Directed combinatorial compound library and high throughput...

C - Chemistry – Metallurgy – 07 – K

Patent

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C07K 9/00 (2006.01) A61K 38/14 (2006.01) C07B 61/00 (2006.01) C07H 19/06 (2006.01) C07H 19/16 (2006.01) C12Q 1/48 (2006.01)

Patent

CA 2334338

A combinatorial library comprising a predetermined collection of nucleoside peptide molecules for inhibiting the transfer of a sugar from a selected sugar nucleotide donor to a selected acceptor by a carbohydrate processing enzyme. The nucleoside peptide molecule comprises (a) a nucleoside monomer; (b) a spacer monomer coupled to the nucleoside monomer wherein the spacer monomer comprises one or more amide linked amino acid residues, or a peptidomimetic; and (c) cap monomers attached to the spacer monomer. The nucleoside peptide molecules differ from each other as to the identity of at least one element of the nucleoside monomer, spacer monomer, or cap monomer.

L'invention concerne une banque combinatoire renfermant une série prédéterminée de molécules peptidiques de nucléoside permettant d'inhiber le transfert d'un sucre d'un donneur sélectionné nucléotidique de sucre à un accepteur sélectionné, transfert effectué par une enzyme de traitement des hydrates de carbone. Cette molécule comprend (a) un monomère de nucléoside; (b) un monomère espaceur couplé à un monomère de nucléoside et contenant un ou plusieurs restes d'aminoacides liés à un amide ou un composé peptidomimétique; et (c) un monomère de coiffage fixé au monomère espaceur. Les molécules peptidiques de nucléoside diffèrent les unes des autres ce qui permet l'identification d'au moins un élément du monomère de nucléoside, du monomère espaceur ou du monomère de coiffage.

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