转铁蛋白受体亲和肽衍生物的制备

Preparation of Transferrin Receptor Binding Peptide Derivative

以2-氯三苯甲基氯(2-CTC)树脂为固相载体、N-芴甲氧羰基(Fmoc)保护氨基酸为原料、N,N′-二异丙基碳二亚胺(DIC)和1-羟基苯并三唑(HOBt)为缩合剂,采用Fmoc固相合成法制备了一种转铁蛋白受体亲和肽(transferrin receptor binding peptide,TfRBP)衍生物,其纯品的HPLC纯度为97.9%,总收率为40.3%,经ESI-MS鉴定其相对分子质量与理论值一致。该方法操作简便、合成周期短、总收率高,为进一步构建TfR靶向多肽-药物偶联物奠定了基础。

Taking 2-chlorotrityl chloride(2-CTC)resin as a solid phase carrier,N-fluorene methoxycarbonyl(Fmoc)protected amino acid as a raw material,and N,N′-diisopropyl carbodiimide(DIC)and 1-hydroxybenzotriazole(HOBt)as condensation agents,we prepared a transferrin receptor binding peptide(TfRBP)derivative by Fmoc solid-phase synthesis.The HPLC purity and the total yield of the pure TfRBP derivative are 97.9%and 40.3%,respectively.The molecular weight of the pure TfRBP derivative is consistent with the theoretical value,which is identified by ESI-MS.The method has the advantages of easy operation,shorter synthetic period,and high total yield,which can lay a foundation for further construction of TfR-targeted peptide-drug conjugate.