(2S,2'R)-analogue of LG190178 is a major active isomer.

Article Details

Citation

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
DrugTargetPropertyMeasurementpHTemperature (°C)
CalcitriolVitamin D3 receptorEC 50 (nM)0.555N/AN/ADetails
CalcitriolVitamin D3 receptorEC 50 (nM)0.0106N/AN/ADetails
CalcitriolVitamin D3 receptorEC 50 (nM)3.52N/AN/ADetails