Nanobodies as Probes and Modulators of Cardiovascular G Protein-Coupled Receptors.
Understanding the activation of G protein-coupled receptors (GPCRs) is of paramount importance to the field of cardiovascular medicine due to the critical physiological roles of these receptors and their prominence as drug targets. Although many cardiovascular GPCRs have been extensively studied as model receptors for decades, new complexities in their regulation continue to emerge. As a result, there is an ongoing need to develop novel approaches to monitor and to modulate GPCR activation. In less than a decade, nanobodies, or recombinant single-domain antibody fragments from camelids, have become indispensable tools for interrogating GPCRs both in purified systems and in living cells. Nanobodies have gained traction rapidly due to their biochemical tractability and their ability to recognize defined states of native proteins. Here, we review how nanobodies have been adopted to elucidate the structure, pharmacology, and signaling of cardiovascular GPCRs, resolving long-standing mysteries and revealing unexpected mechanisms. We also discuss how advancing technologies to discover nanobodies with tailored specificities may expand the impact of these tools for both basic science and therapeutic applications.
Duke Scholars
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- Single-Domain Antibodies
- Signal Transduction
- Receptors, G-Protein-Coupled
- Cardiovascular System & Hematology
- 3214 Pharmacology and pharmaceutical sciences
- 3201 Cardiovascular medicine and haematology
- 1115 Pharmacology and Pharmaceutical Sciences
- 1102 Cardiorespiratory Medicine and Haematology
Citation
Published In
DOI
EISSN
Publication Date
Volume
Issue
Start / End Page
Location
Related Subject Headings
- Single-Domain Antibodies
- Signal Transduction
- Receptors, G-Protein-Coupled
- Cardiovascular System & Hematology
- 3214 Pharmacology and pharmaceutical sciences
- 3201 Cardiovascular medicine and haematology
- 1115 Pharmacology and Pharmaceutical Sciences
- 1102 Cardiorespiratory Medicine and Haematology