Copyright © 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim
Editor-in-Chief: Natalia Ortúzar
Impact Factor: 3.046
ISI Journal Citation Reports © Ranking: 2013: 18/58 (Chemistry Medicinal); 74/254 (Pharmacology & Pharmacy)
Online ISSN: 1860-7187
July 05, 2014
Six Outstanding Posters!
Congratulations to the six poster prize winners at last month's Metals in Medicine Gordon Research Conference, Defining the Future of Medicinal Inorganic Chemistry (June 22–27, Andover, NH, USA): Stacy Barnaby (front left, Northwestern University) Probing the Inherent Stability of siRNA Immobilized on Nanoparticle Constructs; Insiya Fidai (front middle, The Ohio State University) Inactivation of Sortase A Mediated by Metal ATCUN Complexes; Steve Po-Yam Li (back left, City University of Hong Kong) Mitochondria-Targeting Cyclometalated Iridium(III) Poly(ethylene glycol) (PEG) Complexes with Tunable Photodynamic Activity; Martin Ross (front right, The Ohio State University) Insights into the Reactivity and Binding of Catalytic Metallodrugs Targeting the IRES RNA of HCV; Kevin Siters (back right, SUNY Buffalo) Targeting the Human Telomeric G-Quadruplex Using Modified ZnII Macrocycles; and Lindsey van Gemeren (back middle, University of Birmingham) Multimodal Imaging Agents for in vivo Cell Tracking.
The poster prizes were sponsored by ChemMedChem and EurJIC; thanks to conference co-chairs Alan B. Packard and Michael J. Hannon, and vice co-chairs Katherine J. Franz and Nils Metzler-Nolte. For more outstanding inorganic medicinal chemistry, see ChemMedChemIssue 06!
Recently Published Articles
- Novel Hinge-Binding Motifs for Janus Kinase 3 Inhibitors: A Comprehensive Structure–Activity Relationship Study on Tofacitinib Bioisosteres
Matthias Gehringer, Michael Forster, Ellen Pfaffenrot, Silke M. Bauer and Prof. Dr. Stefan A. Laufer
Article first published online: 19 AUG 2014 | DOI: 10.1002/cmdc.201402252
JAK of all trades: A library of tofacitinib bioisosteres was prepared and tested against Janus kinases (JAKs). The hinge binding motif in all of the studied compounds was replaced by a variety of heterocycles mimicking the 7H-pyrrolo[2,3-d]pyrimidine pharmacophore. In view of the promising expectations obtained from molecular modeling, most of the compounds proved to be poorly active, yet crucial structure–activity relationships were deduced.
- Ribonuclease A Inhibition by Carboxymethylsulfonyl-Modified Xylo- and Arabinopyrimidines
Dhrubajyoti Datta, Prof. Swagata Dasgupta and Prof. Tanmaya Pathak
Article first published online: 14 AUG 2014 | DOI: 10.1002/cmdc.201402179
Inhibitors that compete! Carboxymethylsulfonyl-modified nucleosides with xylo and arabino configurations were synthesized in order to assess their inhibitory properties against RNase A. Experimental and theoretical studies established the arabinocytidine analogue as the most effective competitive inhibitor due to proper recognition of the B1 and P1 subsites of the enzyme.
- Recent Advances in The Discovery of N-Myristoyltransferase Inhibitors
Can Zhao and Prof. Shutao Ma
Article first published online: 14 AUG 2014 | DOI: 10.1002/cmdc.201402174
A key target: Fungal infections, parasitic diseases, and cancers remain three major global health problems. N-Myristoyltransferase (NMT) has been identified as a novel and promising target for antifungal, antiparasitic, and anticancer agents. This review highlights recent advances in the discovery of NMT inhibitors, with particular focus on their activities, structure–activity relationships, and mechanisms.
- Design and Characterization of a Twin Ribozyme for Potential Repair of a Deletion Mutation within the Oncogenic CTNNB1-ΔS45 mRNA
Darko Balke, Dr. Irene Zieten, Anne Strahl, Prof. Dr. Oliver Müller and Prof. Dr. Sabine Müller
Article first published online: 11 AUG 2014 | DOI: 10.1002/cmdc.201402166
RNA repair kit: The twin ribozyme mediated repair of a three-nucleotide deletion within an oncogenic transcript is investigated. The twin ribozymes are derived from the hairpin ribozyme by tandem duplication and catalyze two cleavage reactions and two ligation events in a strictly controlled fashion. As a result, small patches of the RNA sequence are exchanged.
- Aptamers as Drug Delivery Vehicles
Sven Kruspe, Florian Mittelberger, Kristina Szameit and Prof. Dr. Ulrich Hahn
Article first published online: 11 AUG 2014 | DOI: 10.1002/cmdc.201402163
Selective delivery: Active drug targeting enhances the efficacy and specificity of systemic therapeutics. Aptamers, artificial nucleic acid ligands, represent powerful targeting tools that can act as cell-specific drug carriers. The advancements from the past decade have provided various approaches that open new gateways for drug administration in cancer therapy.