Literature DB >> 26435527

Hit and lead criteria in drug discovery for infectious diseases of the developing world.

Kei Katsuno1, Jeremy N Burrows2, Ken Duncan3, Rob Hooft van Huijsduijnen2, Takushi Kaneko4, Kiyoshi Kita5, Charles E Mowbray6, Dennis Schmatz2, Peter Warner3, B T Slingsby1.   

Abstract

Reducing the burden of infectious diseases that affect people in the developing world requires sustained collaborative drug discovery efforts. The quality of the chemical starting points for such projects is a key factor in improving the likelihood of clinical success, and so it is important to set clear go/no-go criteria for the progression of hit and lead compounds. With this in mind, the Japanese Global Health Innovative Technology (GHIT) Fund convened with experts from the Medicines for Malaria Venture, the Drugs for Neglected Diseases initiative and the TB Alliance, together with representatives from the Bill &Melinda Gates Foundation, to set disease-specific criteria for hits and leads for malaria, tuberculosis, visceral leishmaniasis and Chagas disease. Here, we present the agreed criteria and discuss the underlying rationale.

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Year:  2015        PMID: 26435527     DOI: 10.1038/nrd4683

Source DB:  PubMed          Journal:  Nat Rev Drug Discov        ISSN: 1474-1776            Impact factor:   84.694


  76 in total

Review 1.  Malaria medicines: a glass half full?

Authors:  Timothy N C Wells; Rob Hooft van Huijsduijnen; Wesley C Van Voorhis
Journal:  Nat Rev Drug Discov       Date:  2015-05-22       Impact factor: 84.694

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Authors:  Jonathan B Baell; Georgina A Holloway
Journal:  J Med Chem       Date:  2010-04-08       Impact factor: 7.446

3.  Rapid, low-technology MIC determination with clinical Mycobacterium tuberculosis isolates by using the microplate Alamar Blue assay.

Authors:  S G Franzblau; R S Witzig; J C McLaughlin; P Torres; G Madico; A Hernandez; M T Degnan; M B Cook; V K Quenzer; R M Ferguson; R H Gilman
Journal:  J Clin Microbiol       Date:  1998-02       Impact factor: 5.948

4.  Phenotypic vs. target-based drug discovery for first-in-class medicines.

Authors:  D C Swinney
Journal:  Clin Pharmacol Ther       Date:  2013-04       Impact factor: 6.875

5.  The Global Health Innovative Technology (GHIT) Fund: financing medical innovations for neglected populations.

Authors:  B T Slingsby; Kiyoshi Kurokawa
Journal:  Lancet Glob Health       Date:  2013-09-24       Impact factor: 26.763

6.  Imaging of Plasmodium liver stages to drive next-generation antimalarial drug discovery.

Authors:  Stephan Meister; David M Plouffe; Kelli L Kuhen; Ghislain M C Bonamy; Tao Wu; S Whitney Barnes; Selina E Bopp; Rachel Borboa; A Taylor Bright; Jianwei Che; Steve Cohen; Neekesh V Dharia; Kerstin Gagaring; Montip Gettayacamin; Perry Gordon; Todd Groessl; Nobutaka Kato; Marcus C S Lee; Case W McNamara; David A Fidock; Advait Nagle; Tae-gyu Nam; Wendy Richmond; Jason Roland; Matthias Rottmann; Bin Zhou; Patrick Froissard; Richard J Glynne; Dominique Mazier; Jetsumon Sattabongkot; Peter G Schultz; Tove Tuntland; John R Walker; Yingyao Zhou; Arnab Chatterjee; Thierry T Diagana; Elizabeth A Winzeler
Journal:  Science       Date:  2011-11-17       Impact factor: 47.728

7.  Chemical genetics of Plasmodium falciparum.

Authors:  W Armand Guiguemde; Anang A Shelat; David Bouck; Sandra Duffy; Gregory J Crowther; Paul H Davis; David C Smithson; Michele Connelly; Julie Clark; Fangyi Zhu; María B Jiménez-Díaz; María S Martinez; Emily B Wilson; Abhai K Tripathi; Jiri Gut; Elizabeth R Sharlow; Ian Bathurst; Farah El Mazouni; Joseph W Fowble; Isaac Forquer; Paula L McGinley; Steve Castro; Iñigo Angulo-Barturen; Santiago Ferrer; Philip J Rosenthal; Joseph L Derisi; David J Sullivan; John S Lazo; David S Roos; Michael K Riscoe; Margaret A Phillips; Pradipsinh K Rathod; Wesley C Van Voorhis; Vicky M Avery; R Kiplin Guy
Journal:  Nature       Date:  2010-05-20       Impact factor: 49.962

8.  Selection and optimization of hits from a high-throughput phenotypic screen against Trypanosoma cruzi.

Authors:  Martine Keenan; Paul W Alexander; Jason H Chaplin; Michael J Abbott; Hugo Diao; Zhisen Wang; Wayne M Best; Catherine J Perez; Scott M J Cornwall; Sarah K Keatley; R C Andrew Thompson; Susan A Charman; Karen L White; Eileen Ryan; Gong Chen; Jean-Robert Ioset; Thomas W von Geldern; Eric Chatelain
Journal:  Future Med Chem       Date:  2013-10       Impact factor: 3.808

Review 9.  Designing the next generation of medicines for malaria control and eradication.

