MEDCHEM NEWS
Online ISSN : 2432-8626
Print ISSN : 2432-8618
ISSN-L : 2432-8618
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Volume 32, Issue 4
Displaying 1-17 of 17 articles from this issue
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  • Axcelead: Your best partner for innovation in a new trend of drug discovery
    Yoshinori Ikeura, Takahiro Tanaka
    2022 Volume 32 Issue 4 Pages 178-183
    Published: November 01, 2022
    Released on J-STAGE: November 01, 2022
    DOIhttps://doi.org/10.14894/medchem.32.4_178
    JOURNAL FREE ACCESS
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    Axcelead Drug Discovery Partners （Axcelead DDP） Inc. is the first solution provider of integrated drug discovery in Japanese pharmaceutical industry. Experienced drug discovery researchers will promote drug discovery research together with customers and contribute to creation of innovative drugs by making full use of the drug discovery platform and knowledge inherited from Takeda Pharmaceutical Company, Ltd., and incorporating the brand-new science and technology. In this column we overview changes in the environment surrounding pharmaceutical industry and new trends in drug discovery research, and introduce Axcelead DDP’s research organizational structure, its unique strengths, and the value （solutions） delivered to customers. In addition, we touch on current situation of the Japanese bio-community and describe the roles and challenges of Axcelead DDP for the establishment / development of a drug discovery ecosystem in Japan.
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WINDOW
  • What I experienced at Scripps aiming to challenge highly original drug discovery seeds
    Masahito Abe
    2022 Volume 32 Issue 4 Pages 184-189
    Published: November 01, 2022
    Released on J-STAGE: November 01, 2022
    DOIhttps://doi.org/10.14894/medchem.32.4_184
    JOURNAL FREE ACCESS
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    In any research area, globalization is necessary for sharing the latest technology and knowledge. In particular, to achieve significant results in drug discovery, global collaboration among multiple research institutes is required. Meanwhile, there are fewer easy drug discovery targets, commonly referred to as low hanging fruit, for developing small molecule drugs; therefore, novel drug discovery targets and modalities are required. Case in point, I was working as a medicinal chemist for a domestic pharmaceutical company, but I decided to move to the US with the goal of working in a research environment focused on discovering novel drug discovery targets and new strategies to target them. In this column, I will elaborate on my research experience as a staff scientist at Scripps and the difference of research environment between industry/academia in Japan and the US and give my personal opinion on these differences.
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ESSAY
  • Anti-inflammatory Bowel Disease Drug Discovery Targeting Retinoid X Receptors
    Hiroki Kakuta
    2022 Volume 32 Issue 4 Pages 190-194
    Published: November 01, 2022
    Released on J-STAGE: November 01, 2022
    DOIhttps://doi.org/10.14894/medchem.32.4_190
    JOURNAL FREE ACCESS
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    Inflammatory bowel disease （IBD） is a chronic inflammatory disease of the intestinal tract that causes diarrhea, bloody stools, and other symptoms. Types of IBD include ulcerative colitis （UC） and Crohn’s disease （CD）. The number of IBD patients is increasing worldwide, with about 220,000 people suffering from UC and 70,000 from CD in Japan. Various drugs are available to treat IBD, depending on the severity of the disease, including 5-aminosalicylic acid （5-ASA）, steroidal anti-inflammatory drugs, and large-molecule drugs such as anti-TNF-α antibodies. However, antibody drugs are more expensive than small-molecule drugs, and over time they lose their therapeutic capacity, which can lead to the need for increased dosing or modification of the therapeutic strategy. Consequently, there is a need for the development of drugs for IBD based on new mechanisms of action. This paper presents an example of research into the development of IBD therapeutics targeting the retinoid X receptor.
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DISCOVERY
  • Discovery of S-217622, an Oral SARS-CoV-2 3CL Protease Inhibitor for Treating COVID-19
    Yuki Tachibana
    2022 Volume 32 Issue 4 Pages 195-200
    Published: November 01, 2022
    Released on J-STAGE: November 01, 2022
    DOIhttps://doi.org/10.14894/medchem.32.4_195
    JOURNAL FREE ACCESS
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    The global pandemic caused by the novel coronavirus, severe acute respiratory syndrome coronavirus 2 （SARS-CoV-2）, has had an unprecedented impact on the economy and life of individuals globally, and safe and efficacious oral agents are urgently required. We discovered a non-peptidic, non-covalent SARS-CoV-2 3CLpro inhibitor S-217622 （Ensitrelvir）, which displayed in vitro and in vivo antiviral activity with preferable DMPK profile for once-daily oral dosing, using an SBDD strategy. The preclinical data support the suitable pharmaceutical properties of Ensitrelvir as a potential oral therapeutic agent for patients with COVID-19, and in clinical trials started in July 2021, favourable pharmacokinetics （Ph1） and clear antiviral effects （Ph2a and Ph2b） have been confirmed. As of July 2022, Ph3 trials are underway and it has been filed for approval as an Emergency Use Authorization in Japan.
