Fig. 3 | Bone Research

Fig. 3

From: Galactose-modified small molecule modulator targets RORα to enhance circadian rhythm and alleviate periodontitis-associated alveolar bone loss

Fig. 3

Exploring the impact of acetal linker design on the targeted regulatory function of RORα. a The small molecules galactose and SR1078 are generated upon the cleavage of Gala-SR by β-galactosidase; The upper part: a schematic diagram illustrates the process of enzymatic hydrolysis. Lower part: MS spectra of Gala-SR after hydrolysis by β-galactosidase; b Binding pose of Gala-SR and SR1078 on the simulated RORα structure predicted by AutodockVina; c The luminescence of HEK293T cells cotransfected with RORα and a reporter containing the G6Pase or FGF21 promoters upstream of a luciferase reporter gene was measured following the addition of 5 μmol/L Gala-SR and combined with β-galactosidase or β-galactosidase inhibitor (n = 4); d The mRNA expression of G6Pase and FGF21 in HepG2 cells treated with 5 μmol/L of Gala-SR and combined with β-galactosidase or β-galactosidase inhibitor. (n = 6). (* represents the comparison with Gala-SR, **P < 0.01); e, f Molecular dynamics simulation of the interaction between Gala-SR, SR1078 and RORα

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