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Antitumor compound bis - [2,6-difluoro-n - (hydroxy-o) benzamide-o] dibutyltin (IV) and human peroxisome proliferator activated receptor hPPAR γ Discussion on interaction ability

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Document pages: 10 pages

Abstract: Organotin (IV) antitumor compound bis - [2,6-difluoro-n - (hydroxy-< κ> O) Benzamide-< κ> O] (dbdf2,6t) is a new patented organotin compound with high antitumor activity and low toxicity. In this study, a variety of methods were used to study dbdf2,6t and hPPAR γ Interactions between proteins, including fluorescence quenching, three-dimensional fluorescence, drug affinity response target stability (darts), ultrafiltration chromatography and molecular docking. The experimental results show that hPPAR γ The quenching process of protein is mainly through hydrophobic interaction to spontaneously form a non radiative ground state complex with dbdf2,6t by static quenching. Dbdf2, 6T can be directly connected with hPPAR γ Protein binding, so that it has anti enzyme activitytic hydrolysis. And the binding mode of DBDF2,6T into hPPARγ protein appeared to have an orientation towards residues of SER342 and GLY284. In conclusion, these methods could comprehensively reveal the interaction details of DBDF2,6T and the hPPARγ protein and established a feasible way to preliminarily identify the agonist compounds for the hPPARγ protein.

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