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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 
 
 

HIV-1 integrase inhibition by pyrrole/imidazole-containing polyamides.

Since HIV-1 integrase (IN) is responsible for catalyzing the insertion of the viral genome into the host cell chromosome, it provides an attractive target for antiviral drug design. We synthesized a set of pyrrole/imidazole-containing polyamides (PAs), specifically interacting within the minor groove of DNA in order to find inhibitors of integrase. All PAs contained different N- and C-terminal groups. A first family of polyamides, the (a) series, contained 3 or 4 heterocyclic rings (pyrrole or imidazole) linearly bound. A second family, the (b) series are 'bifunctional PAs' that contained two linear chains of oligocarboxamides in opposite orientation, each with 3 or 4 pyrrole or imidazole units connected with a flexible spacer. The inhibition of integrase activity by the (a) series depended on their sequence and increased with the number of rings, especially imidazole residues. Bifunctional compounds were tripyrroles with different spacers, or different combinations of pyrroles and imidazoles keeping the same spacer. The affinity of integrase for bifunctional tripyrroles linked by three different spacers (gamma-aminobutyric acid, beta-alanine or glycine) strongly depended on the spacer. Changing from gamma-aminobutyric acid to shorter spacers increased the affinity. The other group of bifunctional PAs containing alternating imidazoles or pyrrole rings, but with the same spacer, showed affinities that depended on the sequence of unnatural amino acids. These data indicate that some of the newly synthesized PAs can provide a rationale for the design of drugs targeting the integration step.[1]

References

  1. HIV-1 integrase inhibition by pyrrole/imidazole-containing polyamides. Zakharova, O.D., Baranova, S., Parissi, V., Ryabinin, V.A., Sinyakov, A.N., Litvak, S., Litvak, L.T., Nevinsky, G.A. J. Pept. Res. (2005) [Pubmed]
 
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