Literature DB >> 23985066

Screening strategies to identify new chemical diversity for drug development to treat kinetoplastid infections.

Rob Don1, Jean-Robert Ioset1.   

Abstract

The Drugs for Neglected Diseases initiative (DNDi) has defined and implemented an early discovery strategy over the last few years, in fitting with its virtual R&D business model. This strategy relies on a medium- to high-throughput phenotypic assay platform to expedite the screening of compound libraries accessed through its collaborations with partners from the pharmaceutical industry. We review the pragmatic approaches used to select compound libraries for screening against kinetoplastids, taking into account screening capacity. The advantages, limitations and current achievements in identifying new quality series for further development into preclinical candidates are critically discussed, together with attractive new approaches currently under investigation.

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Year:  2013        PMID: 23985066     DOI: 10.1017/S003118201300142X

Source DB:  PubMed          Journal:  Parasitology        ISSN: 0031-1820            Impact factor:   3.234


  45 in total

1.  Untargeted LC-MS metabolomic studies of Asteraceae species to discover inhibitors of Leishmania major dihydroorotate dehydrogenase.

Authors:  Lucas A Chibli; Annylory L Rosa; Maria Cristina Nonato; Fernando B Da Costa
Journal:  Metabolomics       Date:  2019-04-04       Impact factor: 4.290

Review 2.  Experimental models in Chagas disease: a review of the methodologies applied for screening compounds against Trypanosoma cruzi.

Authors:  Cristina Fonseca-Berzal; Vicente J Arán; José A Escario; Alicia Gómez-Barrio
Journal:  Parasitol Res       Date:  2018-09-19       Impact factor: 2.289

3.  Drug target identification using a trypanosome overexpression library.

Authors:  Daniela Begolo; Esteban Erben; Christine Clayton
Journal:  Antimicrob Agents Chemother       Date:  2014-07-21       Impact factor: 5.191

4.  In Vitro and In Vivo Studies of the Trypanocidal Effect of Novel Quinolines.

Authors:  A S G Nefertiti; M M Batista; P B Da Silva; D G J Batista; C F Da Silva; R B Peres; E C Torres-Santos; E F Cunha-Junior; E Holt; D W Boykin; R Brun; T Wenzler; M N C Soeiro
Journal:  Antimicrob Agents Chemother       Date:  2018-01-25       Impact factor: 5.191

Review 5.  Hit and lead criteria in drug discovery for infectious diseases of the developing world.

Authors:  Kei Katsuno; Jeremy N Burrows; Ken Duncan; Rob Hooft van Huijsduijnen; Takushi Kaneko; Kiyoshi Kita; Charles E Mowbray; Dennis Schmatz; Peter Warner; B T Slingsby
Journal:  Nat Rev Drug Discov       Date:  2015-10-05       Impact factor: 84.694

6.  Assembling Pharma Resources to Tackle Diseases of Underserved Populations.

Authors:  Dale J Kempf; Kennan C Marsh
Journal:  ACS Med Chem Lett       Date:  2020-03-27       Impact factor: 4.345

7.  Repurposing Strategy of Atorvastatin against Trypanosoma cruzi: In Vitro Monotherapy and Combined Therapy with Benznidazole Exhibit Synergistic Trypanocidal Activity.

Authors:  C F Araujo-Lima; R B Peres; P B Silva; M M Batista; C A F Aiub; I Felzenszwalb; M N C Soeiro
Journal:  Antimicrob Agents Chemother       Date:  2018-08-27       Impact factor: 5.191

8.  A Replicative In Vitro Assay for Drug Discovery against Leishmania donovani.

Authors:  Diana Tegazzini; Rosario Díaz; Fernando Aguilar; Imanol Peña; Jesús L Presa; Vanessa Yardley; Julio J Martin; Jose M Coteron; Simon L Croft; Juan Cantizani
Journal:  Antimicrob Agents Chemother       Date:  2016-05-23       Impact factor: 5.191

9.  Antitrypanosomal and antileishmanial activity of prenyl-1,2,3-triazoles.

Authors:  Exequiel O J Porta; Sebastián N Jäger; Isabel Nocito; Galina I Lepesheva; Esteban C Serra; Babu L Tekwani; Guillermo R Labadie
Journal:  Medchemcomm       Date:  2017-03-10       Impact factor: 3.597

10.  Identification and Characterization of FTY720 for the Treatment of Human African Trypanosomiasis.

Authors:  Amy J Jones; Marcel Kaiser; Vicky M Avery
Journal:  Antimicrob Agents Chemother       Date:  2015-12-14       Impact factor: 5.191

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