Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim
November 21, 2013
Frederick Sanger (1918–2013)
Frederick Sanger, biochemist and two-time Nobel Prize winner, has passed away at the age of 95. His is a household name among researchers in biochemical and biological sciences, for whom 'Sanger sequencing' of DNA has been a staple laboratory procedure for decades, and continues to be, in its myriad modern variations.
Sanger was a pioneer in biomolecular structure elucidation, both for proteins, for which his first Nobel Prize was awarded in 1958 particularly for his work on the structure of insulin, and with nucleic acids, for which his second Nobel Prize came in 1980 for his work in DNA sequencing. He is considered the 'father of genomics'; his research group was the first to sequence the 5-kilobase genome of bacteriophage φX174, and his efforts thus paved the way for determining the genome sequences of a vast range of species.
More about Sanger, who humbly described himself as “just a chap who messed about in a lab”, can be found at the Wellcome Trust Sanger Institute website.
Recently Published Articles
- A Single Subexcitation-Energy Electron Can Induce a Double-Strand Break in DNA Modified by Platinum Chemotherapeutic Drugs
Dr. Mohammad Rezaee, Dr. Elahe Alizadeh, Pierre Cloutier, Prof. Dr. Darel J. Hunting and Prof. Dr. Léon Sanche
Article first published online: 4 DEC 2013 | DOI: 10.1002/cmdc.201300462
Radiosensitization by Pt drugs: Double helix DNA modified by platinum anticancer drugs is highly sensitive to electron resonances, particularly those formed by subexcitation-energy electrons. Only a single, ultra-low-energy electron is required to initiate a series of chemical reactions in the modified DNA, which results in the formation of a double-strand break, that is to say, the most toxic DNA lesion.
- Lactam-Based HDAC Inhibitors for Anticancer Chemotherapy: Restoration of RUNX3 by Posttranslational Modification and Epigenetic Control
Dr. Misun Cho, Dr. Eunhyun Choi, Jae Hyun Kim, Dr. Hwan Kim, Prof. Hwan Mook Kim, Prof. Jang Ik Lee, Prof. Ki-Chul Hwang, Dr. Hyun-Jung Kim and Prof. Gyoonhee Han
Article first published online: 2 DEC 2013 | DOI: 10.1002/cmdc.201300393
Keep it RUNning! Epigenetic and posttranslational stabilization of RUNX3 is regulated by HDACs, leading to cancer suppression. Our γ-lactam-based HDAC inhibitors restored RUNX3 stability by epigenetic and posttranslational regulation. We set selection criteria for identifying potent HDAC inhibitors and found a novel therapeutic agent for gastric cancer.
- Kinetic Properties of Carbohydrate–Lectin Interactions: FimH Antagonists
Dr. Meike Scharenberg, Dr. Xiaohua Jiang, Lijuan Pang, Giulio Navarra, Dr. Said Rabbani, Dr. Florian Binder, Dr. Oliver Schwardt and Prof. Dr. Beat Ernst
Article first published online: 2 DEC 2013 | DOI: 10.1002/cmdc.201300349
Indicators for efficacy: The kinetic properties of carbohydrate–lectin interactions for various FimH antagonists were investigated by surface plasmon resonance. Using the FimH lectin domain in the high-affinity state, surprisingly small dissociation rates were found for the FimH–antagonist complex, resulting in long half-lives in the range of several hours (>3.6 h), which are indictors for high in vivo efficacy.
- The Fight against the Influenza A Virus H1N1: Synthesis, Molecular Modeling, and Biological Evaluation of Benzofurazan Derivatives as Viral RNA Polymerase Inhibitors
Dr. Mafalda Pagano, Dr. Daniele Castagnolo, Dr. Martina Bernardini, Anna Lucia Fallacara, Ilaria Laurenzana, Davide Deodato, Dr. Ulrich Kessler, Dr. Beatrice Pilger, Dr. Lilli Stergiou, Dr. Stephan Strunze, Dr. Cristina Tintori and Prof. Maurizio Botta
Article first published online: 27 NOV 2013 | DOI: 10.1002/cmdc.201300378
In the fight against influenza virus A/WSN/33 (H1N1), the PA–PB1 protein–protein interaction is emerging as a new drug target. To identify small molecules able to inhibit the viral RNA polymerase complex, the benzofurazan scaffold was explored by synthesizing a large library of derivatives. Some compounds showed high anti-H1N1 activity and emerged as effective inhibitors of the PA–PB1 interaction, with IC50 values in the micromolar range.
- Inhibition of Hypoxia-Induced Gene Transcription by Substituted Pyrazolyl Oxadiazoles: Initial Lead Generation and Structure–Activity Relationships
Dr. Michael Härter, Dr. Karl-Heinz Thierauch, Dr. Stephen Boyer, Dr. Ajay Bhargava, Dr. Peter Ellinghaus, Dr. Hartmut Beck, Dr. Susanne Greschat-Schade, Dr. Holger Hess-Stumpp and Dr. Kerstin Unterschemmann
Article first published online: 27 NOV 2013 | DOI: 10.1002/cmdc.201300357
Suppressing HIF target genes: Substituted 5-(1H-pyrazol-3-yl)-1,2,4-oxadiazoles are presented as a novel chemotype to specifically inhibit the hypoxia-induced transcription of target genes of the transcription factor hypoxia-inducible factor (HIF). The new chemotype was derived from 1H-pyrazole-3-carboxamides that had been discovered from a cell-based screen. We present the optimization of the potency and metabolic stability of the initial screening hit.