Cover image for Vol. 11 Issue 16

Editorial Board Chairs: Antonello Mai, Rainer Metternich. Assoc. Editors: David Peralta, Scott Williams (Sr)

Impact Factor: 2.98

ISI Journal Citation Reports © Ranking: 2015: 18/59 (Chemistry Medicinal); 76/253 (Pharmacology & Pharmacy)

Online ISSN: 1860-7187

Associated Title(s): Angewandte Chemie International Edition, Chemistry - A European Journal, Chemistry – An Asian Journal, ChemBioChem, Medicinal Research Reviews, Molecular Informatics

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August 25, 2016

VIP: BAY-876: The First Highly Selective GLUT1 Inhibitor

VIP: BAY-876: The First Highly Selective GLUT1 InhibitorAuthors: Holger Siebeneicher, Arwed Cleve, Hartmut Rehwinkel, Roland Neuhaus, Iring Heisler, Thomas Müller, Marcus Bauser, and Bernd Buchmann*

Using a combination of high-throughput screening and structural modification of initial hits, a collaborative research effort at Bayer AG, Drug Discovery, led to quinoline carboxamides as highly potent, reversible, and competitive inhibitors of the glucose transporter GLUT1, with selectivity factors of >100 against GLUT2, GLUT3, and GLUT4. Read more...

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    Version of Record online: 30 AUG 2016 | DOI: 10.1002/cmdc.201600343

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    Against the wall: Bisphosphonates inhibit the growth of Gram-negative bacteria (Acinetobacter baumannii, Klebsiella pneumoniae, Escherichia coli, and Pseudomonas aeruginosa) at ∼1–4 μg mL−1 levels, targeting farnesyl diphosphate synthase, whereas monophosphonates inhibit Gram-positive bacteria (Staphylococcus aureus and Bacillus subtilis) by targeting undecaprenyl diphosphate synthase and undecaprenyl diphosphate phosphatase.

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    Version of Record online: 26 AUG 2016 | DOI: 10.1002/cmdc.201600331

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    Version of Record online: 25 AUG 2016 | DOI: 10.1002/cmdc.201600384

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