Affinity-Guided Design of Caveolin-1 Ligands for Deoligomerization.

Affinity-Guided Design of Caveolin-1 Ligands for Deoligomerization.
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用于去寡聚化的 Caveolin-1 配体的亲和引导设计。

DOI:
10.1021/acs.jmedchem.5b01536
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发表时间:
2016
影响因子:
7.3
通讯作者:
Weiss,GregoryA
Weiss,GregoryA
中科院分区:
医学1区
文献类型:
--
作者:
Gilliam,AmandaJH;Smith,JoshuaN;Flather,Dylan;Johnston,KevinM;Gansmiller,AndrewM;Fishman,DmitryA;Edgar,JoshuaM;Balk,Mark;Majumdar,Sudipta;Weiss,GregoryA

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Caveolin-1由于其许多细胞作用和相关疾病而成为学术和药物研究的目标。我们报道了肽WL 47(1),一种小的、高亲和力的、选择性的小窝蛋白-1寡聚体破坏剂。通过对合成肽库的筛选和分析进行开发和优化,ligand 1与其T20亲本配体相比具有7500倍的亲和力,并且序列长度减少了80%。配体1将允许有针对性地研究小窝蛋白-1的功能。
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, ligand1has 7500-fold improved affinity compared to its T20 parent ligand and an 80% decrease in sequence length. Ligand1will permit targeted study of caveolin-1 function.
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