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SEMINAR
  • Invention and potential applications of AUTAC, a novel strategy based on selective autophagy
    Daiki Takahashi, Hirokazu Arimoto
    2022 Volume 32 Issue 4 Pages 201-206
    Published: November 01, 2022
    Released on J-STAGE: November 01, 2022
    DOIhttps://doi.org/10.14894/medchem.32.4_201
    JOURNAL FREE ACCESS
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    Degrader technologies, such as PROTACs and SNIPER, hijack the ubiquitin-proteasome pathway, a cellular degradation system, to remove disease-related proteins. Degraders have become a standard method for drug discovery because they can be applied to undruggable targets, including scaffold proteins or pseudoenzymes. The use of autophagy in degrader design would expand the scope of degraders and enable the elimination of a broad range of substrates, such as pathogens, cell organelles, and protein aggregates. In this review article, we describe the status quo of autophagy-based degrader technologies: AUTAC, ATTEC, and AUTOTAC.
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  • Overview and new trends of high-throughput synthesis
    Ryushi Seo, Junko Watanabe
    2022 Volume 32 Issue 4 Pages 207-211
    Published: November 01, 2022
    Released on J-STAGE: November 01, 2022
    DOIhttps://doi.org/10.14894/medchem.32.4_207
    JOURNAL FREE ACCESS
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    High-throughput synthesis technology is based on combinatorial chemistry and has been contributing to the acceleration of small molecule drug discovery research for many years. In recent years, there have been remarkable developments in synthesis-related equipment, including robotics technology, and in drug discovery research that incorporates artificial intelligence （AI）. By incorporating such technologies, high-throughput synthesis continues to evolve. In Astellas, more automated platforms are being leveraged for synthesis, and ADMET prediction models are being actively utilized in library design. In this report, we provide an overview of high-throughput synthesis technology in drug discovery, including design and synthesis, and introduce our company’s efforts to integrate the latest technology into high-throughput synthesis.
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  • Progress in small molecule kinase inhibitor drug discovery and perspectives: Twenty years after the FDA’s approval of the first small molecule kinase inhibitor
    Kiyosei Iio
    2022 Volume 32 Issue 4 Pages 212-216
    Published: November 01, 2022
    Released on J-STAGE: November 01, 2022
    DOIhttps://doi.org/10.14894/medchem.32.4_212
    JOURNAL FREE ACCESS
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    After 20 years of FDA’s approval of Imatinib, as many as 75 small molecule kinase inhibitors have been approved by FDA. The biggest challenge in the early kinase drug discovery era was to generate inhibitors with a high degree of kinase selectivity across the whole kinome. Preferential binding to an inactive form of targeted kinase along with high selectivity of Imatinib led to discovery and design of inhibitors for the same types. With the addition of the covalent inhibitor approach, inhibitors with high kinase selectivity have been generated, overcoming the initial challenges. In this article, the FDA approved drugs are classified into five types, and the binding mode of each representative drug with its features are discussed.
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Coffee Break
REPORT
  • Activities of “Working Group for New Frontier in Drug Discovery”
    Satoshi Yokoshima, Taro Terauchi
    2022 Volume 32 Issue 4 Pages 218-221
    Published: November 01, 2022
    Released on J-STAGE: November 01, 2022
    DOIhttps://doi.org/10.14894/medchem.32.4_218
    JOURNAL FREE ACCESS
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    “Working Group for New Frontier in Drug Discovery” （NF-WG） was launched in 2016 as a subgroup of The Pharmaceutical Society of Japan Division of Medicinal Chemistry with the aim of vitalizing research field of medicinal chemistry. NF-WG, which consists of diverse member from various pharmaceutical companies and universities, has worked on Medicinal Chemistry Symposium to make it more valuable for all participants, for example, poster categorization system and luncheon seminar were newly incorporated. Furthermore, new program, “Round-table discussion with industry scientists” was initiated as a quite unique opportunity for interaction between industry scientists and students. We will continue to take on new challenges to enhance connectivity between scientists in medicinal chemistry field, because “Fostering Relationship” is fundamental key word for NF-WG.
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