Literature DB >> 15837314

Discovery and optimisation of potent, selective, ethanolamine inhibitors of bacterial phenylalanyl tRNA synthetase.

Richard L Jarvest1, Symon G Erskine, Andrew K Forrest, Andrew P Fosberry, Martin J Hibbs, Joanna J Jones, Peter J O'Hanlon, Robert J Sheppard, Angela Worby.   

Abstract

High throughput screening of Staphylococcus aureus phenylalanyl tRNA synthetase (FRS) identified ethanolamine 1 as a sub-micromolar hit. Optimisation studies led to the enantiospecific lead 64, a single-figure nanomolar inhibitor. The inhibitor series shows selectivity with respect to the mammalian enzyme and the potential for broad spectrum bacterial FRS inhibition.

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Year:  2005        PMID: 15837314     DOI: 10.1016/j.bmcl.2005.03.003

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  7 in total

1.  IA, database of known ligands of aminoacyl-tRNA synthetases.

Authors:  Mieczyslaw Torchala; Marcin Hoffmann
Journal:  J Comput Aided Mol Des       Date:  2007-09-20       Impact factor: 3.686

2.  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

3.  Discovering new classes of Brugia malayi asparaginyl-tRNA synthetase inhibitors and relating specificity to conformational change.

Authors:  Sai Chetan K Sukuru; Thibaut Crepin; Youli Milev; Liesl C Marsh; Jonathan B Hill; Regan J Anderson; Jonathan C Morris; Anjali Rohatgi; Gavin O'Mahony; Morten Grøtli; Franck Danel; Malcolm G P Page; Michael Härtlein; Stephen Cusack; Michael A Kron; Leslie A Kuhn
Journal:  J Comput Aided Mol Des       Date:  2006-04-28       Impact factor: 3.686

4.  High Throughput Screen Identifies Natural Product Inhibitor of Phenylalanyl-tRNA Synthetase from Pseudomonas aeruginosa and Streptococcus pneumoniae.

Authors:  Yanmei Hu; Stephanie O Palmer; Hector Munoz; James M Bullard
Journal:  Curr Drug Discov Technol       Date:  2014

5.  The role of a novel auxiliary pocket in bacterial phenylalanyl-tRNA synthetase druggability.

Authors:  Ayome Abibi; Andrew D Ferguson; Paul R Fleming; Ning Gao; Laurel I Hajec; Jun Hu; Valerie A Laganas; David C McKinney; Sarah M McLeod; D Bryan Prince; Adam B Shapiro; Ed T Buurman
Journal:  J Biol Chem       Date:  2014-06-16       Impact factor: 5.157

6.  3-(2-Formyl-phen-oxy)propanoic acid.

Authors:  Alain Collas; Christophe M L Vande Velde; Frank Blockhuys
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2010-09-30

7.  Phenylalanyl tRNA synthetase (PheRS) substrate mimics: design, synthesis, molecular dynamics and antimicrobial evaluation.

Authors:  Nada A Noureldin; Jennifer Richards; Hend Kothayer; Mohammed M Baraka; Sobhy M Eladl; Mandy Wootton; Claire Simons
Journal:  RSC Adv       Date:  2022-01-20       Impact factor: 3.361

  7 in total

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