Bifunctional epitope-agonist ligands of the bradykinin B2 receptor
| Authors: | Gera, Lajos; Roy, Caroline; Marceau, François |
| Abstract: | Two bradykinin (BK) B2 receptor agonists N-terminally extended with the myc epitope were synthesized and evaluated: myc-KPG-BK and myc-KGP-B-9972. The latter was modeled on the inactivation-resistant agonist B-9972 (D-Arg0, Hyp3, Igl5, Oic7, Igl8-BK) and is also resistant to endosomal inactivation. Despite a large loss of affinity relative to the parent peptide, the tagged analogs are conventional agonists in the umbilical vein contractility assay and compete for [3H]BK binding at the rabbit B2 receptor. Endocytosed myc-KGP-B-9972 most effectively carried AlexaFluor-488-conjugated anti-myc monoclonal antibodies into intact cells expressing the B2 receptor. Results support the prospects of functionally-active cargoes entering cells in a pharmacologically controlled manne |
| Document Type: | Article de recherche |
| Issue Date: | 2 February 2013 |
| Open Access Date: | 17 November 2017 |
| Document version: | AM |
| Permalink: | http://hdl.handle.net/20.500.11794/15875 |
| This document was published in: | Biological Chemistry, Vol. 394 (3), (2013) https://doi.org/10.1515/hsz-2012-0286 De Gruyter |
| Alternative version: | 10.1515/hsz-2012-0286 23241671 |
| Collection: | Articles publiés dans des revues avec comité de lecture |
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