Cover image for Vol. 10 Issue 12

Editor-in-Chief: Natalia Ortúzar

Impact Factor: 2.968

ISI Journal Citation Reports © Ranking: 2014: 19/59 (Chemistry Medicinal); 83/255 (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

Recently Published Issues

See all

Latest News

Browse more news


Follow ChemMedChem on Twitter

November 24, 2015

Editor's Picks: Issue 12/2015

Editor's Picks: Issue 12/2015The Editor's picks for issue 12 report studies that address aberrant lipid metabolism. The Full Paper by Overkleeft, Aerts, and colleagues is focused on three enzymes involved in the metabolism of glucosylceramide, while another Full Paper by Tacke and co-workers discusses silicon-containing agonists of receptors that mediate antilipolytic effects. Read more...

Remember, these articles are free to access throughout December! Be sure to sign up for e-mail alerts or follow us on Facebook or Twitter to stay updated with the latest news.

Your Comment...

[Browse more news]

Recently Published Articles

  1. The Lysosomal Protein Saposin B Binds Chloroquine

    Dr. Brian P. Huta, Matthew R. Mehlenbacher, Yan Nie, Xuelei Lai, Dr. Chloe Zubieta, Prof. Fadi Bou-Abdallah and Prof. Robert P. Doyle

    Article first published online: 30 NOV 2015 | DOI: 10.1002/cmdc.201500494

    Thumbnail image of graphical abstract

    Unravelling the mystery of CQ: The full extent of chloroquine (CQ) pharmacology in humans remains unclear. Herein, using isothermal titration calorimetry (ITC) and fluorescence quenching experiments, we demonstrate that the lysosomal protein saposin B (sapB), critical for select lipid degradation, binds CQ with implications for CQ function and toxicity. Additionally, the X-ray crystal structure of sapB–CQ, the first complete crystal structure of sapB with a small-molecule substrate, shows one molecule of CQ bind to the sapB dimer.

  2. Identification of Small-Molecule Inhibitors of the Antiapoptotic Protein Myeloid Cell Leukaemia-1 (Mcl-1)

    Dr. Andrew M. Beekman, Dr. Maria A. O'Connell and Dr. Lesley A. Howell

    Article first published online: 30 NOV 2015 | DOI: 10.1002/cmdc.201500488

    Thumbnail image of graphical abstract

    Breaking up the party: Overexpression of the antiapoptosis Bcl-2 protein family members is commonly observed in cancers, with myeloid cell leukemia-1 (Mcl-1) often being responsible for resistance to radio and chemotherapy. Exploiting the Mcl-1 selective apoptosis regulating protein Noxa, novel small molecules capable of modulating Mcl-1 are identified and evaluated.

  3. Serpin A1 C-Terminal Peptides as Collagen Turnover Modulators

    Simona Pascarella, Dr. Caterina Tiberi, Dr. Giuseppina Sabatino, Dr. Francesca Nuti, Prof. Anna Maria Papini, Prof. Lisa Giovannelli and Prof. Paolo Rovero

    Article first published online: 30 NOV 2015 | DOI: 10.1002/cmdc.201500472

    Thumbnail image of graphical abstract

    Time to heal: A) Synthesis of overlapping peptides of serpin A1 C-terminal portion: SA1-I, SA1-II, SA1-III. B) Biological screening on cultured normal human dermal fibroblasts: dose–response curve for peptide SA1-III. Our data highlight that this decapeptide is a promising lead compound for further development in the search for wound-healing agents to be included in future pharmaceutical formulas.

  4. Design, Synthesis and Evaluation of Triazole-Pyrimidine Analogues as SecA Inhibitors

    Jianmei Cui, Jinshan Jin, Arpana Sagwal Chaudhary, Ying-hsin Hsieh, Hao Zhang, Chaofeng Dai, Krishna Damera, Weixuan Chen, Phang C. Tai and Binghe Wang

    Article first published online: 26 NOV 2015 | DOI: 10.1002/cmdc.201500447

    Thumbnail image of graphical abstract

    One stone, several birds! The SecA inhibitors discovered in this study are broad-spectrum antimicrobials with the intrinsic ability to null the effect of efflux pumps. They are therefore effective against multidrug-resistant bacterial strains, can inhibit virulence factor secretion, and are very active against strains of bacteria that are resistant to antibiotics in current use, including vancomycin.

  5. Inspired by Nature: The 3-Halo-4,5-dihydroisoxazole Moiety as a Novel Molecular Warhead for the Design of Covalent Inhibitors

    Dr. Andrea Pinto, Dr. Lucia Tamborini, Dr. Gregorio Cullia, Prof. Paola Conti and Prof. Carlo De Micheli

    Article first published online: 26 NOV 2015 | DOI: 10.1002/cmdc.201500496

    Thumbnail image of graphical abstract

    A hint from Nature: 3-Halo-4,5-dihydroisoxazole, a component of the naturally occurring antibiotic acivicin, is a powerful warhead for the covalent inhibition of target enzymes. Here, we describe the use of this moiety in medicinal chemistry to develop covalent inhibitors of parasitic and bacterial enzymes, and human targets involved in the modulation of neuronal metabolic pathways or tumor cell metabolism.