Article
Essential but Not Vulnerable: Indazole Sulfonamides Targeting Inosine Monophosphate Dehydrogenase as Potential Leads against Mycobacterium tuberculosis.
ACS infectious diseases - 13 Jan 2017
Park Yumi, Pacitto Angela, Bayliss Tracy, Cleghorn Laura A T, Wang Zhe, Hartman Travis, Arora Kriti, Ioerger Thomas R, Sacchettini Jim, Rizzi Menico, Donini Stefano, Blundell Tom L, Ascher David B, Rhee Kyu, Breda Ardala, Zhou Nian, Dartois Veronique, Jonnala Surendranadha Reddy, Via Laura E, Mizrahi Valerie, Epemolu Ola, Stojanovski Laste, Simeons Fred, Osuna-Cabello Maria, Ellis Lucy, MacKenzie Claire J, Smith Alasdair R C, Davis Susan H, Murugesan Dinakaran, Buchanan Kirsteen I, Turner Penelope A, Huggett Margaret, Zuccotto Fabio, Rebollo-Lopez Maria Jose, Lafuente-Monasterio Maria Jose, Sanz Olalla, Diaz Gracia Santos, Lelièvre Joël, Ballell Lluis, Selenski Carolyn, Axtman Matthew, Ghidelli-Disse Sonja, Pflaumer Hannah, Bösche Markus, Drewes Gerard, Freiberg Gail M, Kurnick Matthew D, Srikumaran Myron, Kempf Dale J, Green Simon R, Ray Peter C, Read Kevin, Wyatt Paul, Barry Clifton E, Boshoff Helena I
Abstract excerpt
A potent, noncytotoxic indazole sulfonamide was identified by high-throughput screening of >100,000 synthetic compounds for activity against Mycobacterium tuberculosis (Mtb). This noncytotoxic compound did not directly inhibit cell wall biogenesis but triggered a slow lysis of Mtb cells as measured by release of intracellular green fluorescent protein (GFP). Isolation of resistant mutants followed by whole-genome...
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