首页> 外国专利> D-APTIDE AND RETRO-INVERSO APTIDE WITH MAINTAINED TARGET AFFINITY AND IMPROVED STABILITY

D-APTIDE AND RETRO-INVERSO APTIDE WITH MAINTAINED TARGET AFFINITY AND IMPROVED STABILITY

机译:目标亲和力和稳定性得到改善的D肽和逆向肽

摘要

The present invention is characterized by a D-aptamer-like peptide (D-Aptide) or retro-inverso Aptide which specifically binds to a target comprising: (a) a structure stabilizing region comprising parallel, antiparallel or parallel and antiparallel D-amino acid strands with interstrand noncovalent bonds; and (b) a target binding region I and a target binding region II comprising randomly selected n and m D-amino acids, respectively, and coupled to both ends of the structure stabilizing region. The D-Aptide or retro-inverso Aptide has the sequence of the same or opposite direction to L-Aptide, wherein the stability to proteases is improved while maintaining the affinity to a target compared with L-Aptide. The D-Aptide of the present invention has substantially the same target affinity and a remarkably improved stability compared with L-Aptide which is different from a general technical knowledge.
机译:本发明的特征在于与靶标特异性结合的D-适体样肽(D-Aptide)或逆反-Aptide,其包括:(a)结构稳定区域,其包含平行,反平行或平行和反平行D-氨基酸具有链间非共价键的链; (b)分别包含随机选择的n和m个D-氨基酸的靶结合区I和靶结合区II,并结合到结构稳定区的两端。 D-肽或逆-逆肽具有与L-肽相同或相反方向的序列,其中与L-肽相比,对蛋白酶的稳定性得到改善,同时保持了对靶标的亲和力。与L-肽相比,本发明的D-肽具有基本相同的靶亲和力和显着改善的稳定性,这不同于一般技术知识。

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