Exploring the interaction of anti-androgen drug-bicalutamide with human alpha-2-macroglobulin: A biophysical investigation

International Journal of Biological Macromolecules
Mohammad Khalid ZiaFahim Halim Khan

Abstract

Bicalutamide (BCT), a drug used in the treatment of prostate cancer, antagonises the actions of androgens, at the receptor level, thereby inhibiting the growth of prostate tumours. Alpha-2-macroglobulin (α2M), a pan-proteinase inhibitor, inhibits proteinase, regardless of specificity and catalytic mechanism. α2M is deficient in patients of advanced prostate cancer with bone metastases. Our studies explored the interaction of BCT with α2M and analysed the BCT induced structural alteration to the α2M. The result suggests that BCT decreases the antiproteolytic potential and causes structural and functional change in human α2M. UV-visible absorption spectroscopy confirms the formation of α2M-BCT complex. Fluorescence analysis shows significant quenching in fluorescence intensity of α2M upon binding with BCT. Synchronous fluorescence result suggests the interaction of BCT with α2M changed the microenvironment around tyrosine residues. Secondary structure of α2M also undergoes a slight change upon complexation with the drug as evident by shift in negative ellipticity in far UV CD spectroscopy. FTIR results confirm the alteration in secondary structure of α2M upon drug interaction. Molecular docking studies show that BCT bind to a mon...Continue Reading

Citations

Sep 24, 2019·Journal of Biomolecular Structure & Dynamics·Tooba SiddiquiFahim Halim Khan
Jul 22, 2019·Journal of Fluorescence·Tooba SiddiquiFahim Halim Khan
Aug 6, 2019·Journal of Biomolecular Structure & Dynamics·Mohd Aamir Qureshi, Saleem Javed
Jun 15, 2021·International Journal of Biological Macromolecules·Georges JourdiPascale Gaussem

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