MEDCHEM NEWS
Online ISSN : 2432-8626
Print ISSN : 2432-8618
ISSN-L : 2432-8618
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Displaying 1-18 of 18 articles from this issue
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  • Activity of the New Modality Research Group in Drug Discovery
    Hitoshi Kuboniwa
    2024 Volume 34 Issue 1 Pages 7-11
    Published: February 01, 2024
    Released on J-STAGE: February 01, 2024
    DOIhttps://doi.org/10.14894/medchem.34.1_7
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    This research group was launched in November 2019 with the mission of “contributing to the world through innovation by promoting Japan’s drug discovery modality research and industry and continuously creating new treatments.”. The three pillars of our activities are: (1) Four subject matter expert working group (smeWG) activities by experts (next generation antibody drugs, nucleic acid drugs, gene and cell therapy, new treatment technologies) (2) Public relations, lectures, and awareness activities (3) Recommendations and practical activities. This paper will explain the activity of this study-group.
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WINDOW
  • Drug Discovery Research at Pfizer
    Kentaro Futatsugi
    2024 Volume 34 Issue 1 Pages 12-16
    Published: February 01, 2024
    Released on J-STAGE: February 01, 2024
    DOIhttps://doi.org/10.14894/medchem.34.1_12
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    “Time is Life” - deliver transformational medicines at lightspeed for patients. With this spirit in mind, I’ve been immersing myself into drug discovery research at Pfizer. This viewpoint will describe my personal view of Pfizer’s evolving drug discovery research organization, molecular design philosophy, and selected influential guiding principles I’ve learned at Pfizer.
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ESSAY
  • Cutting-edge bio-imaging and detection technologies for drug discovery
    Yasuteru Urano
    2024 Volume 34 Issue 1 Pages 17-19
    Published: February 01, 2024
    Released on J-STAGE: February 01, 2024
    DOIhttps://doi.org/10.14894/medchem.34.1_17
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    In drug discovery, it is important to first understand disease factors in the living cells, animals, and patients then discover effective therapeutic targets, and consider how perturbations can be applied to these targets. In addition, for diseases with high unmet medical needs, it is an important issue how to realize personalized and precision medicine. Furthermore, in Japan, which has a universal health insurance system, drug discovery must also take into account the economic sustainability of healthcare. From these perspectives, there are high expectations for drug discovery research centered on the development of small functional molecules and drugs, with live measurement and detection technology of diseases being a central issue. In this special issue, we asked four groups that have achieved remarkable results based on various principles and strategies to comment on their latest achievements.
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  • Bio-imaging with novel activatable Raman probes utilizing aggregate formation
    Hiroyoshi Fujioka, Mako Kamiya
    2024 Volume 34 Issue 1 Pages 20-24
    Published: February 01, 2024
    Released on J-STAGE: February 01, 2024
    DOIhttps://doi.org/10.14894/medchem.34.1_20
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    Raman imaging, which detects molecular vibration, has attracted significant attention as imaging method with higher multiplexability than fluorescence. We have been working on developing activatable Raman probes which can detect target enzyme activities and succeeded to detect plural enzyme activities in live cells. However, these probes could not detect region with target enzyme activities in tissues because of their poor cellular retention. Therefore, we tried to overcome the problem and developed novel activatable Raman probes with improved cellular retention utilizing aggregate formation. The newly developed probes could detect targeted region specifically in Drosophila tissues.
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  • Hyperpolarized MRI molecular probes for investigation of biological phenomena and pathological diagnosis
    Hiroyuki Yatabe, Shinsuke Sando
    2024 Volume 34 Issue 1 Pages 25-29
    Published: February 01, 2024
    Released on J-STAGE: February 01, 2024
    DOIhttps://doi.org/10.14894/medchem.34.1_25
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    Hyperpolarization techniques dramatically improve the sensitivity of nuclear magnetic resonance imaging (NMR/MRI) molecular probes enabling in vivo detection that is typically difficult with conventional NMR/MRI. Dynamic nuclear polarization (DNP) , one of hyperpolarization techniques, has been applied for real-time monitoring of metabolic reactions and pathological diagnosis through metabolic analysis of highly sensitive molecular probes. For example, [1-13C] pyruvate, a representative DNP-NMR molecular probe, has been utilized for pathological diagnosis of various cancers based on its metabolic rate to [1-13C] lactate. However, there are very few practical DNP-NMR molecular probes, and their design guidelines have not been established. We have developed various DNP-NMR molecular probes through precise molecular design. In this manuscript, we introduce examples of DNP-NMR molecular probes with long hyperpolarization lifetimes and fast enzymatic reactions developed based on relaxation theory and mechanistic insight into molecular recognition.
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  • The forefront of Oxidized Lipid Research: From Detection and Structural Analysis to Disease Control
    Ken-ichi Yamada
    2024 Volume 34 Issue 1 Pages 30-35
    Published: February 01, 2024
    Released on J-STAGE: February 01, 2024
    DOIhttps://doi.org/10.14894/medchem.34.1_30
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    Recently, lipid-derived radicals and oxidized lipids have been reported to be closely involved in cell death (especially, ferroptosis) and inflammatory reactions and have attracted much attention. Therefore, inhibitors targeting oxidized lipids, especially lipid-derived radicals important in lipid peroxidation reactions, also called radical-trapping antioxidants (RTAs) , have been actively studied. In this article, we describe the detection and structural analysis techniques for lipid radicals and oxidized lipids and review more recent findings on new compound screening systems for RTA.
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  • Targeting non-canonical nucleic acid structures stabilized under cellular conditions
    Yoshiki Hashimoto, Keiko Kawauchi, Daisuke Miyoshi
    2024 Volume 34 Issue 1 Pages 36-42
    Published: February 01, 2024
    Released on J-STAGE: February 01, 2024
    DOIhttps://doi.org/10.14894/medchem.34.1_36
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    It is well-known that structure and function of biomolecules, involving protein and nucleic acids, depend on the surrounding molecular environment. Noteworthy, a molecular environment inside a cell is totally different from one in test tube, where most of biochemical and biophysical experiments have been conducted. Inside living cells, there are up to 400g/L of biomolecules. These biomolecules occupy up to 40% of the total cell volume, inducing multimolecular crowding biosystem in a cell. Therefore, one should take this multimolecular crowding into account when we study property of biomolecules in a cell. In this article, we introduce molecular environment in a cell. We then show how multimolecular crowding structure and stability of nucleic acids. Finally, we discuss how to target non-canonical nucleic acid structures, especially G-quadruplex, by small molecules toward cancer treatment.
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DISCOVERY
  • Organic chemistry and medicinal chemistry, and drug development studies of pharmaceutical academia in Japan
    Satoshi Shuto
    2024 Volume 34 Issue 1 Pages 43-46
    Published: February 01, 2024
    Released on J-STAGE: February 01, 2024
    DOIhttps://doi.org/10.14894/medchem.34.1_43
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    Staffs of pharmaceutical academia should describe that “organic chemistry is essential for pharmaceutical sciences”, This is because that drugs are organic molecules so that organic chemistry is irreplaceable science to understand drugs. Efficacy, toxicity, and ADME of drugs are unequivocally dependent on the chemical structure of drugs as a organic molecule. From this viewpoint of that drugs are organic molecules controlling body conditions, understanding pharmacodynamics and pharmacokinetics of drugs should be background not only for researchers on drugs but also for pharmacists. It is important that drug development studies in academia must be science.
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