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Exploration on the Interaction Ability of Antitumor Compound Bis-[2,6-difluoro-N-(hydroxyl-<κ>O)benzamidato-<κ>O]dibutylitin(IV) with Human Peroxisome Proliferator-Activated Receptor hPPARγ
Joint Authors
Mai, Jiaqi
Qiao, Xiaozhi
Ji, Xiaoqing
Li, Qingshan
Li, Yunlan
Source
Bioinorganic Chemistry and Applications
Issue
Vol. 2018, Issue 2018 (31 Dec. 2018), pp.1-10, 10 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2018-06-10
Country of Publication
Egypt
No. of Pages
10
Main Subjects
Abstract EN
Diorganotin(IV) antitumor compound bis-[2,6-difluoro-N-(hydroxyl-<κ>O)benzamidato-<κ>O] (DBDF2,6T) was one of the novel patent organotin compounds with high antitumor activity and relatively low toxicity.
In this study, several methods were used to study the interaction between DBDF2,6T and hPPARγ protein, including fluorescence quenching, three-dimensional (3D) fluorescence, drug affinity responsive target stability (DARTS), ultrafiltration-LC, and molecular docking.
According to the experimental results, the quenching process of the hPPARγ protein was induced by static quenching mode to form a nonradiative ground-state complex with DBDF2,6T spontaneously, mainly through the hydrophobic force.
DBDF2,6T could bind to the hPPARγ protein directly and give the protein the ability of antienzymatic 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.
American Psychological Association (APA)
Mai, Jiaqi& Li, Yunlan& Qiao, Xiaozhi& Ji, Xiaoqing& Li, Qingshan. 2018. Exploration on the Interaction Ability of Antitumor Compound Bis-[2,6-difluoro-N-(hydroxyl-<κ>O)benzamidato-<κ>O]dibutylitin(IV) with Human Peroxisome Proliferator-Activated Receptor hPPARγ. Bioinorganic Chemistry and Applications،Vol. 2018, no. 2018, pp.1-10.
https://search.emarefa.net/detail/BIM-1123120
Modern Language Association (MLA)
Mai, Jiaqi…[et al.]. Exploration on the Interaction Ability of Antitumor Compound Bis-[2,6-difluoro-N-(hydroxyl-<κ>O)benzamidato-<κ>O]dibutylitin(IV) with Human Peroxisome Proliferator-Activated Receptor hPPARγ. Bioinorganic Chemistry and Applications No. 2018 (2018), pp.1-10.
https://search.emarefa.net/detail/BIM-1123120
American Medical Association (AMA)
Mai, Jiaqi& Li, Yunlan& Qiao, Xiaozhi& Ji, Xiaoqing& Li, Qingshan. Exploration on the Interaction Ability of Antitumor Compound Bis-[2,6-difluoro-N-(hydroxyl-<κ>O)benzamidato-<κ>O]dibutylitin(IV) with Human Peroxisome Proliferator-Activated Receptor hPPARγ. Bioinorganic Chemistry and Applications. 2018. Vol. 2018, no. 2018, pp.1-10.
https://search.emarefa.net/detail/BIM-1123120
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-1123120