LIGANDS THAT TARGET HCV-E2 BINDING SITES ON CD81 A

专利名称：LIGANDS THAT TARGET HCV-E2 BINDING

SITES ON CD81 AND THERAPEUTICMETHODS USING THEM

发明人：Hassan AZZAZY,Reem Al-Olaby,Rodney

Balhorn

申请号：US14717635申请日：20150520

公开号：US20150328329A1公开日：20151119

摘要：Ligands that target the HCV-E2 binding site and methods of making and usingthem. A series of ligand binding sites on the large extracellular loop of the openconformation of CD81 have been identified. Several important sites were located inregions identified by mutational studies to be the site of E2 binding. Ligands that

recognize these sites were identified. Linking together two or three ligands that bind withlow or moderate affinities to different structurally unique sites on a target protein wereused to generate small molecule ligand conjugates that exhibit very high affinities totheir CD81 targets. Hybrid ligand molecules were also designed using fragment-baseddrug design methods to generate analogs of the ligands that bind more tightly to theprotein than the parent compounds. Identification and design of groups of compoundsthat bind to CD81 for use as therapeutics for treating patients infected by Hepatitis Cvirus and other viruses that interact with CD81. By binding to CD81, these molecules canblock 1) HCV and other viral entry into cells (infection), 2) inflammatory responses causedby HCV and other viral infections, and 3) the induction of HCV associated cancers.

申请人：American University of Cairo

地址：New Cairo EG

国籍：EG

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