Medicinal chemistry of vitamin A: Development of synthetic retinoid,Am80 (Tamibarotene) and future prospects

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  • Fujii Shinya
    Laboratory of Organic and Medicinal Chemistry, Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University
  • Kagechika Hiroyuki
    Laboratory of Organic and Medicinal Chemistry, Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University

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Other Title
  • V．ビタミンA の創薬化学：合成レチノイドAm80（タミバロテン）の開発と将来展望
  • ビタミンAの創薬化学 : 合成レチノイドAm80(タミバロテン)の開発と将来展望
  • ビタミン A ノ ソウヤッカガク : ゴウセイ レチノイド Am80(タミバロテン)ノ カイハツ ト ショウライ テンボウ
  • 特集　―脂溶性ビタミン研究70 年―

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Description

Retinoid regulates various biological phenomena, such as cell proliferation, differentiation, morphogenesis, immunity, and metabolism, by binding and activating two types of nuclear receptors, retinoic acid receptors (RARs) and retinoid X receptors (RXRs). Since the discovery of these nuclear receptors, various specific modulators for both RARs and RXRs have been developed. Among them, some RAR and RXR specific agonists including Am80 (tamibarotene), an RARα/ β-selective agonist are in clinical use. Based on the recent progress in the research on the retinoid functions, the potential clinical utilities of retinoids towards metabolic diseases, autoimmune diseases, and neurodegenerative diseases have been elucidated. Here, the development of synthetic retinoids in the last 30 years, and the future prospect of the retinoid therapy are overviewed.

Journal

  • VITAMINS

    VITAMINS 94 (3), 137-142, 2020-03-25

    THE VITAMIN SOCIETY OF JAPAN

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