Cover image for Vol. 12 Issue 22

Editorial Board Chairs: Karl-Heinz Altmann, Antonello Mai, Rainer Metternich. Editor: David Peralta

Impact Factor: 3.225

ISI Journal Citation Reports © Ranking: 2016: 17/60 (Chemistry Medicinal); 73/257 (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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November 14, 2017

VIP: Substrate-Analog Furin Inhibitors

VIP: Substrate-Analog Furin InhibitorsTeodora Ivanova, Kornelia Hardes, Stephanie Kallis, Sven O. Dahms, Manuel E. Than, Sebastian Künzel, Eva Böttcher-Friebertshäuser, Iris Lindberg, Guan-Sheng Jiao, Ralf Bartenschlager, Torsten Steinmetzer

The serine protease furin carries out important physiological functions in the processing of vital protein precursors, but it also contributes to numerous diseases and has emerged as a potential host target, especially for the short-term treatment of acute furin-dependent viral infections.

The strongest furin inhibitor known so far is the tetrabasic substrate-analogue structure MI-1148 (4-guanidinomethyl-phenylacetyl-Arg-tert-Leu-Arg-4-amidinobenzylamide). Read more...

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    Dulce C. Guzmán-Ocampo, Rodrigo Aguayo-Ortiz, Lucia Cano-González, Prof. Dr. Rafael Castillo, Prof. Dr. Alicia Hernández-Campos and Prof. Dr. Laura Dominguez

    Version of Record online: 23 NOV 2017 | DOI: 10.1002/cmdc.201700530

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    NZ–β-tubulin complex: Nocodazole (NZ) inhibits microtubule polymerization by binding to the β-tubulin subunit. In this study we evaluated the effect of the protonated states of titratable residues and structural water molecules in the binding mode of NZ, using different computational approaches. Our results suggest that the protonated state of E198 and the water molecule located between G235 and C239 are key structural features for the binding of NZ to β-tubulin.

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    Version of Record online: 23 NOV 2017 | DOI: 10.1002/cmdc.201700451

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