MEDCHEM NEWS
Online ISSN : 2432-8626
Print ISSN : 2432-8618
ISSN-L : 2432-8618
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Volume 32, Issue 2
Displaying 1-20 of 20 articles from this issue
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WINDOW
  • A story of necessary but unprofitable medicines
    Tatsuro Kuzuki
    2022 Volume 32 Issue 2 Pages 66-71
    Published: May 01, 2022
    Released on J-STAGE: May 01, 2022
    DOIhttps://doi.org/10.14894/medchem.32.2_66
    JOURNAL FREE ACCESS
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    You may be aware of a Japanese proverb “Kusuri Kusou Bai” （a medicine costs 9 times more than its cost of goods）. It tells us that medicines have been very expensive since long ago. Nowadays, pharmaceutical companies will seek to develop new medicines in more profitable areas to cover the huge costs of R&D （Research and Development）. This idea seems quite reasonable from the viewpoint of market economy. But in reality, it may lead to lost opportunities to develop much needed medicines, if we do not reconsider this concept.
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ESSAY
  • J-PUBLIC -Toward Construction of “All Japan” Compound Library-
    Haruna Iwaoka
    2022 Volume 32 Issue 2 Pages 72-76
    Published: May 01, 2022
    Released on J-STAGE: May 01, 2022
    DOIhttps://doi.org/10.14894/medchem.32.2_72
    JOURNAL FREE ACCESS
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    “Japan Public Library Consortium （J-PUBLIC）” has been established by nine companies in April 2020. J-PUBLIC is a consortium, that jointly manages and uses diverse compound libraries, aims to construct of “All Japan’’ Compound Library. As the first step, we started sharing the library of members （companies）, and then established members （academia） as a new participation category and opened the library to Japanese academia. This article describes the background and characteristic of the consortium as well as expectations for diverse compound library.
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  • Polymer designing for next generation mRNA therapeutics
    Satoshi Uchida
    2022 Volume 32 Issue 2 Pages 77-80
    Published: May 01, 2022
    Released on J-STAGE: May 01, 2022
    DOIhttps://doi.org/10.14894/medchem.32.2_77
    JOURNAL FREE ACCESS
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    Lipid nanoparticles （LNPs） show promise in the delivery of mRNA therapeutics. Meanwhile, polyplex micelles （PMs） possess properties different from LNPs, offering different options in the therapeutic application of mRNA. After in vivo local injections, PMs provide efficient protein expression from mRNA without inducing tissue damage and inflammatory responses, contributing to efficient tissue repair and protection in disease models. Furthermore, PMs can target various organs without intrinsic tropism to a specific organ in systemic delivery. Indeed, PMs effectively deliver mRNA to tumors for anti-angiogenic therapy. Moreover, intracellular degradation of mRNA is prevented by fine-tuning of polycation structures, leading to prolonged protein expression from mRNA. These technologies provide an excellent platform for future clinical translation of mRNA therapeutics.
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DISCOVERY
  • Discovery of Enarodustat （Enaroy®） as a novel HIF-PH Inhibitor
    Yosuke Ogoshi, Takuya Matsui, Ikuo Mitani, Masahiro Yokota, Hiroyuki A ...
    2022 Volume 32 Issue 2 Pages 81-86
    Published: May 01, 2022
    Released on J-STAGE: May 01, 2022
    DOIhttps://doi.org/10.14894/medchem.32.2_81
    JOURNAL FREE ACCESS
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    Since FG-2216, a pioneer HIF-prolyl hydroxylase （PH） inhibitor, was reported to show hematopoiesis in patients on hemodialysis, orally active HIF-PH inhibitors have been expected as a new therapeutic option. On the basis of the pharmacophore for HIF-PH inhibitors, we synthesized various scaffolds and identified several fused heterocyclic compounds as promising lead compounds. Our lead optimization to improve cell permeability and selection by in vivo screening led to the discovery of enarodustat, which showed hematopoiesis with daily oral dosing.
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SEMINAR
  • Molecular design and application of fluorescent probes for drug discovery research
    Kenjiro Hanaoka
    2022 Volume 32 Issue 2 Pages 87-92
    Published: May 01, 2022
    Released on J-STAGE: May 01, 2022
    DOIhttps://doi.org/10.14894/medchem.32.2_87
    JOURNAL FREE ACCESS
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    Fluorescent probes are smart molecules which can show an off/on fluorescence change in response to the specific reaction with biomolecules. These probes are utilized as tools in fluorescence imaging for visualizing the biological phenomena inside living cells and animals. So far, many fluorescent probes from 350nm （UV region） to 600nm （red region） have been developed. On the other hand, the authors have recently succeeded in developing novel fluorophores, i.e., Si-rhodamines and TokyoMagentas, which emit the fluorescence in 600nm to 750nm region （the far-red to near-infrared region）, and these fluorophores enable the development of various fluorescent probes in this long wavelength region. In this text, these novel fluorophores and the development of fluorescent probes based on them will be introduced, then the possibility of these long-wavelength fluorescent probes in the drug discovery process will be discussed.
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  • Activities of Targeted Alpha Therapy at Osaka University
    Kazuya Kabayama, Yoshifumi Shirakami, Kazuko Kaneda, Tadashi Watabe, A ...
    2022 Volume 32 Issue 2 Pages 93-98
    Published: May 01, 2022
    Released on J-STAGE: May 01, 2022
    DOIhttps://doi.org/10.14894/medchem.32.2_93
    JOURNAL FREE ACCESS
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    Targeted Alpha Therapy （TAT） is one of the drug therapies to kill cancer cells by delivering high-energy alpha emitting nuclides to them. We have been developing and evaluating a short-lived alpha emitting nuclides, astatine-211 （211At）, and drug candidate compounds labeled with it. In this article, we review the results of our cross-departmental collaborative research and development, mainly conducted at Osaka University, including the production/purification of 211At, synthesis of targeting molecules, and the path to clinical trials.
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Coffee Break
REPORT
  • Report on 19th Annual Discovery on Target
    Ryo Sakakibara
    2022 Volume 32 Issue 2 Pages 102-104
    Published: May 01, 2022
    Released on J-STAGE: May 01, 2022
    DOIhttps://doi.org/10.14894/medchem.32.2_102
    JOURNAL FREE ACCESS
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    The 19th Annual Discovery on Target was held from September 27th, 2021 to 30th. This is an international conference that covers not only chemical but also biological modalities and involves researchers with diverse expertise. There are many sessions on drug discovery, including methodologies for identifying therapeutic target and hit compounds, and hot therapeutic approach such as RNA-targeted drug discovery and PROTACs. This report focuses on drug discovery approaches that challenge undruggable targets that are difficult to target with conventional approaches.
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