排序方式: 共有44条查询结果,搜索用时 0 毫秒
41.
42.
43.
Zhen Yang Sheng Jiang Feng Li Yatao Qiu Jianhua Gu Roderic I. Pettigrew Mauro Ferrari Dale J. Hamilton Zheng Li 《Angewandte Chemie (Weinheim an der Bergstrasse, Germany)》2019,131(16):5326-5330
Interaction of multiple entities and receptors, or multivalency is widely applied to achieve high affinity ligands for diagnostic and therapeutic purposes. However, lack of knowledge on receptor distribution in living subjects remains a challenge for rational structure design. Herein, we develop a force measurement platform to probe the distribution and separation of the cell surface vascular endothelial growth factor receptors (VEGFR) in live cells, and use this to assess the geometry of appropriate linkers for distinct multivalent binding modes. A tetravalent lead ZD‐4, which was developed from an antitumor drug ZD6474 (Vandetanib) with combined hybrid binding effects, yielded a 2000‐fold improvement in the binding affinity to VEGFR with IC50 value of 25 pm . We confirmed the improved affinity by the associated increase of tumor uptake in the VEGFR‐targeting positron emission tomography (PET) imaging using U87 tumor xenograft mouse model. 相似文献
44.