Literature DB >> 33139282

Lack of Specificity of Phenotypic Screens for Inhibitors of the Mycobacterium tuberculosis FAS-II System.

Anna E Grzegorzewicz1,2, Joël Lelièvre3, Jorge Esquivias3, Bhanupriya Angala1, Jiuyu Liu4, Richard E Lee4, Michael R McNeil1, Mary Jackson5.   

Abstract

Phenotypic screening of inhibitors of the essential Mycobacterium tuberculosis FAS-II dehydratase HadAB led to the identification of GSK3011724A, a compound previously reported to inhibit the condensation step of FAS-II. Whole-cell-based and cell-free assays confirmed the lack of activity of GSK3011724A against the dehydratase despite evidence of cross-resistance between GSK3011724A and HadAB inhibitors. The nature of the resistance mechanisms is suggestive of alterations in the FAS-II interactome reducing access of GSK3011724A to KasA.
Copyright © 2020 American Society for Microbiology.

Entities:  

Keywords:  (3R)-hydroxyacyl-ACP dehydratase; FAS-II; Mycobacteriumzzm321990; drug development; mycolic acids; phenotypic screening; tuberculosis; β-ketoacyl synthase

Year:  2020        PMID： 33139282      PMCID： PMC7927822          DOI： 10.1128/AAC.01914-20

Source DB:  PubMed          Journal:  Antimicrob Agents Chemother        ISSN： 0066-4804            Impact factor:   5.191


  20 in total

1.  Thiolactomycin and related analogues as novel anti-mycobacterial agents targeting KasA and KasB condensing enzymes in Mycobacterium tuberculosis.

Authors:  L Kremer; J D Douglas; A R Baulard; C Morehouse; M R Guy; D Alland; L G Dover; J H Lakey; W R Jacobs; P J Brennan; D E Minnikin; G S Besra
Journal:  J Biol Chem       Date:  2000-06-02       Impact factor: 5.157

2.  Mechanisms of Resistance Associated with the Inhibition of the Dehydration Step of Type II Fatty Acid Synthase in Mycobacterium tuberculosis.

Authors:  Anna E Grzegorzewicz; Clifford Gee; Sourav Das; Jiuyu Liu; Juan Manuel Belardinelli; Victoria Jones; Michael R McNeil; Richard E Lee; Mary Jackson
Journal:  ACS Infect Dis       Date:  2019-12-11       Impact factor: 5.084

3.  Effects of ethionamide and isoxyl on mycolic acid synthesis in Mycobacterium tuberculosis BCG.

Authors:  F G Winder; P B Collins; D Whelan
Journal:  J Gen Microbiol       Date:  1971-06

4.  Protein-protein interactions within the Fatty Acid Synthase-II system of Mycobacterium tuberculosis are essential for mycobacterial viability.

Authors:  Romain Veyron-Churlet; Olivier Guerrini; Lionel Mourey; Mamadou Daffé; Didier Zerbib
Journal:  Mol Microbiol       Date:  2004-12       Impact factor: 3.501

5.  The missing piece of the type II fatty acid synthase system from Mycobacterium tuberculosis.

Authors:  Emmanuelle Sacco; Adrian Suarez Covarrubias; Helen M O'Hare; Paul Carroll; Nathalie Eynard; T Alwyn Jones; Tanya Parish; Mamadou Daffé; Kristina Bäckbro; Annaïk Quémard
Journal:  Proc Natl Acad Sci U S A       Date:  2007-09-05       Impact factor: 11.205

Review 6.  New approaches to target the mycolic acid biosynthesis pathway for the development of tuberculosis therapeutics.

Authors:  E Jeffrey North; Mary Jackson; Richard E Lee
Journal:  Curr Pharm Des       Date:  2014       Impact factor: 3.116

7.  Synergistic Lethality of a Binary Inhibitor of Mycobacterium tuberculosis KasA.

Authors:  Pradeep Kumar; Glenn C Capodagli; Divya Awasthi; Matthew B Neiditch; Joel S Freundlich; David Alland; Riju Shrestha; Karishma Maharaja; Paridhi Sukheja; Shao-Gang Li; Daigo Inoyama; Matthew Zimmerman; Hsin Pin Ho Liang; Jansy Sarathy; Marizel Mina; George Rasic; Riccardo Russo; Alexander L Perryman; Todd Richmann; Aditi Gupta; Eric Singleton; Sheetal Verma; Seema Husain; Patricia Soteropoulos; Zhe Wang; Roxanne Morris; Gene Porter; Gautam Agnihotri; Padmini Salgame; Sean Ekins; Kyu Y Rhee; Nancy Connell; Véronique Dartois
Journal:  mBio       Date:  2018-12-18       Impact factor: 7.867

8.  Synthesis, antitubercular activity and mechanism of resistance of highly effective thiacetazone analogues.

Authors:  Geoffrey D Coxon; Derek Craig; Rosa Milagros Corrales; Emilie Vialla; Laila Gannoun-Zaki; Laurent Kremer
Journal:  PLoS One       Date:  2013-01-03       Impact factor: 3.240

9.  Fueling open-source drug discovery: 177 small-molecule leads against tuberculosis.

Authors:  Lluís Ballell; Robert H Bates; Rob J Young; Daniel Alvarez-Gomez; Emilio Alvarez-Ruiz; Vanessa Barroso; Delia Blanco; Benigno Crespo; Jaime Escribano; Rubén González; Sonia Lozano; Sophie Huss; Angel Santos-Villarejo; José Julio Martín-Plaza; Alfonso Mendoza; María José Rebollo-Lopez; Modesto Remuiñan-Blanco; José Luis Lavandera; Esther Pérez-Herran; Francisco Javier Gamo-Benito; José Francisco García-Bustos; David Barros; Julia P Castro; Nicholas Cammack
Journal:  ChemMedChem       Date:  2013-01-10       Impact factor: 3.466

10.  Release of 50 new, drug-like compounds and their computational target predictions for open source anti-tubercular drug discovery.

Authors:  María Jose Rebollo-Lopez; Joël Lelièvre; Daniel Alvarez-Gomez; Julia Castro-Pichel; Francisco Martínez-Jiménez; George Papadatos; Vinod Kumar; Gonzalo Colmenarejo; Grace Mugumbate; Mark Hurle; Vanessa Barroso; Rob J Young; María Martinez-Hoyos; Rubén González del Río; Robert H Bates; Eva Maria Lopez-Roman; Alfonso Mendoza-Losana; James R Brown; Emilio Alvarez-Ruiz; Marc A Marti-Renom; John P Overington; Nicholas Cammack; Lluís Ballell; David Barros-Aguire
Journal:  PLoS One       Date:  2015-12-07       Impact factor: 3.240
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  1 in total

1.  Results from a large cross-sectional study assessing Chlamydia trachomatis, Ureaplasma spp. and Mycoplasma hominis urogenital infections in patients with primary infertility.

Authors:  Daniela Andrea Paira; Guillermo Molina; Andrea Daniela Tissera; Carolina Olivera; Rosa Isabel Molina; Ruben Dario Motrich
Journal:  Sci Rep       Date:  2021-07-01       Impact factor: 4.379
  1 in total

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