(2S,2'R)-analogue of LG190178 is a major active isomer.
Article Details
- CitationCopy to clipboard
Hakamata W, Sato Y, Okuda H, Honzawa S, Saito N, Kishimoto S, Yamashita A, Sugiura T, Kittaka A, Kurihara M
(2S,2'R)-analogue of LG190178 is a major active isomer.
Bioorg Med Chem Lett. 2008 Jan 1;18(1):120-3. Epub 2007 Nov 5.
- PubMed ID
- 18054230 [ View in PubMed]
- Abstract
Vitamin D receptor (VDR) ligands are therapeutic agents for the treatment of psoriasis, osteoporosis, and secondary hyperparathyroidism. VDR ligands also show immense potential as therapeutic agents for autoimmune diseases and cancers of the skin, prostate, colon, and breast as well as leukemia. LG190178 is a novel non-secosteroidal ligand for VDR. We synthesized and evaluated stereoisomers of LG190178 and found that only an (2S,2'R)-analogue of LG190178 (YR301) had strong activity.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Calcitriol Vitamin D3 receptor EC 50 (nM) 0.555 N/A N/A Details Calcitriol Vitamin D3 receptor EC 50 (nM) 0.0106 N/A N/A Details Calcitriol Vitamin D3 receptor EC 50 (nM) 3.52 N/A N/A Details