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The Identification of Naturally Occurring Neoruscogenin as a Bioavailable, Potent and High-Affinity Agonist of the Nuclear Receptor RORa (NR1F1)

S. Helleboid, C. Haug, K. Lamottke, Y. Zhou, J. Wei, S. Daix, L. Cambula, G. Rigou, D. W. Hum, R. Walczak, Journal of Biomolecular Screening, Jul 2013, DOI: 10.1177/1087057113497095.

New target validation has always been a challenge for the pharmaceutical industry with respect to the potential therapeutic value. Information obtained through genetic gain- and/or loss-of-function approaches is of course of great value, but it does not replace target validation through pharmacological stimulation or inhibition of a target with selective and potent chemical ligands. The identification of such ligands usually takes 18 to 24 months or even more in programs where medicinal chemistry starts from high-throughput screening (HTS)–derived hit compounds identified in chemical libraries.

Since it is essential to provide high-quality proof-of-concept validations early in the drug discovery process, technologies that enable the identification of potent, selective, and bioavailable chemical probes are of crucial interest, even if the resulting compounds require further optimization for development into a pharmaceutical product.

 See abstract in English

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