Targeting human telomeric G-quadruplex DNA with curcumin and its synthesized analogues under molecular crowding conditions
IR@CECRI: CSIR-Central Electrochemical Research Institute, Karaikudi
View Archive Info| Field | Value | |
| Title |
Targeting human telomeric G-quadruplex DNA
with curcumin and its synthesized analogues under
molecular crowding conditions
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| Creator |
Jha, N.S.
Satyendra , M. Mamidi, S. Ashalatha, S. Archita , M. Jha, S.K. Avadhesha , S. |
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| Subject |
Industrial Metal Finishing
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| Description |
The formation of telomeric G-quadruplexes has been shown to inhibit telomerase activity. Indeed, a number
of small molecules capable of p-stacking with G-tetrads have shown the ability to inhibit telomerase activity
through the stabilization of G-quadruplexes. Curcumin displays a wide spectrum of medicinal properties
ranging from anti-bacterial, anti-viral, anti-protozoal, anti-fungal and anti-inflammatory to anti-cancer
activity. We have investigated the interactions of curcumin and its structural analogues with the human
telomeric sequence AG3(T2AG3)3 under molecular crowding conditions. Experimental studies indicated
the existence of a AG3(T2AG3)3/curcumin complex with binding affinity of 0.72 � 106 M1 under
molecular crowding conditions. The results from UV-visible absorption spectroscopy, a fluorescent TO
displacement assay, circular dichroism and molecular docking studies, imply that curcumin and their
analogues interact with G-quadruplex DNA via groove binding. While other analogs of curcumin studied
here bind to G-quadruplexes in a qualitatively similar manner their affinities are relatively lower in
comparison to curcumin. The Knoevenagel condensate, a methoxy-benzylidene derivative of curcumin,
also exhibited significant binding to G-quadruplex DNA, although with two times decreased affinity. Our
study establishes the potential of curcumin as a promising natural product for G-quadruplex specific ligands.
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| Publisher |
Royal Society of Chemistry
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| Date |
2016
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| Type |
Article
PeerReviewed |
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| Format |
application/pdf
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| Identifier |
http://cecri.csircentral.net/3187/1/213-2016.pdf
Jha, N.S. and Satyendra , M. and Mamidi, S. and Ashalatha, S. and Archita , M. and Jha, S.K. and Avadhesha , S. (2016) Targeting human telomeric G-quadruplex DNA with curcumin and its synthesized analogues under molecular crowding conditions. RSC Advances, 6. pp. 7474-7487. ISSN 2046-2069 |
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| Relation |
http://www.rsc.org/advances
http://cecri.csircentral.net/3187/ |
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