論文 - 詳細
| RRC ID | 74466 |
|---|---|
| 著者 | Yoshihara A, Kawasaki H, Masuno H, Takada K, Numoto N, Ito N, Hirata N, Kanda Y, Ishizawa M, Makishima M, Kagechika H, Tanatani A. |
| タイトル | Lithocholic Acid Amides as Potent Vitamin D Receptor Agonists. |
| ジャーナル | Biomolecules |
| Abstract |
1α,25-Dihydroxyvitamin D3 [1α,25(OH)2D3, 1] is an active form of vitamin D3 and regulates various biological phenomena, including calcium and phosphate homeostasis, bone metabolism, and immune response via binding to and activation of vitamin D receptor (VDR). Lithocholic acid (LCA, 2) was identified as a second endogenous agonist of VDR, though its potency is very low. However, the lithocholic acid derivative 3 (Dcha-20) is a more potent agonist than 1α,25(OH)2D3, (1), and its carboxyl group has similar interactions to the 1,3-dihydroxyl groups of 1 with amino acid residues in the VDR ligand-binding pocket. Here, we designed and synthesized amide derivatives of 3 in order to clarify the role of the carboxyl group. The synthesized amide derivatives showed HL-60 cell differentiation-inducing activity with potency that depended upon the substituent on the amide nitrogen atom. Among them, the N-cyanoamide 6 is more active than either 1 or 3. |
| 巻・号 | 12(1) |
| 公開日 | 2022-1-14 |
| DOI | 10.3390/biom12010130 |
| PII | biom12010130 |
| PMID | 35053278 |
| PMC | PMC8773473 |
| MeSH | Amides / pharmacology Cholecalciferol Humans Lithocholic Acid* / metabolism Lithocholic Acid* / pharmacology Protein Binding Receptors, Calcitriol* / metabolism |
| IF | 4.082 |
| オルトメトリクス指標 |
オルトメトリクス指標項目
|
| 最多言及媒体 | X(Twitter) |
| 各媒体での言及数の合計 | 1 |
| 過去6か月間でのオルトメトリクス指標の変動値 | 0.0 |
| リソース情報 | |
| ヒト・動物細胞 | 293(RCB1637) |