Literature DB >> 21384024

Inhibitors of an essential mycobacterial cell wall lipase (Rv3802c) as tuberculosis drug leads.

Nicholas P West1, Katie M Cergol, Millie Xue, Elizabeth J Randall, Warwick J Britton, Richard J Payne.   

Abstract

The first targeted inhibitors of an essential M. tuberculosis cell wall lipase, Rv3802c, are described. Lead compounds exhibited nanomolar inhibition of the enzyme, and encouraging antibacterial activity against M. tuberculosis in vitro, supporting Rv3802c as a novel TB drug target. © The Royal Society of Chemistry 2011

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Year:  2011        PMID: 21384024     DOI: 10.1039/c0cc05635a

Source DB:  PubMed          Journal:  Chem Commun (Camb)        ISSN: 1359-7345            Impact factor:   6.222


  12 in total

1.  Large scale structural rearrangement of a serine hydrolase from Francisella tularensis facilitates catalysis.

Authors:  Ekaterina V Filippova; Leigh A Weston; Misty L Kuhn; Brett Geissler; Alexandra M Gehring; Nicola Armoush; Chinessa T Adkins; George Minasov; Ievgeniia Dubrovska; Ludmilla Shuvalova; James R Winsor; Luke D Lavis; Karla J F Satchell; Daniel P Becker; Wayne F Anderson; R Jeremy Johnson
Journal:  J Biol Chem       Date:  2013-02-19       Impact factor: 5.157

2.  Optimization of cell receptor-specific targeting through multivalent surface decoration of polymeric nanocarriers.

Authors:  Suzanne M D'Addio; Steven Baldassano; Lei Shi; Lila Cheung; Douglas H Adamson; Matthew Bruzek; John E Anthony; Debra L Laskin; Patrick J Sinko; Robert K Prud'homme
Journal:  J Control Release       Date:  2013-02-16       Impact factor: 9.776

3.  Biochemical and microbiological evaluation of N-aryl urea derivatives against mycobacteria and mycobacterial hydrolases.

Authors:  Abhishek Vartak; Christopher Goins; Vinicius Calado Nogueira de Moura; Celine M Schreidah; Alexander D Landgraf; Boren Lin; Jianyang Du; Mary Jackson; Donald R Ronning; Steven J Sucheck
Journal:  Medchemcomm       Date:  2019-06-04       Impact factor: 3.597

4.  Structural Basis for the Strict Substrate Selectivity of the Mycobacterial Hydrolase LipW.

Authors:  Magy G McKary; Jan Abendroth; Thomas E Edwards; R Jeremy Johnson
Journal:  Biochemistry       Date:  2016-12-12       Impact factor: 3.162

5.  Far-red fluorogenic probes for esterase and lipase detection.

Authors:  Katie R Tallman; Kimberly E Beatty
Journal:  Chembiochem       Date:  2014-12-02       Impact factor: 3.164

6.  Synthesis and kinetic evaluation of cyclophostin and cyclipostins phosphonate analogs as selective and potent inhibitors of microbial lipases.

Authors:  Vanessa Point; Raj K Malla; Sadia Diomande; Benjamin P Martin; Vincent Delorme; Frederic Carriere; Stephane Canaan; Nigam P Rath; Christopher D Spilling; Jean-François Cavalier
Journal:  J Med Chem       Date:  2012-11-07       Impact factor: 7.446

7.  Characterization of Tetrahydrolipstatin and Stereoderivatives on the Inhibition of Essential Mycobacterium tuberculosis Lipid Esterases.

Authors:  Christopher M Goins; Thanuja D Sudasinghe; Xiaofan Liu; Yanping Wang; George A O'Doherty; Donald R Ronning
Journal:  Biochemistry       Date:  2018-04-10       Impact factor: 3.162

8.  Structural basis for lipid binding and mechanism of the Mycobacterium tuberculosis Rv3802 phospholipase.

Authors:  Christopher M Goins; Celine M Schreidah; Steven Dajnowicz; Donald R Ronning
Journal:  J Biol Chem       Date:  2017-12-15       Impact factor: 5.157

9.  Measuring the Global Substrate Specificity of Mycobacterial Serine Hydrolases Using a Library of Fluorogenic Ester Substrates.

Authors:  Braden Bassett; Brent Waibel; Alex White; Heather Hansen; Dominique Stephens; Andrew Koelper; Erik M Larsen; Charles Kim; Adam Glanzer; Luke D Lavis; Geoffrey C Hoops; R Jeremy Johnson
Journal:  ACS Infect Dis       Date:  2018-04-16       Impact factor: 5.084

Review 10.  Microbial esterases and ester prodrugs: An unlikely marriage for combating antibiotic resistance.

Authors:  Erik M Larsen; R Jeremy Johnson
Journal:  Drug Dev Res       Date:  2018-10-10       Impact factor: 4.360

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