MEDCHEM NEWS
Online ISSN : 2432-8626
Print ISSN : 2432-8618
ISSN-L : 2432-8618
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Volume 33, Issue 4
Displaying 1-19 of 19 articles from this issue
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  • Expectations and Challenges for RNA-Targeted Small Molecule Drug Discovery
    Kazuhiko Nakatani
    2023 Volume 33 Issue 4 Pages 158-164
    Published: November 01, 2023
    Released on J-STAGE: November 01, 2023
    DOIhttps://doi.org/10.14894/medchem.33.4_158
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    Small molecule drug discovery research targeting RNA is accelerating. Although academia has long suggested that RNA is a potential drug discovery target, the proposal has been neglected in our country. In my laboratory, our goal has been to present as many facts as possible that “small molecules that bind to nucleic acids can be involved in the regulation of functional expression in vivo” so that not only the academic world but also the industrial world can realize the potential of the combination of small molecules and nucleic acids. In the following, I would like to introduce my research to date, and give my opinion on the challenges of RNA-targeted small molecule drug discovery, which is now attracting the attention of many people.
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ESSAY
  • The current situation in microbiome drug development
    Yun-Gi Kim
    2023 Volume 33 Issue 4 Pages 170-175
    Published: November 01, 2023
    Released on J-STAGE: November 01, 2023
    DOIhttps://doi.org/10.14894/medchem.33.4_170
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    In recent years, accumulating evidence indicates that dysbiosis of gut microbiota is associated with various diseases. In fact, restoring gut dysbiosis may lead to disease treatment, prevention, and alleviation of pathology. Therefore, many companies are being established worldwide to develop microbiome drugs that cure and prevent diseases by improving the gut environment (microbiome) . The development of microbiome drugs has received a great deal of interest over the past decade. Although there have been clinical and regulatory success stories, there have also been layoffs and bankruptcies at multiple microbiome companies for several reasons. In this section, I would like to discuss the development status of drug discovery focusing on the microbiome, including my own experiences.
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  • Everything for your research and development ─KISHIDA’s activities for drug discovery consortiums
    Susumu Igarashi, Toshihiro Watanabe
    2023 Volume 33 Issue 4 Pages 176-180
    Published: November 01, 2023
    Released on J-STAGE: November 01, 2023
    DOIhttps://doi.org/10.14894/medchem.33.4_176
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    Japanese pharmaceutical companies have recognized the advancement of open innovation in the 2010s, several drug discovery consortiums for joint purchasing of chemical libraries, joint constructing of them, or joint use of building blocks were established. Drug discovery support in KISHIDA CHEMICAL CO. LTD. (KISHIDA) started a chemical bank business as a slogan of “Everything for your research and development” and has participated in several drug discovery consortiums. In this essay, we overview characteristic of the consortiums and introduce KISHIDA’s activities for them.
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DISCOVERY
  • Discovery of HDAC8-selective inhibitors and their application to PROTACs
    Yasunobu Yamashita, Yuri Takada, Yukihiro Itoh, Takayoshi Suzuki
    2023 Volume 33 Issue 4 Pages 181-186
    Published: November 01, 2023
    Released on J-STAGE: November 01, 2023
    DOIhttps://doi.org/10.14894/medchem.33.4_181
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    Histone deacetylase 8 (HDAC8) , one of the zinc-dependent HDACs, catalyzes the deacetylation of non-histone proteins such as cohesion. HDAC8 not only has a catalytic function but also serves a scaffolding function where it interacts with transcription factors such as STAT3 and CREB to regulate gene expression. HDAC8 is involved in the growth of T-cell leukemia and it is a promising target of anticancer drugs. Therefore, conventional inhibitors and PROteolysis TArgeting Chimeras (PROTACs) are interesting because they inhibit the catalytic function and both catalytic/scaffolding functions of HDAC8, respectively. Based on this background, we have attempted a drug discovery study on HDAC8. Herein, we present the identification of HDAC8 selective inhibitors through screenings of a library constructed by click chemistry, its structural optimization, and the development of an HDAC8 PROTAC based on the identified HDAC8 inhibitors.
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SEMINAR
  • Development of anti-SARS-CoV-2 agents based on HIV researches
    Hirokazu Tamamura
    2023 Volume 33 Issue 4 Pages 187-192
    Published: November 01, 2023
    Released on J-STAGE: November 01, 2023
    DOIhttps://doi.org/10.14894/medchem.33.4_187
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    The COVID-19 pandemic, which was caused by a positive-strand RNA virus SARS-CoV-2, has expanded throughout the world and continues for more than three years. In the past three decades, we have been developing anti-HIV-1 agents including protease inhibitors. According to the classification of viruses, HIV-1 and SARS-CoV-2 belong to RNA viruses and have some common characteristics. Therefore, we envisioned to apply our obtained knowledge and achievements in the researches on HIV/AIDS to the development of novel SARS-CoV-2 main protease (Mpro) inhibitors. As a result, potent and biostable inhibitors against SARS-CoV-2 Mpro were designed and synthesized.
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  • Research on risk factors on the onset of dialysis-related amyloidosis and strategy for prevention of amyloidosis
    Kichitaro Nakajima, Keiichi Yamaguchi, Yuji Goto
    2023 Volume 33 Issue 4 Pages 193-198
    Published: November 01, 2023
    Released on J-STAGE: November 01, 2023
    DOIhttps://doi.org/10.14894/medchem.33.4_193
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    Dialysis-related amyloidosis (DRA) is a type of systemic amyloidosis specific for long-term dialysis patients, which is caused by aberrant proteinaceous aggregates called amyloid fibrils, mainly composed of β2-microglobulin (β2m) . The onset mechanism of this disease remains to be clarified. Here, we analyzed the effects of sera collected from dialysis patients on β2m amyloid formation by means of an originally developed ultrasonic amyloid inducer and explored the risk factors controlling the onset of DRA. As a summary of this paper, we review recent strategies for the prevention and treatment of amyloidosis and discuss the effective option to eradicate amyloidosis from the perspective of physical chemistry.
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