel polymorphisms in Plasmodium falciparum ABC transporter genes are associated with major ACT antimalarial drug resistance.

Authors:  Maria Isabel Veiga; Pedro Eduardo Ferreira; Louise Jörnhagen; Maja Malmberg; Aminatou Kone; Berit Aydin Schmidt; Max Petzold; Anders Björkman; Francois Nosten; Jose Pedro Gil
Journal:  PLoS One       Date:  2011-05-25       Impact factor: 3.240

10.  A chemical genomic analysis of decoquinate, a Plasmodium falciparum cytochrome b inhibitor.

Authors:  Tae-Gyu Nam; Case W McNamara; Selina Bopp; Neekesh V Dharia; Stephan Meister; Ghislain M C Bonamy; David M Plouffe; Nobutaka Kato; Susan McCormack; Badry Bursulaya; Hangjun Ke; Akhil B Vaidya; Peter G Schultz; Elizabeth A Winzeler
Journal:  ACS Chem Biol       Date:  2011-09-08       Impact factor: 5.100

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  37 in total

1.  Fully functionalized small-molecule probes for integrated phenotypic screening and target identification.

Authors:  Justin S Cisar; Benjamin F Cravatt
Journal:  J Am Chem Soc       Date:  2012-06-13       Impact factor: 15.419

2.  The importance of molecular complexity in the design of screening libraries.

Authors:  Shahul H Nilar; Ngai Ling Ma; Thomas H Keller
Journal:  J Comput Aided Mol Des       Date:  2013-09       Impact factor: 3.686

3.  In Silico screening on the three-dimensional model of the Plasmodium vivax SUB1 protease leads to the validation of a novel anti-parasite compound.

Authors:  Anthony Bouillon; David Giganti; Christophe Benedet; Olivier Gorgette; Stéphane Pêtres; Elodie Crublet; Christine Girard-Blanc; Benoit Witkowski; Didier Ménard; Michael Nilges; Odile Mercereau-Puijalon; Véronique Stoven; Jean-Christophe Barale
Journal:  J Biol Chem       Date:  2013-05-07       Impact factor: 5.157

Review 4.  Three-dimensional structures in the design of therapeutics targeting parasitic protozoa: reflections on the past, present and future.

Authors:  Wim G J Hol
Journal:  Acta Crystallogr F Struct Biol Commun       Date:  2015-04-16       Impact factor: 1.056

5.  Systems-level antimicrobial drug and drug synergy discovery.

Authors:  Terry Roemer; Charles Boone
Journal:  Nat Chem Biol       Date:  2013-04       Impact factor: 15.040

6.  Extensive Shared Chemosensitivity between Malaria and Babesiosis Blood-Stage Parasites.

Authors:  Aditya S Paul; Cristina K Moreira; Brendan Elsworth; David R Allred; Manoj T Duraisingh
Journal:  Antimicrob Agents Chemother       Date:  2016-07-22       Impact factor: 5.191

7.  Does Plasmodium falciparum have an Achilles' heel?

Authors:  Liao Y Chen
Journal:  Malar Chemother Control Elimin       Date:  2014-04-05

Review 8.  Antimalarial drug discovery - approaches and progress towards new medicines.

Authors:  Erika L Flannery; Arnab K Chatterjee; Elizabeth A Winzeler
Journal:  Nat Rev Microbiol       Date:  2013-11-11       Impact factor: 60.633

9.  Identification of Novel Plasmodium falciparum Hexokinase Inhibitors with Antiparasitic Activity.

Authors:  Mindy I Davis; Stephen L Patrick; Walker M Blanding; Varun Dwivedi; Jimmy Suryadi; Jennifer E Golden; Nathan P Coussens; Olivia W Lee; Min Shen; Matthew B Boxer; Matthew D Hall; Elizabeth R Sharlow; Mark E Drew; James C Morris
Journal:  Antimicrob Agents Chemother       Date:  2016-09-23       Impact factor: 5.191

10.  Dihydroquinazolinone inhibitors of proliferation of blood and liver stage malaria parasites.

Authors:  Emily R Derbyshire; Jaeki Min; W Armand Guiguemde; Julie A Clark; Michele C Connelly; Andreia D Magalhães; R Kiplin Guy; Jon Clardy
Journal:  Antimicrob Agents Chemother       Date:  2013-12-23       Impact factor: 5.191

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