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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
Recently Published Issues
August 25, 2016
VIP: BAY-876: The First Highly Selective GLUT1 Inhibitor
Authors: 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...
Recently Published Articles
- Development of Dipeptidic hGPR54 Agonists
Dr. Christelle Doebelin, Isabelle Bertin, Séverine Schneider, Dr. Martine Schmitt, Dr. Jean-Jacques Bourguignon, Dr. Caroline Ancel, Dr. Valerie Simonneaux, Dr. Frédéric Simonin and Dr. Frédéric Bihel
Version of Record online: 26 AUG 2016 | DOI: 10.1002/cmdc.201600331
The simpler, the better: By using palladium-catalyzed reactions on supported peptides, we synthesized a series of dipeptides that act as agonists of the human KiSS1-derived peptide receptor (hGPR54). However, we showed that the simple N-benzoylated dipeptide Bz-RW-NH2 is sufficient to induce a significant increase in levels of circulating testosterone when administered to rats at a dose of 10 mg kg−1 (i.p.).
- Immunoproteasome β5i-Selective Dipeptidomimetic Inhibitors
Dr. Pradeep K. Singh, Hao Fan, Xiuju Jiang, Prof. Dr. Lei Shi, Prof. Dr. Carl F. Nathan and Prof. Dr. Gang Lin
Version of Record online: 25 AUG 2016 | DOI: 10.1002/cmdc.201600384
You β, you β, you bet! Class-wide inhibitors of immunoproteasome β5i that are highly selective over constitutive proteasome β5c were serendipitously identified by incorporating β-amino acids into dipeptides. One of these compounds was found to inhibit T cell proliferation. Compounds like these may be used to treat autoimmune and inflammatory diseases with lower mechanism-based cytotoxicity than agents that also inhibit the constitutive proteasome.
- Insights into the in vitro Anticancer Effects of Diruthenium-1
Prof. Dr. habil. Aneta Koceva-Chyła, Dr. Karolina Matczak, Msc. Paweł Hikisz, Msc. Kamil Durka, Msc. Krzysztof Kochel, Prof. Georg Süss-Fink, Dr. Julien Furrer and Dr. habil. Konrad Kowalski
Version of Record online: 25 AUG 2016 | DOI: 10.1002/cmdc.201600315
Ruthless ruthenium! The dinuclear trithiolato-bridged arene ruthenium complex DiRu-1 exhibits nanomolar-level cytotoxicity toward human cancer cells MCF-7 (estrogen-responsive breast adenocarcinoma), MDA-MB-231 (triple-negative breast adenocarcinoma), and HepG2 (hepatocellular carcinoma). MCF-7 cells are the most responsive to DiRu-1 (IC50=77.2±1.4 nm). DiRu-1 triggers apoptosis, necrosis, mitotic catastrophe, and autophagy of MCF-7 cells, increases the levels of reactive oxygen species, and induces DNA lesions. It also arrests the MCF-7 cell cycle at the G2/M checkpoint.
- Development of Potent and Metabolically Stable APJ Ligands with High Therapeutic Potential
Dr. Cathleen Juhl, Dr. Sylvia Els-Heindl, Ria Schönauer, Dr. Gorden Redlich, Dr. Erik Haaf, Dr. Frank Wunder, Prof. Dr. Bernd Riedl, Dr. Nils Burkhardt, Prof. Dr. Annette G. Beck-Sickinger and Dr. Donald Bierer
Version of Record online: 25 AUG 2016 | DOI: 10.1002/cmdc.201600307
Tough as nails: The shortest known endogenous apelin receptor ligand was modified by unnatural amino acids, cyclization, and palmitoylation to increase the metabolic stability. In vitro and in vivo stability tests revealed Palm-QRPRLSHKGP-Nle-Aib-F as a very active and stable apelin analogue.
- Flavonoids and Naphthoflavonoids: Wider Roles in the Modulation of Cytochrome P450 Family 1 Enzymes
Jinyun Dong, Qijing Zhang, Qing Cui, Guang Huang, Dr. Xiaoyan Pan and Prof. Shaoshun Li
Version of Record online: 23 AUG 2016 | DOI: 10.1002/cmdc.201600316
Cytochrome P450 family 1 enzymes (CYP1s) are implicated in carcinogenesis and drug resistance. Some natural and synthetic flavonoids and naphthoflavonoids have been documented to exert pronounced effects in the modulation of CYP1s, including roles as inhibitors, substrates, and aryl hydrocarbon receptor (AhR) ligands. Understanding the relationship between CYP1s and the structures of these compounds will significantly aid efforts in anticancer drug discovery.