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Structure-based design of substituted biphenyl ethylene ethers as ligands binding in the hydrophobic pocket of gp41 and blocking the helical bundle formation.

Abstract：

:A series of substituted biphenyl ethylene ether compounds has been designed to target the gp41N-trimer in order to inhibit formation of the six-helical bundle that represents the end state of gp41-mediated viral fusion. A size exclusion HPLC based helical bundle formation (HBF) assay was developed to evaluate in vitro inhibitory affinity of the inhibitors. The most potent compound 1 had an IC(50) of 31microM. The binding of compound 1 to the proposed hydrophobic pocket of gp41 was further validated by site-directed peptide mutagenesis experiments.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Liu B,Joseph RW,Dorsey BD,Schiksnis RA,Northrop K,Bukhtiyarova M,Springman EB

doi

10.1016/j.bmcl.2009.08.018

subject

Has Abstract

pub_date

2009-10-01 00:00:00

pages

5693-7

issue

19

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(09)01137-8

journal_volume

19

pub_type

杂志文章

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