Synthesis and biophysical studies of hairpin polyamides targeting the Brn-3b and GATA-3 transcriptional sites

Heterocyclic communications

article

Balaji Babu¹  Hilary Mackay¹  Abby Prast¹  Kristin Dittenhafer¹  Ryan Davis¹  Christopher Tronrud¹  Toni Rice¹  Sameer Chavda¹  Moses Lee¹ 

[1] Department of Chemistry, Hope College

关键词: Brn-3b;    DNA;    GATA-3;    hairpin polyamides;    minor groove;    transcriptional factors;   

DOI  :  10.1515/HC.2010.002

学科分类：内科医学

来源: De Gruyter

【 摘 要 】

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.

【 授权许可】

CC BY|CC BY-NC-ND