title: Enoyl acyl carrier protein reductase inhibitors: a patent review (2006 - 2010).
abstract: BACKGROUND
  Bacterial enoyl acyl carrier protein reductase (ENR) specificity reduces the double bond in enoyl thioester substrates in the final enzymatic step of the elongation cycle of the fatty acid synthase-II pathway. Its function is essential for bacterial organism survival, making it an attractive target for the development of novel antibiotics. The structural features and therapeutic potential of this enzyme have stimulated the rational design of ENR inhibitors, and important progress has been achieved to date.
  
  
  METHODS
  This review describes recent advances made in the search for ENR inhibitors, as reflected by patent applications filed from 2006 to 2010, together with an overview of the relevant literature. The first section of this paper provides a background of the biology of ENR, followed by a description of its structure and function. The main section describes the substrate specificities for ENR, and the structure-based rational design of patent inhibitors originating from different companies and academic groups.
  
  
  CONCLUSIONS
  The increase in the number of ENR inhibitors bodes well for the development of new therapeutics against multidrug-resistant bacteria. The challenge is now to improve the pharmacokinetic parameters of these inhibitors and translate them into clinical studies.
authors.affiliation: Guangzhou Institutes of Biomedicine and Health, Key Laboratory of Regenerative Biology and Institute of Chemical Biology, Chinese Academy of Sciences, No. 190, Kaiyuan Avenue, Science Park, Guangzhou, 510530, China.
authors.forename: Xiaoyun
authors.initials: X
authors.lastname: Lu
authors.forename: Kun
authors.initials: K
authors.lastname: Huang
authors.forename: Qidong
authors.initials: Q
authors.lastname: You
mesh_terms: D000900:Anti-Bacterial Agents / Q000494:pharmacology*; D001424:Bacterial Infections / Q000188:drug therapy / Q000201:enzymology; D016503:Drug Delivery Systems; D015195:Drug Design; D024901:Drug Resistance, Multiple, Bacterial; D050753:Enoyl-(Acyl-Carrier-Protein) Reductase (NADH) / Q000037:antagonists & inhibitors* / Q000378:metabolism; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D006801:Humans; D010330:Patents as Topic; D011485:Protein Binding; D013379:Substrate Specificity
chemical_list: D000900:Anti-Bacterial Agents; D004791:Enzyme Inhibitors; D050753:Enoyl-(Acyl-Carrier-Protein) Reductase (NADH)