title: Discovery of a 1,2-bis(3-indolyl)ethane that selectively inhibits the pyruvate kinase of methicillin-resistant Staphylococcus aureus over human isoforms.
abstract: Methicillin-resistant Staphylococcus aureus pyruvate kinase (MRSA PK) has recently been identified as a target for development of novel antibacterial agents. Testing a series of 1,2-bis(3-indolyl)ethanes against MRSA PK has led to the discovery of a potent inhibitor that is selective over human isoforms.
authors.affiliation: Division of Infectious Diseases, Department of Medicine, University of British Columbia, Vancouver V5Z 3J5, Canada.
authors.forename: Roya
authors.initials: R
authors.lastname: Zoraghi
authors.affiliation: Centre for Drug Research and Development (CDRD), Vancouver, British Columbia, Canada.
authors.forename: Sara
authors.initials: S
authors.lastname: Campbell
authors.affiliation: Centre for Drug Research and Development (CDRD), Vancouver, British Columbia, Canada.
authors.forename: Catrina
authors.initials: C
authors.lastname: Kim
authors.affiliation: Centre for Drug Research and Development (CDRD), Vancouver, British Columbia, Canada.
authors.forename: Edie M
authors.initials: EM
authors.lastname: Dullaghan
authors.affiliation: School of Chemical Sciences, University of Auckland, 23 Symonds Street, Auckland, New Zealand.
authors.forename: Lachlan M
authors.initials: LM
authors.lastname: Blair
authors.affiliation: School of Chemical Sciences, University of Auckland, 23 Symonds Street, Auckland, New Zealand.
authors.forename: Rachel M
authors.initials: RM
authors.lastname: Gillard
authors.affiliation: Division of Infectious Diseases, Department of Medicine, University of British Columbia, Vancouver V5Z 3J5, Canada; Department of Microbiology and Immunology, University of British Columbia, Vancouver V5Z 3J5, Canada.
authors.forename: Neil E
authors.initials: NE
authors.lastname: Reiner
authors.affiliation: School of Chemical Sciences, University of Auckland, 23 Symonds Street, Auckland, New Zealand.
authors.forename: Jonathan
authors.initials: J
authors.lastname: Sperry
mesh_terms: D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D004353:Drug Evaluation, Preclinical; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D004980:Ethane / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D006801:Humans; D007211:Indoles / Q000737:chemistry; D055624:Methicillin-Resistant Staphylococcus aureus / Q000187:drug effects; D011485:Protein Binding; D020033:Protein Isoforms / Q000037:antagonists & inhibitors / Q000378:metabolism; D011770:Pyruvate Kinase / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D000900:Anti-Bacterial Agents; D004791:Enzyme Inhibitors; D007211:Indoles; D020033:Protein Isoforms; C030374:indole; D011770:Pyruvate Kinase; D004980:Ethane
keywords: Antibacterial; Indole; MRSA; Pyruvate kinase