A structured peptide scaffold for displaying turn libraries...

C - Chemistry – Metallurgy – 12 – N

Patent

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C12N 15/10 (2006.01) C07K 1/04 (2006.01) C07K 14/705 (2006.01) C07K 14/71 (2006.01) C07K 14/73 (2006.01) C07K 14/735 (2006.01) G01N 33/68 (2006.01)

Patent

CA 2376232

The invention is directed to a model system for structure-activity analysis of peptide or protein molecules involved in important biological processes. Provided by the invention are combinatorial peptide libraries comprising disulfide-constrained cyclic peptides with sequences favorable for energy stabilized conformations. A preferred embodiment of the invention is directed to peptides containing .beta.-turn tetrapeptide that form structured .beta.- hairpin scaffold in solution. Methods of selecting and using such peptides are provided herein, which are useful for mimicking in vivo molecular interactions and designing therapeutic agents. Thus, the invention has profound utility for biological studies and drug development.

L'invention concerne un système modèle permettant d'effectuer une analyse des rapports structure-activité dans des molécules peptidiques ou protéiniques intervenant dans des processus biologiques importants. L'invention concerne également des bibliothèques combinatoires de peptides comprenant des peptides cycliques à contrainte disulfure avec des séquences favorables à des conformations stables. Un mode de réalisation préféré de l'invention concerne des peptides contenant des tétrapeptides à enroulement .beta. qui forment un échafaudage en épingle à cheveux .beta. en solution. L'invention concerne des méthodes de sélection et d'utilisation de ces peptides, utiles pour mimer des interactions moléculaires in vivo et élaborer des agents thérapeutiques. Cette invention présente donc une grande utilité pour les études biologiques et l'élaboration de médicaments.

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