Bifunctional epitope-agonist ligands of the bradykinin B2 receptor

Authors: Gera, Lajos; Roy, CarolineMarceau, 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
This document was published in: Biological Chemistry, Vol. 394 (3), (2013)
De Gruyter
Alternative version: 10.1515/hsz-2012-0286
Collection:Articles publiés dans des revues avec comité de lecture

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