Literature DB >> 18394721

Drugging the Plasmodium kinome: the benefits of academia-industry synergy.

Didier Leroy1, Christian Doerig.   

Abstract

Malaria remains a major killer in many parts of the world. Recently, the development of nonprofit organisations aimed at fighting this deadly scourge incited academic and industrial scientists to merge their expertise in drug-target validation and lead discovery. Expectations are clear: identification and characterisation of new molecules showing high efficacy, low toxicity and little propensity to induce resistance in the parasite. In this context, protein kinase inhibitors represent an attractive possibility. Here, we compare traditional target-based drug-discovery approaches with innovative exploratory paths (parallel screening, cell-based assays, integrated systems biology and allosteric inhibition) and discuss the benefits of acadaemia-industry cooperation. Early characterisation of distribution, metabolism, pharmacokinetic (DMPK) and toxicology parameters are considered as well.

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Year:  2008        PMID: 18394721     DOI: 10.1016/j.tips.2008.02.005

Source DB:  PubMed          Journal:  Trends Pharmacol Sci        ISSN: 0165-6147            Impact factor:   14.819


  10 in total

1.  Thousands of chemical starting points for antimalarial lead identification.

Authors:  Francisco-Javier Gamo; Laura M Sanz; Jaume Vidal; Cristina de Cozar; Emilio Alvarez; Jose-Luis Lavandera; Dana E Vanderwall; Darren V S Green; Vinod Kumar; Samiul Hasan; James R Brown; Catherine E Peishoff; Lon R Cardon; Jose F Garcia-Bustos
Journal:  Nature       Date:  2010-05-20       Impact factor: 49.962

2.  A Divergent SAR Study Allows Optimization of a Potent 5-HT2c Inhibitor to a Promising Antimalarial Scaffold.

Authors:  Félix Calderón; Jaume Vidal-Mas; Jeremy Burrows; Juan Carlos de la Rosa; María Belén Jiménez-Díaz; Teresa Mulet; Sara Prats; Jorge Solana; Michael Witty; Francisco Javier Gamo; Esther Fernández
Journal:  ACS Med Chem Lett       Date:  2012-02-09       Impact factor: 4.345

3.  An Invitation to Open Innovation in Malaria Drug Discovery: 47 Quality Starting Points from the TCAMS.

Authors:  Félix Calderón; David Barros; José María Bueno; José Miguel Coterón; Esther Fernández; Francisco Javier Gamo; José Luís Lavandera; María Luisa León; Simon J F Macdonald; Araceli Mallo; Pilar Manzano; Esther Porras; José María Fiandor; Julia Castro
Journal:  ACS Med Chem Lett       Date:  2011-08-03       Impact factor: 4.345

4.  Global kinomic and phospho-proteomic analyses of the human malaria parasite Plasmodium falciparum.

Authors:  Lev Solyakov; Jean Halbert; Mahmood M Alam; Jean-Philippe Semblat; Dominique Dorin-Semblat; Luc Reininger; Andrew R Bottrill; Sharad Mistry; Abdirhaman Abdi; Clare Fennell; Zoe Holland; Claudia Demarta; Yvan Bouza; Audrey Sicard; Marie-Paule Nivez; Sylvain Eschenlauer; Tenzing Lama; Divya Catherine Thomas; Pushkar Sharma; Shruti Agarwal; Selina Kern; Gabriele Pradel; Michele Graciotti; Andrew B Tobin; Christian Doerig
Journal:  Nat Commun       Date:  2011-11-29       Impact factor: 14.919

Review 5.  Exploring the Plasmodium falciparum cyclic-adenosine monophosphate (cAMP)-dependent protein kinase (PfPKA) as a therapeutic target.

Authors:  Nina M Haste; Hana Talabani; Alex Doo; Anais Merckx; Gordon Langsley; Susan S Taylor
Journal:  Microbes Infect       Date:  2012-05-22       Impact factor: 2.700

6.  Phylogenomics of phosphoinositide lipid kinases: perspectives on the evolution of second messenger signaling and drug discovery.

Authors:  James R Brown; Kurt R Auger
Journal:  BMC Evol Biol       Date:  2011-01-05       Impact factor: 3.260

7.  Current developments in the therapy of protozoan infections.

Authors:  Mario Zucca; Dianella Savoia
Journal:  Open Med Chem J       Date:  2011-03-09

8.  A suitable RNA preparation methodology for whole transcriptome shotgun sequencing harvested from Plasmodium vivax-infected patients.

Authors:  Catarina Bourgard; Stefanie C P Lopes; Marcus V G Lacerda; Letusa Albrecht; Fabio T M Costa
Journal:  Sci Rep       Date:  2021-03-03       Impact factor: 4.379

9.  Malaria protein kinase CK2 (PfCK2) shows novel mechanisms of regulation.

Authors:  Michele Graciotti; Mahmood Alam; Lev Solyakov; Ralf Schmid; Glenn Burley; Andrew R Bottrill; Christian Doerig; Paul Cullis; Andrew B Tobin
Journal:  PLoS One       Date:  2014-03-21       Impact factor: 3.240

10.  Asparagine requirement in Plasmodium berghei as a target to prevent malaria transmission and liver infections.

Authors:  Viswanathan A Nagaraj; Dhanunjay Mukhi; Vinayagam Sathishkumar; Pradeep A Subramani; Susanta K Ghosh; Rajeev R Pandey; Manjunatha C Shetty; Govindarajan Padmanaban
Journal:  Nat Commun       Date:  2015-11-04       Impact factor: 14.919

  10 in total

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