Peptide analogs and mimetics suitable for in vivo use in the...

C - Chemistry – Metallurgy – 07 – K

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C07K 7/64 (2006.01) A61K 38/12 (2006.01) A61P 25/28 (2006.01) C07C 229/34 (2006.01) C07K 5/02 (2006.01) C07K 14/47 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2389041

The present invention is an inhibitory peptide capable of inhibiting .beta. pleated sheet formation in amyloid .beta.-peptide. The inhibitory peptide is a .beta.sheet breaker peptide analog designed by chemical modification of .beta. sheet breaker peptide capable of inhibiting .beta. pleated sheet formation in amyloid .beta.-peptide. The present invention also includes an inhibitory peptide capable of inhibiting conformational changes in prion PrP protein associated with amyloidosis. The inhibitory peptide being a .beta.sheet breaker peptide analog designed by chemical modification of a .beta.sheet breaker peptide capable of inhibiting the conformational changes in prior PrP protein associated with amyloidosis. In addition, the present invention includes a peptide mimetic with the structure PMiA.beta.5. In another embodiment, the peptide mimetic has the structure PMiPrP13. In yet another embodiment, the peptide mimetic has the structure PMiPrP5.

L'invention concerne un peptide inhibiteur capable d'inhiber une formation de repli en .beta.-feuille dans un .beta.-peptide amyloïde. Ce peptide inhibiteur est un analogue peptidique de rupture de .beta.-feuille conçu par modification chimique d'un peptide de rupture de .beta.-feuille capable d'inhiber la formation de repli en .beta.-feuille dans un .beta.-peptide amyloïde. Elle concerne également un peptide inhibiteur capable d'inhiber des modifications de conformation dans la protéine PrP de type prion associé à l'amyloïdose. Ce peptide inhibiteur est un analogue peptidique de rupture de .beta.-feuille conçu par modification chimique d'un peptide de rupture de .beta.-feuille capable d'inhiber les modifications de conformation de la protéine PrP de type prion associée à l'amyloïdose. Elle concerne, de plus, un mimétique de peptide représenté par la formule suivante: PMiA.beta.5. Dans un autre mode de réalisation, ce mimétique de peptide présente la structure suivante:PMiPrP13. Dans encore un autre mode de réalisation, ce mimétique de peptide présente la structure suivante: PMiPrP5.

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