ChemMatrix resin for the synthesis of complex peptides and combinatorial libraries

TULLA-PUCHE, JUDIT; GARCÍA MARTIN, F.; MARANI, MARIELA MIRTA; PARADIS-BAS, MARTA; OLIVEIRA, ELIANDRE; GARCIA RAMOS, Y.; CAMPERI, SILVIA ANDREA; COTE, SIMON; CASCONE, OSVALDO; ALBERICIO, FERNANDO

Canada

Simposio; 20th American Peptide Society Symposium; 2007

  Enfurtivide (T-20 or fuzeon),  a 36-residue peptide which corresponds to 638 to 673 amino acid residues of the transmembrane protein gp41 from HIV-1, is the first fusion inhibitor for the treatment of HIV. Due to its highly hydrphobic sequence, large scale synthesis of T-20 has relied on a mixed solution-solid phase strategy, by synthesis shorter peptides on solid-phase , and coupling them in solution. We report here that by using ChemMatixm, a totally-based PEG resin which had performed excellently for the synthesis of complex and highly structured peptides, T-20 can be obtained in a stepwise manner, thus avoiding time-consuming steps such as precipitation and purification opf the peptide fragments. ChemMatix resin, which swells very well in biocomplatible solvents, can also be used for the synthsis