Furan based cyclic homo-oligopeptides bind G-quadruplex selectively and repress c-MYC transcription

Agarwal, Tani ; Roy, Saumya ; Chakraborty, Tushar Kanti ; Maiti, Souvik (2010) Furan based cyclic homo-oligopeptides bind G-quadruplex selectively and repress c-MYC transcription Bioorganic & Medicinal Chemistry Letters, 20 (15). pp. 4346-4349. ISSN 0960-894X

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Official URL: http://www.sciencedirect.com/science/article/pii/S...

Related URL: http://dx.doi.org/10.1016/j.bmcl.2010.06.080

Abstract

We demonstrate the synthesis and selective binding of two novel furan based tricyclic homo-oligopeptides to G-quadruplex and using Real Time PCR show its repressive effect on c-MYC transcription. CD spectroscopy and FRET melting studies show that these ligands can induce G-quadruplex structures in the G rich 22 mer c-MYC DNA sequence and further stabilize the structure. Using real time polymerase chain reaction we observed that up to 70% downregulation of c-MYC transcripts upon ligand treatment in HeLa cells.

Item Type:Article
Source:Copyright of this article belongs to Elsevier Science.
Keywords:Quadruplex; Cancer; c-MYC; Macrocyclic Compounds; Oligopeptides
ID Code:69577
Deposited On:14 Nov 2011 03:52
Last Modified:14 Nov 2011 03:52

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