Chemically modified cd4 peptide fragments having...

C - Chemistry – Metallurgy – 07 – K

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530/7, 167/103.8

C07K 14/73 (2006.01) A61K 38/04 (2006.01) A61K 38/17 (2006.01) C07K 7/04 (2006.01)

Patent

CA 2022523

CHEMICALLY MODIFIED CD4 PEPTIDE FRAGMENTS HAVING ANTI-RETROVIRAL PROPERTIES ABSTRACT OF THE DISCLOSURE A general method of derivitizing and selecting fragments of CD4 peptides that exhibit enhanced (relative to the original fragment) capacity to modulate a CD4-dependent virus-induced cellular response. In one aspect, peptide compositions comprising a sequence of human CD4 which includes at least a core sequence of seven consecutive amino acids of the N-terminal proximal sequence or a sequence including the cysteine at position 84 (C84) are provided. At least one amino acid side chain is derivatized, such as the cysteine at position 84 (C84) or the glutamic acid at position 85 (E85). Various groups may be used as derivatizing groups, including aryl-containing substituents, or in the case of cysteine, a thioether resulting from the reaction between the thio group of the cysteine and a maleimide. The resulting compositions may be used prophylactically or therapeutically for inhibiting interactions between CD4 and retroviral proteins. 87.

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