与环开放链接器的特定位点酶依赖结合改善了针对HER2的ADC的安全性和稳定性

Lei Huang1, Gang Qin2,3, Chengcheng Gong4

  • 1National Key Laboratory of Immunity and Inflammation, National Clinical Research Center for Digestive Diseases, Changhai Clinical Research Unit, Department of Gastroenterology, The First Affiliated Hospital of Naval Medical University/Changhai Hospital, Naval Medical University, 168 Changhai Road, Shanghai, China.

Nature communications
|November 3, 2025
PubMed
概括

特定位点的依赖酶结合 (LDC) 提高了抗体-药物结合物的稳定性和安全性. 新的ADCs,GQ1001和GQ1005,在耐火的HER2阳性癌症中显示出有效性,毒性降低.

相关概念视频

Ligand Binding and Linkage00:49

Ligand Binding and Linkage

Allosteric proteins have more than one ligand binding site; the binding of a ligand to any of these sites influences the binding of ligands to the other sites. When a protein is allosteric, its binding sites are called coupled or linked.  In the case of enzymes, the site that binds to the substrate is known as the active site and the other site is known as the regulatory site. When a ligand binds to the regulatory site, this leads to conformational changes in the protein that can influence...
5.5K
Conservative Site-specific Recombination and Phase Variation02:53

Conservative Site-specific Recombination and Phase Variation

Because the DNA segments are cut and reorganized in a direction-specific manner, site-specific recombination has emerged as an efficient genetic engineering technique. Flippase and Cyclization recombinases or Flp and Cre, respectively, are two members of the tyrosine recombinase family derived from bacteriophages, that are used to mediate site-specific DNA insertions, deletions, and targeted expression of proteins in mammalian cell lines.
The recognition sites for Cre recombinase called LoxP...
6.6K