申请人:University of Pittsburgh - Of the Commonwealth System of Higher Education
公开号:US20140128388A1
公开(公告)日:2014-05-08
Drug candidates for inhibition of HIV-1 replication can target Src family kinases (SFK), such as Hck, that interact with Nef protein of the virus. Compounds characterized by such inhibitory activity were identified via an assay for kinase activity of an SFK in a Nef:SFK complex. Illustrative of inhibitors identified using the kinase assay are various 2,3-diaminoquinaxolines and furo[2,3-d]pyrimidines. The inventive inhibitors were found to arrest HIV-1 viral replication in vitro.
针对HIV-1复制的药物候选物可以针对Src家族激酶(SFK),例如与病毒的Nef蛋白相互作用的Hck。通过对Nef:SFK复合物中SFK的激酶活性进行测定,鉴定了具有这种抑制活性的化合物。使用激酶测定鉴定的抑制剂的例子包括各种2,3-二氨基喹啉和呋喃[2,3-d]嘧啶。发明的抑制剂被发现可以在体外阻止HIV-1病毒复制。