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

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Agarwal T,Roy S,Chakraborty TK,Maiti S

doi

10.1016/j.bmcl.2010.06.080

subject

Has Abstract

pub_date

2010-08-01 00:00:00

pages

4346-9

issue

15

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(10)00854-1

journal_volume

20

pub_type

杂志文章

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