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CGRP Receptor
Calcitonin gene-related peptide (CGRP) is a 37-amino acid neuropeptide that is involved in different physiological processes in humans. CGRP is a peptide neurotransmitter that is produced in peripheral sensory neurons and numerous sites throughout the CNS. CGRP is generated by cleavage of a pro-peptide precursor and packaged into dense core vesicles for transport to axon terminals and other release sites within the neuron. The CGRP receptor is a complex of several proteins, each of which is required for the ligand specificity and function of the receptor. The CGRP receptor complex also includes two cytoplasmic proteins that associate with the CALCRL–RAMP1 heterodimer to mediate signal transduction.
Receptor-mediated increases in intracellular cAMP activate protein kinase A (PKA), which results in the phosphorylation of multiple downstream targets, including potassium-sensitive ATP channels (KATP channels), extracellular signal-related kinases (ERKs) and transcription factors such as cAMP-responsive element-binding protein (CREB).An important feature of CGRP signalling is the regulation and desensitization of the receptor following its activation by an agonist. The potent vasodilatory effects of CGRP in cerebral arteries fitted with the prevailing view at the time that cerebral vasodilation was an important component of headache. Since its description as playing a key role in the pathophysiology of migraine, our knowledge on CGRP has increased substantially, leading to a robust interest in targeting CGRP to treat migraine.
References
1.Bigal ME,et al. Br J Clin Pharmacol. 2015 Jun;79(6):886-95.
2.Edvinsson L,et al. Nat Rev Neurol. 2018 Jun;14(6):338-350.
Receptor-mediated increases in intracellular cAMP activate protein kinase A (PKA), which results in the phosphorylation of multiple downstream targets, including potassium-sensitive ATP channels (KATP channels), extracellular signal-related kinases (ERKs) and transcription factors such as cAMP-responsive element-binding protein (CREB).An important feature of CGRP signalling is the regulation and desensitization of the receptor following its activation by an agonist. The potent vasodilatory effects of CGRP in cerebral arteries fitted with the prevailing view at the time that cerebral vasodilation was an important component of headache. Since its description as playing a key role in the pathophysiology of migraine, our knowledge on CGRP has increased substantially, leading to a robust interest in targeting CGRP to treat migraine.
References
1.Bigal ME,et al. Br J Clin Pharmacol. 2015 Jun;79(6):886-95.
2.Edvinsson L,et al. Nat Rev Neurol. 2018 Jun;14(6):338-350.
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