University of Medicine and Dentistry of New Jersey

Other

Ikramul Huq

Tariq M Rana

Natarajan Tamilarasu

This invention relates to the use of oligourea molecules to specifically inhibit protein-nucleic acid interactions. In particular, it provides an oligourea molecule that competes with the Tat molecule for the TAR RNA of HIV-1. Also provided is a method specifically inhibiting protein-nucleic and interactions, and kits.

Tat-derived oligourea and its method of production and use in high affinity and specific binding HIV-1 TAR RNA

Inhibition of HIV-1 replication using d-amino acid peptides

Tat-inhibitory oligocarbamate derivatives of the formula I ##STR1## and analogs thereof, and the biologically and pharmaceutically acceptable salts thereof exhibit advantageous properties, including specific binding to TAR RNA with high affinities, and stability of the resultant oligocarbamate-RNA complexes to proteolytic digestion. Site-specific photocrosslinking experiments using a photoactive analog (4-thio-uracil) containing TAR RNA indicate that these oligocarbamates interact with RNA in the major groove. These oligocarbamates are thus capable of competing with the TAR RNA-binding domain of Tat protein and thus are useful as a therapeutic agents in the treatment of AIDS.

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Edison, NJ, United States of America

Ikramul Huq