Role of 13-(di)phenylalkyl berberine derivatives in the modulation of the activity of human topoisomerase IB

International Journal of Biological Macromolecules
Sara VieiraAlessandro Desideri

Abstract

Topoisomerases IB are anticancer and antimicrobial targets whose inhibition by several natural and non-natural compounds has been documented. The inhibition effect by berberine and some 13-(di)phenylalkyl berberine derivatives has been tested towards human topoisomerase IB. Derivatives belonging to the 13-diphenylalkyl series display an efficient inhibition of the DNA relaxation and cleavage step, that increases upon pre-incubation with the enzyme. The religation step of the enzyme catalytic cycle is not affected by compounds and only slightly upon pre-incubation. The binding of the protein to the DNA substrate occurs also in the presence of the compounds, as monitored by a DNA shift assay, indicating that the compounds are not able to inhibit the formation of the enzyme-DNA complex but that they act as catalytic inhibitors.

References

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Citations

Jul 20, 2016·Archives of Biochemistry and Biophysics·Venn VuteyAlessandro Desideri
Aug 6, 2016·Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences·Wenchao WangQingyong Li
Jan 11, 2017·Journal of Medicinal Chemistry·Giovanni CapranicoGiovanni Chillemi
Apr 3, 2018·Journal of Biomolecular Structure & Dynamics·Urmila SahaGopinatha Suresh Kumar
Sep 27, 2019·Dalton Transactions : an International Journal of Inorganic Chemistry·Monize M da SilvaAlzir A Batista
Apr 5, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Solomon Habtemariam
Dec 8, 2020·Beilstein Journal of Organic Chemistry·Jonas BecherChristopher Stremmel
May 1, 2021·International Journal of Molecular Sciences·Alessio OttavianiAlessandro Desideri

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