Authors:  Jeremy N Burrows; Rob Hooft van Huijsduijnen; Jörg J Möhrle; Claude Oeuvray; Timothy N C Wells
Journal:  Malar J       Date:  2013-06-06       Impact factor: 2.979

Review 10.  New drugs to treat multidrug-resistant tuberculosis: the case for bedaquiline.

Authors:  Eric Leibert; Mauricio Danckers; William N Rom
Journal:  Ther Clin Risk Manag       Date:  2014-07-29       Impact factor: 2.423

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  142 in total

1.  Tetrahydrophthalazinone Inhibitor of Phosphodiesterase with In Vitro Activity against Intracellular Trypanosomatids.

Authors:  Julianna Siciliano de Araújo; Raiza Brandão Peres; Patrícia Bernardino da Silva; Marcos Meuser Batista; Geert Jan Sterk; Louis Maes; Guy Caljon; Rob Leurs; Harry P de Koning; Titilola D Kalejaiye; Maria de Nazaré Correia Soeiro
Journal:  Antimicrob Agents Chemother       Date:  2021-02-17       Impact factor: 5.191

Review 2.  New antituberculous drugs derived from natural products: current perspectives and issues in antituberculous drug development.

Authors:  Masayuki Igarashi; Yoshimasa Ishizaki; Yoshiaki Takahashi
Journal:  J Antibiot (Tokyo)       Date:  2017-11-01       Impact factor: 2.649

Review 3.  Chemical probes and drug leads from advances in synthetic planning and methodology.

Authors:  Christopher J Gerry; Stuart L Schreiber
Journal:  Nat Rev Drug Discov       Date:  2018-04-13       Impact factor: 84.694

4.  A Novel Fluorescence Resonance Energy Transfer-Based Screen in High-Throughput Format To Identify Inhibitors of Malarial and Human Glucose Transporters.

Authors:  Thomas E Kraft; Monique R Heitmeier; Marina Putanko; Rachel L Edwards; Ma Xenia G Ilagan; Maria A Payne; Joseph M Autry; David D Thomas; Audrey R Odom; Paul W Hruz
Journal:  Antimicrob Agents Chemother       Date:  2016-11-21       Impact factor: 5.191

Review 5.  Phenotypic Screens in Antimalarial Drug Discovery.

Authors:  Marisa L Hovlid; Elizabeth A Winzeler
Journal:  Trends Parasitol       Date:  2016-05-27

6.  Octopus: a platform for the virtual high-throughput screening of a pool of compounds against a set of molecular targets.

Authors:  Eduardo Habib Bechelane Maia; Vinícius Alves Campos; Bianca Dos Reis Santos; Marina Santos Costa; Iann Gabriel Lima; Sandro J Greco; Rosy I M A Ribeiro; Felipe M Munayer; Alisson Marques da Silva; Alex Gutterres Taranto
Journal:  J Mol Model       Date:  2017-01-07       Impact factor: 1.810

7.  8-Aryl-6-chloro-3-nitro-2-(phenylsulfonylmethyl)imidazo[1,2-a]pyridines as potent antitrypanosomatid molecules bioactivated by type 1 nitroreductases.

Authors:  Cyril Fersing; Clotilde Boudot; Julien Pedron; Sébastien Hutter; Nicolas Primas; Caroline Castera-Ducros; Sandra Bourgeade-Delmas; Alix Sournia-Saquet; Alain Moreau; Anita Cohen; Jean-Luc Stigliani; Geneviève Pratviel; Maxime D Crozet; Susan Wyllie; Alan Fairlamb; Alexis Valentin; Pascal Rathelot; Nadine Azas; Bertrand Courtioux; Pierre Verhaeghe; Patrice Vanelle
Journal:  Eur J Med Chem       Date:  2018-08-01       Impact factor: 6.514

8.  Open Lab as a source of hits and leads against tuberculosis, malaria and kinetoplastid diseases.

Authors:  Lluís Ballell; Mike Strange; Nicholas Cammack; Alan H Fairlamb; Leszek Borysiewicz
Journal:  Nat Rev Drug Discov       Date:  2016-03-29       Impact factor: 84.694

9.  Effect of Itraconazole-Ezetimibe-Miltefosine Ternary Therapy in Murine Visceral Leishmaniasis.

Authors:  Valter V Andrade-Neto; Karina M Rebello; Thais M Pereira; Eduardo Caio Torres-Santos
Journal:  Antimicrob Agents Chemother       Date:  2021-02-22       Impact factor: 5.191

10.  Identification via a Parallel Hit Progression Strategy of Improved Small Molecule Inhibitors of the Malaria Purine Uptake Transporter that Inhibit Plasmodium falciparum Parasite Proliferation.

Authors:  Yvett Sosa; Roman Deniskin; I J Frame; Matthew S Steiginga; Deepak Bandyopadhyay; Todd L Graybill; Lorena A Kallal; Michael T Ouellette; Andrew J Pope; Katherine L Widdowson; Robert J Young; Myles H Akabas
Journal:  ACS Infect Dis       Date:  2019-08-14       Impact factor: 5.084

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