Affinity-Guided Design of Caveolin-1 Ligands for Deoligomerization
详细信息 查看全文
- 作者：Amanda J. H. Gilliam ; Joshua N. Smith ; Dylan Flather ; Kevin M. Johnston ; Andrew M. Gansmiller ; Dmitry A. Fishman ; Joshua M. Edgar ; Mark Balk ; Sudipta Majumdar ; Gregory A. Weiss
- 刊名：Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：April 28, 2016
- 年：2016
- 卷：59
- 期：8
- 页码：4019-4025
- 全文大小：409K
- 年卷期：0
- ISSN：1520-4804
文摘
Caveolin-1 is a target for academic and pharmaceutical research due to its many cellular roles and associated diseases. We report peptide WL47 (1), a small, high-affinity, selective disrupter of caveolin-1 oligomers. Developed and optimized through screening and analysis of synthetic peptide libraries, ligand 1 has 7500-fold improved affinity compared to its T20 parent ligand and an 80% decrease in sequence length. Ligand 1 will permit targeted study of caveolin-1 function.