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The First Locked Side-Chain Analogues of Calcitriol (1α,25-Dihydroxyvitamin D3) Induce Vitamin D Receptor Transcriptional Activity

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journal contribution
posted on 30.10.2003, 00:00 by Xenxo Pérez-García, Antonio Rumbo, María Jesús Larriba, Paloma Ordóñez, Alberto Muñoz, Antonio Mouriño
We describe the synthesis of the first locked side-chain analogues of the natural hormone 1α,25-(OH)2-D3 and their effects on gene transcription in human colon cancer cells. Analogue 2 was more potent than 1α,25-(OH)2-D3 at inducing vitamin D receptor (VDR) transcriptional activity. Analogues 3a and 3b show potency similar to that of 1α,25-(OH)2-D3, whereas 3c was less active. The novel analogues efficiently bind VDR in vivo to induce transcription from a consensus vitamin D responsive element (VDRE).