MEDCHEM NEWS
Online ISSN : 2432-8626
Print ISSN : 2432-8618
ISSN-L : 2432-8618
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Volume 33, Issue 1
Displaying 1-16 of 16 articles from this issue
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  • Towa Pharmaceutical’s Research and Development Initiatives
    Osamu Uchikawa, Yutaka Okuda
    2023 Volume 33 Issue 1 Pages 6-10
    Published: February 01, 2023
    Released on J-STAGE: February 01, 2023
    DOIhttps://doi.org/10.14894/medchem.33.1_6
    JOURNAL FREE ACCESS
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    Generic drug development has been conducted using ready-made APIs purchased from domestic and foreign API manufacturers for drug formulation development. However, in recent years, there have been frequent situations in which this business model has not worked with regard to the quality and stable supply of APIs. In order to prepare for such a situation, we established the Business Development Division (currently API Business Division) in 2011 to realize the self-manufacturing of APIs, and in 2017 we launched the Fundamental Technology Laboratory (currently Innovative Technology Research Division) to develop our own formulation technology. The various efforts that have been made over the years to achieve the ultimate commercialization of products (creating products with the No.1 overall product competitiveness) by tirelessly improving and enhancing them using the latest and best technologies and know-how to serve people’s health are finally coming to fruition.
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WINDOW
  • The activities of the Japan Scripps Society and recent trends in the Scripps Research Institute
    Seiya Kitamura, Ikuo Fujii
    2023 Volume 33 Issue 1 Pages 11-15
    Published: February 01, 2023
    Released on J-STAGE: February 01, 2023
    DOIhttps://doi.org/10.14894/medchem.33.1_11
    JOURNAL FREE ACCESS
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    The Japan Scripps Society is a research network whose members are researchers who have worked in The Scripps Research Institute (TSRI) as graduate students, postdoctoral fellows, or visiting scientists. The society organizes annual symposiums and social gatherings to promote research exchange and personal communication among its members. The unique feature of the Japan Scripps Society is that the membership consists of the almost same number of researchers from universities and industries. Therefore, in the symposiums, unlike ordinary academic conferences, lectures and Q&A sessions are conducted from the viewpoints of both academics and industries, providing an excellent opportunity for academics to study the needs of companies. In this column, we introduce the activities of the Japan Scripps Society as well as recent trends in the Scripps Research Institute.
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ESSAY
  • Nicotinamide mononucleotide for the potential treatment of age-associated dry eye disease
    Sui-Wen Hsiao, Masao Doi
    2023 Volume 33 Issue 1 Pages 16-20
    Published: February 01, 2023
    Released on J-STAGE: February 01, 2023
    DOIhttps://doi.org/10.14894/medchem.33.1_16
    JOURNAL FREE ACCESS
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    Meibomian gland dysfunction (MGD) is the most common cause of dry eye, with incidence increasing with age. Here we show that (re)activation of local intracrine activity through nicotinamide adenine dinucleotide (NAD+)-dependent circadian 3β-hydroxyl-steroid dehydrogenase (3β-HSD) activity ameliorates age-associated MGD and MGD-associated dry eye disease. The loss of blood-circulating sex-steroid hormones is a hallmark of aging in both men and women; however, exogenous steroid hormone replacement therapy has been limited owing to its adverse side effects. Given this limitation of systemic steroid supplementation, the potential merit of local intracrine activity activation by topical supplementation of NAD+ bioprecursor (nonsteroidal agent) warrants further clinical evaluation for MGD treatment.
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DISCOVERY
  • Discovery of YH-53 as a 3CL Protease Inhibitor for SARS-CoV-2
    Yoshio Hayashi, Sho Konno
    2023 Volume 33 Issue 1 Pages 21-27
    Published: February 01, 2023
    Released on J-STAGE: February 01, 2023
    DOIhttps://doi.org/10.14894/medchem.33.1_21
    JOURNAL FREE ACCESS
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    SARS-CoV-2 identified as the causative agent for the current coronavirus disease (COVID-19) utilizes 3CL protease (3CLpro) which is an essential viral enzyme for the viral replications. Therefore, 3CLpro is a promising drug target for the development of antiviral agents for coronavirus diseases. We have been developing a series of peptide-type 3CLpro inhibitors since the outbreak of SARS in 2003. In the current research, we demonstrated that YH-53 is effective against SARS-CoV-2. Here we describe our efforts to develop YH-53.
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SEMINAR
  • 3D electron diffraction and solid-state NMR towards crystalline structure solution of small molecules
    Yusuke Nishiyama
    2023 Volume 33 Issue 1 Pages 28-32
    Published: February 01, 2023
    Released on J-STAGE: February 01, 2023
    DOIhttps://doi.org/10.14894/medchem.33.1_28
    JOURNAL FREE ACCESS
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    Brief introduction to three-dimensional (3D) electron diffraction (ED) , which solves crystalline structures of micro- to nano-sized crystals, is given. Geometry optimization is conducted by the first-principle quantum computation which also provides NMR chemical shift values. By comparing the experimental and calculated solid-state NMR chemical shifts, it is shown that non-hydrogen atoms are accurately located by 3D ED, however, hydrogens are not. It is mandatory to use first-principle quantum computation to locate hydrogens accurately together with evaluation by solid-state NMR.
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  • Redox-Driven Antibody Modifications
    Motomu Kanai, Kounosuke Oisaki, Moe Toyobe
    2023 Volume 33 Issue 1 Pages 33-37
    Published: February 01, 2023
    Released on J-STAGE: February 01, 2023
    DOIhttps://doi.org/10.14894/medchem.33.1_33
    JOURNAL FREE ACCESS
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    The selective amino acid chemical modifications selectively modify only one of 20 canonical amino acids in peptides and proteins. Lysine and cysteine are often targeted for selective modifications using the nucleophilicity of their side chains. These reactions are applied to antibody-drug conjugates for clinical use. Recently, selective modifications targeting residues other than lysine and cysteine have been reported. However, small peptides and proteins have been the main substrates. Conjugation and functionalization of antibodies, large protein complexes comprising several domains and subunits, are still limited. In this manuscript, we discuss selective tyrosine, tryptophan, and methionine modifications based on the unique redox properties of these amino acids and reactants, their applications to antibody modifications, and the functional evaluation of the conjugates.
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Coffee Break
REPORT
  • ACBI's Strategic Student Recruiting Efforts from Emerging Asian Countries
    Motonari Uesugi, Mitsue Nakashima
    2023 Volume 33 Issue 1 Pages 39-41
    Published: February 01, 2023
    Released on J-STAGE: February 01, 2023
    DOIhttps://doi.org/10.14894/medchem.33.1_39
    JOURNAL FREE ACCESS
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    Asian Chemical Biology Initiative (ACBI) has been influential in promoting chemical biology research and education throughout the Asian region. Since its inception in April 2011, more than 100 members from Japan, Korea, China, Singapore, and India have participated in this bold initiative, impacting the professors and students from emerging Asian countries including Vietnam, Thailand, the Philippines, Malaysia, Indonesia, Mongolia, and Myanmar. This report will walk you through the unprecedented journey the ACBI has taken over 10 years, with a special focus on one of ACBI’s unique strategies: how it has been attracting outstanding international students from emerging Asian countries.
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