Cover image for Vol. 10 Issue 5

Editor-in-Chief: Natalia Ortúzar

Impact Factor: 3.046

ISI Journal Citation Reports © Ranking: 2013: 18/58 (Chemistry Medicinal); 75/256 (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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March 28, 2015

Editor's Picks: Issue 04/2015

Editor's Picks: Issue 04/2015Editor's picks for issue 04: This month, two Full Papers by Markus Pietsch and co-workers and Michael Wiese and colleagues describe various ways to overcome drug resistance in cancer using small-molecule therapeutics. Read more...

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  1. Approaching ‘Kit-Type’ Labelling with 68Ga: The DATA Chelators

    Dr. Johanna Seemann, Dr. Bradley P. Waldron, Prof. Dr. Frank Roesch and Prof. Dr. David Parker

    Article first published online: 21 APR 2015 | DOI: 10.1002/cmdc.201500092

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    Made easier with DATA: The development of kit-type labelling of 68Ga radiopharmaceuticals is a crucial goal that has gathered momentum, with the desire for even simpler radiolabelling protocols and the development of GMP-compliant 68Ge/68Ga generators. The DATA chelators facilitate quantitative complexation of 68Ga at ambient temperature quickly, simply, and efficiently—characteristics that have the potential to make the elusive 68Ga labelling kit a reality.

  2. MS Binding Assays for the Three Monoamine Transporters Using the Triple Reuptake Inhibitor (1R,3S)-Indatraline as Native Marker

    Stefanie H. Grimm, Dr. Georg Höfner and Prof. Dr. Klaus T. Wanner

    Article first published online: 20 APR 2015 | DOI: 10.1002/cmdc.201500084

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    The power of MS Binding Assays! We report an MS-based technique for determining monoamine transporter inhibitor affinities. The investigation of a broad series of known inhibitors in competitive MS Binding Assays demonstrated the reliability, high sample throughput, and robustness of the assays. This MS Binding Assay technique is a powerful substitute for radioligand binding assays addressing hDAT, hNET, and hSERT.

  3. Selective Targeting of the TPX2 Site of Importin-α Using Fragment-Based Ligand Design

    Dr. Rhian S. Holvey, Dr. Eugene Valkov, Prof. David Neal, Dr. Murray Stewart and Prof. Chris Abell

    Article first published online: 20 APR 2015 | DOI: 10.1002/cmdc.201500014

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    Fragments for challenging PPIs: Minor-site-specific compounds were identified and characterised for the TPX2–importin-α protein–protein interaction (PPI), a potential anticancer target. Structure-guided synthesis led to more potent compounds and identified a source of ligand selectivity between the two sites of the importin-α protein.

  4. Protein Flexibility in Drug Discovery: From Theory to Computation

    Dr. Rosa Buonfiglio, Prof. Maurizio Recanatini and Dr. Matteo Masetti

    Article first published online: 17 APR 2015 | DOI: 10.1002/cmdc.201500086

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    Flex and stretch: The mechanisms of biomolecular recognition are strongly coupled to the intrinsic dynamic of proteins. Accounting for protein flexibility in structure-based drug discovery is still a challenging task. This review describes the most important computational methods to model protein flexibility in light of the recent advances in the theories of biomolecular recognition.

  5. 2-Substituted 6-(Het)aryl-7-deazapurine Ribonucleosides: Synthesis, Inhibition of Adenosine Kinases, and Antimycobacterial Activity

    Dr. Vincent Malnuit, Dr. Lenka Poštová Slavětínská, Dr. Petr Nauš, Dr. Petr Džubák, Prof. Marián Hajdúch, Dr. Jiřina Stolaříková, Dr. Jan Snášel, Dr. Iva Pichová and Prof. Dr. Michal Hocek

    Article first published online: 16 APR 2015 | DOI: 10.1002/cmdc.201500081

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    Specific for Mtb ADK: A series of diverse 2-substituted 6-heteroaryl-7-deazapurine ribonucleosides was prepared and the title compounds were found to be potent and selective inhibitors of Mycobacterium tuberculosis (but not human) adenosine kinase. Unfortunately, their antimycobacterial activity was observed to be weak, probably due to poor uptake or parallel biosynthesis.