靶向结直肠癌细胞中memHsp70+表型的铂（IV）奥沙利铂-肽缀合物
Platinum(iv) oxaliplatin-peptide conjugates targeting memHsp70+ phenotype in colorectal cancer cells.
作者信息
McKeon A M, Noonan J, Devocelle M, Murphy B M, Griffith D M
机构信息
Department of Pharmaceutical & Medicinal Chemistry, Royal College of Surgeons in Ireland, 123 St. Stephens Green, Dublin 2, Ireland.
出版信息
Chem Commun (Camb). 2017 Oct 12;53(82):11318-11321. doi: 10.1039/c7cc04764a.
Novel Pt(iv) tumour penetrating peptide (TPP) conjugates are reported. They are the first example of metallodrugs to target a membrane bound heat shock protein 70 positive (memHSP70+) phenotype in cancer cells. The conjugates exhibit superior cytotoxicity as compared to oxaliplatin alone in Pt resistant colorectal cancer cells with relatively high memHSP70+ expression. Substitution of TPP in Pt(iv) peptide conjugates with scrambled peptide (ScP) essentially abolishes the observed cytotoxicity.
报道了新型的铂（IV）肿瘤穿透肽（TPP）偶联物。它们是金属药物靶向癌细胞中膜结合热休克蛋白70阳性（memHSP70+）表型的首个实例。与单独使用奥沙利铂相比，这些偶联物在具有相对较高memHSP70+表达的铂耐药结肠癌细胞中表现出更强的细胞毒性。用乱序肽（ScP）取代铂（IV）肽偶联物中的TPP基本消除了观察到的细胞毒性。
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