The Picower Institute for Medical Research

Bristol-myers Squibb Compnay

Omar K Haffar

Michael I Bukrinsky

Senliang Pan

Steven G Nadler

James J Blake

Jeffrey S Cleaveland

Novel polypeptide inhibitors of cytoplasmic protein nuclear translocation are disclosed. The inhibitors are comprised of a signal sequence and at least two nuclear localization sequences. The polypeptides are useful as immunosuppression, antiviral and antitumor agents.

Peptide inhibitors of nuclear protein translocation having nuclear

There is disclosed a structural genus of compounds, defined according to coordinates in three-dimensional space, that binds amino moieties on neighboring lysine residues in a tyrosine residue 29 pocket of the matrix protein component of the HIV preintegration complex (PIC), thereby preventing the PIC from binding to karyopherin .alpha. and preventing nuclear importation and integration of the HIV viral genome into the host cell DNA, thereby preventing viral infection.

HIV matrix protein tyrosine position 29 pocket binders

There is disclosed a genus of compounds that have anti-HIV infection therapeutic activity and inhibit nuclear localization of the HIV preintegration complex.

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Seattle, WA, United States of America

Omar K Haffar