Cover image for Vol. 12 Issue 18

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); 73/256 (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 23, 2016

13th WCMBC in Steamboat Springs: January 2017

13th WCMBC in Steamboat Springs: January 2017ChemMedChem will be sponsoring the next Winter Conference on Medicinal & Bioorganic Chemistry this coming January 22nd–26th in Steamboat Springs, Colorado. The organizers have lined up another impressive list of presenters for this year's event. And as if excellent cutting-edge science weren't enough, this meeting comes with a healthy dose of play time too: unforgettable skiing in the bright sun and deep snow of northern Colorado. Make sure to register soon!

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Recently Published Articles

  1. Biophysical Screening of a Focused Library for the Discovery of CYP121 Inhibitors as Novel Antimycobacterials

    Dr. Christian Brengel, Dr. Andreas Thomann, Dr. Alexander Schifrin, Dr. Giuseppe Allegretta, Ahmed A. M. Kamal, Dr. Jörg Haupenthal, Isabell Schnorr, Dr. Sang Hyun Cho, Prof. Dr. Scott G. Franzblau, Dr. Martin Empting, Dr. Jens Eberhard and Prof. Dr. Rolf W. Hartmann

    Version of Record online: 26 SEP 2017 | DOI: 10.1002/cmdc.201700363

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    A new anti-TB arsenal: This study describes the discovery of new inhibitors of CYP121 from M. tuberculosis by a systematic screening of a focused P450 inhibitor library combining surface plasmon resonance spectroscopy and a heme coordination assay. Further biological characterizations and mode-of-action studies resulted in a frontrunner compound with superior antimycobacterial efficacy and a decreased toxicity profile relative to the reference compound econazole.

  2. WNK Signaling Inhibitors as Potential Antihypertensive Drugs

    Mubarak A. AlAmri, Dr. Hachemi Kadri, Binar A. Dhiani, Shumail Mahmood, Abdulrahman Elzwawi and Dr. Youcef Mehellou

    Version of Record online: 26 SEP 2017 | DOI: 10.1002/cmdc.201700425

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    Various components of the WNK signaling cascade have been validated in vivo as viable targets for antihypertensive drugs. A selection of kinase and protein–protein interaction inhibitors, which have shown great promise in lowering blood pressure in vivo, have been reported. Herein we provide insight into the discovery the various reported WNK signaling inhibitors and offer an outlook into the future of targeting the WNK signaling pathway.

  3. A Selective Biligand Inhibitor of CK2 Increases Caspase-3 Activity in Cancer Cells and Inhibits Platelet Aggregation

    Hedi Rahnel, Dr. Kaido Viht, Dr. Darja Lavogina, Dr. Olga Mazina, Tõiv Haljasorg, Dr. Erki Enkvist and Dr. Asko Uri

    Version of Record online: 26 SEP 2017 | DOI: 10.1002/cmdc.201700457

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    True multitasking: Biligand inhibitors that may be developed into drug candidates or applied to study signaling pathways regulated by CK2 were constructed. Per-esterification of inhibitor ARC-772 [shown, Kd(CK2)=0.3 nm] supported intracellular uptake [shown, c (in cells)=100 μm]. Relative to CX-4945 (currently in clinical trials), ARC-772 revealed higher cellular efficiency.

  4. (R-X-R)4-motif peptides containing conformationally constrained cyclohexane-derived spacers: Effect on cellular uptake

    Govind S Bhosle and Moneesha Fernandes

    Accepted manuscript online: 26 SEP 2017 01:20AM EST | DOI: 10.1002/cmdc.201700498

  5. DNA microcapsule for photo-triggered drug release system

    Yukiko Kamiya, Yoshinobu Yamada, Takahiro Muro, Kazunori Matsuura and Hiroyuki Asanuma

    Accepted manuscript online: 25 SEP 2017 10:21PM EST | DOI: 10.1002/cmdc.201700512