A Peptide-Duocarmycin Conjugate Targeting the Thomsen-Friedenreich Antigen Has Potent and Selective Antitumor Activity.,Bioconjugate Chemistry

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A Peptide-Duocarmycin Conjugate Targeting the Thomsen-Friedenreich Antigen Has Potent and Selective Antitumor Activity.
Bioconjugate Chemistry ( IF 4.0 ) Pub Date : 2020-06-09 , DOI: 10.1021/acs.bioconjchem.0c00282
Oliver Charles Cartwright ₁ , Andrew Michael Beekman ₁ , Marco M D Cominetti ₁ , David A Russell ₂ , Mark Searcey _{1,

2}

Affiliation

Solid-phase synthesis allowed the rapid generation of a peptide–drug conjugate. A peptide targeting the Thomsen-Friedenreich antigen (TFα) was conjugated to the alkylating subunit of the potent cytotoxin duocarmycin SA. The compound, containing a cathepsin B cleavable linker, was shown to be active and selective against TFα expressing tumor cell lines.

中文翻译：

靶向Thomsen-Friedenreich抗原的肽-杜卡姆结合物具有有效的选择性抗肿瘤活性。

固相合成可以快速生成肽-药物结合物。将靶向Thomsen-Friedenreich抗原（TFα）的肽与有效的细胞毒素Duocarmycin SA的烷基化亚基偶联。该化合物含有组织蛋白酶B可裂解的连接子，显示出对表达TFα的肿瘤细胞系具有活性和选择性。

更新日期：2020-07-15

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