Bifunctional epitope-agonist ligands of the bradykinin B2 receptor
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Lajos Gera
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 manner.
©2013 by Walter de Gruyter Berlin Boston
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- Pro-angiogenic effect of human kallikrein-related peptidase 12 (KLK12) in lung endothelial cells does not depend on kinin-mediated activation of B2 receptor
- Review
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- Research Articles/Short Communications
- Genes and Nucleic Acids
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Articles in the same Issue
- Masthead
- Masthead
- Guest Editorial
- Highlight: Kinin 2012 in Paris
- Highlight: Kinin 2012 in Paris
- Plasma kallikrein-kinin system and diabetic retinopathy
- Tissue kallikrein, blood pressure regulation, and hypertension: insight from genetic kallikrein deficiency
- Carboxypeptidase M augments kinin B1 receptor signaling by conformational crosstalk and enhances endothelial nitric oxide output
- Interactions between BdkrB2 and p53 genes in the developing kidney
- Further pharmacological evaluation of a novel synthetic peptide bradykinin B2 receptor agonist
- Role of kinin B2 receptors in opioid-induced hyperalgesia in inflammatory pain in mice
- Clinical impact of an angiotensin I-converting enzyme insertion/deletion and kinin B2 receptor +9/-9 polymorphisms in the prognosis of renal transplantation
- Bifunctional epitope-agonist ligands of the bradykinin B2 receptor
- Pro-angiogenic effect of human kallikrein-related peptidase 12 (KLK12) in lung endothelial cells does not depend on kinin-mediated activation of B2 receptor
- Review
- Mitochondrial pathways in sarcopenia of aging and disuse muscle atrophy
- Research Articles/Short Communications
- Genes and Nucleic Acids
- A genetic variant in the promoter region of miR-34b/c is associated with a reduced risk of colorectal cancer
- Protein Structure and Function
- SH3-mediated targeting of Wrch1/RhoU by multiple adaptor proteins
