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Binding of the putative anticancer agent chelerythrine to double stranded poly(A): Calorimetry and spectral characterization studies

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Title Binding of the putative anticancer agent chelerythrine to double stranded poly(A): Calorimetry and spectral characterization studies
 
Creator Basu, Pritha
Basu, Anirban
Kumar, Gopinatha Suresh
 
Subject Chemistry
 
Description The benzophenanthridine plant alkaloid chelerythrine was recently reported to bind to single stranded
polyriboadenylic acid [ss poly(A)] through an entropy driven process with remarkably high binding affinity
(�107 M�1) (Basu and Suresh Kumar, 2015). Considering the anticancer effects of chelerythrine along with
its potential to be developed as an RNA targeted drug due to its high affinity to ss poly(A), here we studied
the binding of chelerythrine to double stranded (ds) poly(A). The binding was characterized thermodynamically
by enthalpy and entropy changes, and enthalpy-entropy compensation behaviour. The binding thermally stabilized the structure. The binding led to hypochromic and bathochromic effects in the visible absorption spectrum of chelerythrine and enhanced its fluorescence intensity. An intercalative binding mode was deduced from fluorescence quenching, anisotropy, and viscometric studies. The binding of chelerythrine to the ds poly(A) was significantly weaker than its binding to ss poly(A). The results may lead to designing RNA targeted therapeutics and a useful agent in gene regulation in eukaryotic cells.
 
Date 2016
 
Type Article
PeerReviewed
 
Format application/pdf
 
Identifier http://www.eprints.iicb.res.in/2689/1/J._Chem._Thermodynamics_103_(2016)_228%E2%80%93233.pdf
Basu, Pritha and Basu, Anirban and Kumar, Gopinatha Suresh (2016) Binding of the putative anticancer agent chelerythrine to double stranded poly(A): Calorimetry and spectral characterization studies. J. Chem. Thermodynamics, 103. pp. 228-233.
 
Relation http://dx.doi.org/10.1016/j.jct.2016.08.019
http://www.eprints.iicb.res.in/2689/