[EN] CONJUGATE FOR TREATING MALARIA<br/>[FR] CONJUGUÉ UTILISABLE EN VUE DU TRAITEMENT DU PALUDISME
申请人:UNIV STELLENBOSCH
公开号:WO2016024240A1
公开(公告)日:2016-02-18
A peptide-polymer conjugate is provided for use in treating malaria infections, and in particular terminal or drug resistant malaria infections. The conjugate is formed from a polymer to which a peptide having activity against a malaria parasite is covalently attached. The peptide is a cyclic decapeptide from the closely-related group of tyrocidines, tryptocidines, phenycidines and gramicidin S, and the polymer is a hydrophilic and biocompatible polymer with a terminal thiol, such as poly(N-vinylpyrrolidone) (PVP). The polymer chains can be decorated with a hydrophilic targeting ligand that specifically targets an epitope on red blood cells, and in particular red blood cells infected with a plasmodial parasite. A method for synthesising the peptide-polymer conjugate is also provided.
提供了一种用于治疗疟疾感染的肽-聚合物共轭物,特别是终末期或耐药性疟疾感染。该共轭物由一种聚合物形成,其中共价连接了对疟原虫具有活性的肽。该肽是来自与腺苷环化素、色胺环化素、苯甲环化素和青霉素S密切相关的腺苷十肽群的环十肽,而聚合物是一种具有末端硫醇的亲水性和生物相容性聚合物,例如聚(N-乙烯吡咯烷酮)(PVP)。聚合物链可以装饰有一个亲水性靶向配体,该配体特异性地靶向红细胞上的一个表位,特别是感染疟原虫的红细胞。还提供了一种合成肽-聚合物共轭物的方法。