Literature DB >> 17962072

Target assessment for antiparasitic drug discovery.

Julie A Frearson1, Paul G Wyatt, Ian H Gilbert, Alan H Fairlamb.   

Abstract

Drug discovery is a high-risk, expensive and lengthy process taking at least 12 years and costing upwards of US$500 million per drug to reach the clinic. For neglected diseases, the drug discovery process is driven by medical need and guided by pre-defined target product profiles. Assessment and prioritisation of the most promising targets for entry into screening programmes is crucial for maximising the chances of success. Here, we describe criteria used in our drug discovery unit for target assessment and introduce the 'traffic-light' system as a prioritisation and management tool. We hope this brief review will stimulate basic scientists to acquire additional information necessary for drug discovery.

Entities:  

Mesh:

Substances:

Year:  2007        PMID: 17962072      PMCID: PMC2979298          DOI: 10.1016/j.pt.2007.08.019

Source DB:  PubMed          Journal:  Trends Parasitol        ISSN: 1471-4922


  51 in total

1.  A doubly inducible system for RNA interference and rapid RNAi plasmid construction in Trypanosoma brucei.

Authors:  Vincent P Alibu; Lilian Storm; Simon Haile; Christine Clayton; David Horn
Journal:  Mol Biochem Parasitol       Date:  2005-01       Impact factor: 1.759

2.  Structure-based maximal affinity model predicts small-molecule druggability.

Authors:  Alan C Cheng; Ryan G Coleman; Kathleen T Smyth; Qing Cao; Patricia Soulard; Daniel R Caffrey; Anna C Salzberg; Enoch S Huang
Journal:  Nat Biotechnol       Date:  2007-01       Impact factor: 54.908

3.  Designer drugs: pipe-dreams or realities?

Authors:  W E Gutteridge
Journal:  Parasitology       Date:  1997       Impact factor: 3.234

Review 4.  Validating targets for antiparasite chemotherapy.

Authors:  C C Wang
Journal:  Parasitology       Date:  1997       Impact factor: 3.234

Review 5.  Structure-based drug discovery for Plasmodium falciparum.

Authors:  Christopher Mehlin
Journal:  Comb Chem High Throughput Screen       Date:  2005-02       Impact factor: 1.339

6.  A tightly regulated inducible expression system for conditional gene knock-outs and dominant-negative genetics in Trypanosoma brucei.

Authors:  E Wirtz; S Leal; C Ochatt; G A Cross
Journal:  Mol Biochem Parasitol       Date:  1999-03-15       Impact factor: 1.759

7.  A novel mode of Gleevec binding is revealed by the structure of spleen tyrosine kinase.

Authors:  Shane Atwell; Jason M Adams; John Badger; Michelle D Buchanan; Ingeborg K Feil; Karen J Froning; Xia Gao; Jörg Hendle; Kevin Keegan; Barbara C Leon; Hans J Müller-Dieckmann; Vicki L Nienaber; Brian W Noland; Kai Post; K R Rajashankar; Aurora Ramos; Marijane Russell; Stephen K Burley; Sean G Buchanan
Journal:  J Biol Chem       Date:  2004-10-26       Impact factor: 5.157

8.  Procyclic Trypanosoma brucei cell lines deficient in ornithine decarboxylase activity.

Authors:  F Li; S B Hua; C C Wang; K M Gottesdiener
Journal:  Mol Biochem Parasitol       Date:  1996-06       Impact factor: 1.759

9.  Ornithine decarboxylase gene deletion mutants of Leishmania donovani.

Authors:  Y Jiang; S C Roberts; A Jardim; N S Carter; S Shih; M Ariyanayagam; A H Fairlamb; B Ullman
Journal:  J Biol Chem       Date:  1999-02-05       Impact factor: 5.157

10.  Incorporating a rapid-impact package for neglected tropical diseases with programs for HIV/AIDS, tuberculosis, and malaria.

Authors:  Peter J Hotez; David H Molyneux; Alan Fenwick; Eric Ottesen; Sonia Ehrlich Sachs; Jeffrey D Sachs
Journal:  PLoS Med       Date:  2006-01       Impact factor: 11.069

View more
  59 in total

1.  Drug discovery: Fat-free proteins kill parasites.

Authors:  George A M Cross
Journal:  Nature       Date:  2010-04-01       Impact factor: 49.962

2.  Triclosan is minimally effective in rodent malaria models.

Authors:  Werner Baschong; Sergio Wittlin; Kirstine A Inglis; Alan H Fairlamb; Simon L Croft; T R Santha Kumar; David A Fidock; Reto Brun
Journal:  Nat Med       Date:  2011-01       Impact factor: 53.440

3.  The anti-trypanosome drug fexinidazole shows potential for treating visceral leishmaniasis.

Authors:  Susan Wyllie; Stephen Patterson; Laste Stojanovski; Frederick R C Simeons; Suzanne Norval; Robert Kime; Kevin D Read; Alan H Fairlamb
Journal:  Sci Transl Med       Date:  2012-02-01       Impact factor: 17.956

Review 4.  Kinetoplastids: related protozoan pathogens, different diseases.

Authors:  Ken Stuart; Reto Brun; Simon Croft; Alan Fairlamb; Ricardo E Gürtler; Jim McKerrow; Steve Reed; Rick Tarleton
Journal:  J Clin Invest       Date:  2008-04       Impact factor: 14.808

5.  Genetic validation of aminoacyl-tRNA synthetases as drug targets in Trypanosoma brucei.

Authors:  Savitha Kalidas; Igor Cestari; Severine Monnerat; Qiong Li; Sandesh Regmi; Nicholas Hasle; Mehdi Labaied; Marilyn Parsons; Kenneth Stuart; Margaret A Phillips
Journal:  Eukaryot Cell       Date:  2014-02-21

6.  Novel non-peptidic vinylsulfones targeting the S2 and S3 subsites of parasite cysteine proteases.

Authors:  Clifford Bryant; Iain D Kerr; Moumita Debnath; Kenny K H Ang; Joseline Ratnam; Rafaela S Ferreira; Priyadarshini Jaishankar; DongMei Zhao; Michelle R Arkin; James H McKerrow; Linda S Brinen; Adam R Renslo
Journal:  Bioorg Med Chem Lett       Date:  2009-09-03       Impact factor: 2.823

Review 7.  Structure-based ligand design and the promise held for antiprotozoan drug discovery.

Authors:  William N Hunter
Journal:  J Biol Chem       Date:  2008-12-22       Impact factor: 5.157

8.  Chemical validation of trypanothione synthetase: a potential drug target for human trypanosomiasis.

Authors:  Leah S Torrie; Susan Wyllie; Daniel Spinks; Sandra L Oza; Stephen Thompson; Justin R Harrison; Ian H Gilbert; Paul G Wyatt; Alan H Fairlamb; Julie A Frearson
Journal:  J Biol Chem       Date:  2009-10-14       Impact factor: 5.157

9.  A comparative study of methylglyoxal metabolism in trypanosomatids.

Authors:  Neil Greig; Susan Wyllie; Stephen Patterson; Alan H Fairlamb
Journal:  FEBS J       Date:  2008-12-03       Impact factor: 5.542

10.  Development and validation of a cytochrome c-coupled assay for pteridine reductase 1 and dihydrofolate reductase.

Authors:  Emma J Shanks; Han B Ong; David A Robinson; Stephen Thompson; Natasha Sienkiewicz; Alan H Fairlamb; Julie A Frearson
Journal:  Anal Biochem       Date:  2009-09-11       Impact factor: 3.365

View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.