Direct evaluation of polarity of the ligand binding pocket in retinoid X receptor using a fluorescent solvatochromic agonist

High selectivity of small-molecule drug candidates for their target molecule is important to minimize potential side effects. One factor that contributes to the selectivity is the internal polarity of the ligand-binding pocket (LBP) in the target molecule, but this is difficult to measure. Here, we...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2023-11, Vol.96, p.129536-129536, Article 129536
Hauptverfasser: Miura, Kizuku, Fujihara, Michiko, Watanabe, Masaki, Takamura, Yuta, Kawasaki, Mayu, Nakano, Shogo, Kakuta, Hiroki
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Sprache:eng
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