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- Title
Synthesis and biophysical studies of hairpin polyamides targeting the Brn-3b and GATA-3 transcriptional sites.
- Authors
Babu, Balaji; Mackay, Hilary; Prast, Abby; Dittenhafer, Kristin; Davis, Ryan; Tronrud, Christopher; Rice, Toni; Chavda, Sameer; Lee, Moses
- Abstract
Hairpin polyamide analogs of distamycin A ( 1 ) were designed and synthesized to evaluate their ability to bind 5'-ATAGA-3' and 5'-AGATA-3'sequences which are important elements for controlling the function of the Brn-3b and GATA-3 transcriptional factors, respectively. The hairpin polyamides are composed of pyrrole and imidazole units linked together via a γ-aminobutyrate (GABA) unit. Hairpins 2b (Py-Py-Im-γ-Py-Py-Py) and 2c (Im-Py-Py-γ-Py-Py-Py) were synthesized to target the respective Brn-3b and GATA-3 cognate sequences. Preliminary biophysical studies including thermal denaturation and circular dichroism were performed and the results ascertained the binding of hairpins 2a and 2b to their respective cognate DNA sequences.
- Publication
Heterocyclic Communications, 2010, Vol 16, Issue 4-6, p221
- ISSN
0793-0283
- Publication type
Article
- DOI
10.1515/HC.2010.002