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A Conjugate of an Anti-Epidermal Growth Factor Receptor (EGFR) VHH and a Cell-Penetrating Peptide Drives Receptor Internalization and Blocks EGFR Activation
ChemBioChem ( IF 2.6 ) Pub Date : 2017-11-07 06:00:30 , DOI: 10.1002/cbic.201700444
Sanne A. M. van Lith 1 , Dirk van den Brand 2, 3 , Rike Wallbrecher 2 , Sander M. J. van Duijnhoven 1 , Roland Brock 2 , William P. J. Leenders 1, 2
Affiliation  

On target: A cell-penetrating peptide (CPP) is conjugated to a recombinant llama single-domain antibody (VHH) against the epidermal growth factor receptor (EGFR) through chemoselective sortase A mediated coupling. This conjugate targets the EGFR for efficient internalization into the cell and blocks activation by the ligand; thus providing a novel modality for targeted downregulation of oncogenic membrane receptors in cancer therapy.

中文翻译:

抗表皮生长因子受体(EGFR)VHH和细胞穿透肽的共轭物驱动受体内在化并阻止EGFR激活

目标:通过化学选择性分选酶A介导的偶联,将细胞穿透肽(CPP)与针对表皮生长因子受体(EGFR)的重组美洲驼单域抗体(VHH)偶联。该缀合物靶向EGFR,以有效地内化到细胞中并阻断配体的激活。因此为癌症治疗中致癌膜受体的靶向下调提供了新的方法。
更新日期:2017-11-07
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