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Re-engineering the Immune Response to Metastatic Cancer: Antibody-Recruiting Small Molecules Targeting the Urokinase Receptor
- Authors
- Rullo, Anthony F.; Fitzgerald, Kelly J.; Muthusamy, Viswanathan; Liu, Min; Yuan, Cai; Huang, Mingdong; Kim, Minsup; Cho, Art E.; Spiegel, David A.
- Issue Date
- 7-3월-2016
- Publisher
- WILEY-V C H VERLAG GMBH
- Keywords
- antitumor agents; cell recognition; drug design; immunology; medicinal chemistry
- Citation
- ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, v.55, no.11, pp.3642 - 3646
- Indexed
- SCIE
SCOPUS
- Journal Title
- ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
- Volume
- 55
- Number
- 11
- Start Page
- 3642
- End Page
- 3646
- ISSN
- 1433-7851
- Abstract
- Developing selective strategies to treat metastatic cancers remains a significant challenge. Herein, we report the first antibody-recruiting small molecule (ARM) that is capable of recognizing the urokinase-type plasminogen activator receptor (uPAR), a uniquely overexpressed cancer cell-surface marker, and facilitating the immune-mediated destruction of cancer cells. A co-crystal structure of the ARM-U2/uPAR complex was obtained, representing the first crystal structure of uPAR complexed with a non-peptide ligand. Finally, we demonstrated that ARM-U2 substantially suppresses tumor growth invivo with no evidence of weight loss, unlike the standard-of-care agent doxorubicin. This work underscores the promise of antibody-recruiting molecules as immunotherapeutics for treating cancer.
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