In this video, we continue to focus on GPCR receptors, particularly on calcitonin gene-related peptide receptors. Calcitonin Gene-Related Peptide (CGRP) is a 37 amino acid neuropeptide. CGRP levels are elevated during migraine attacks. Dysregulation of CGRP, a potent vasodilator, is directly implicated in the pathogenesis of migraine. CGRP binds to and signals through the CGRP receptor (CGRP-R), a heterodimer containing the calcitonin receptor like receptor (CLR), a class B GPCR, and RAMP1, a receptor activity-modifying protein. Drugs act by blocking access to the peptide-binding cleft at the interface of CLR and RAMP1. These structures illustrate how small molecules bind to and modulate the activity of a class B GPCR, and highlight the challenges of designing potent receptor antagonists for the treatment of migraine and other class B GPCR-related diseases. Reference: Bucknell et al (2020). Structure-Based Drug Discovery of HTL22562: A Calcitonin Gene-Related Peptide Receptor Antagonist for Acute Treatment of Migraine. J Med Chem. 23;63(14):7906-7920. doi: DOWNLOAD NANOME FOR FREE Oculus: Steam: Viveport: SideQuest: SUPPORTED VR HEADSETS Oculus Rift Oculus Quest HTC Vive Complete list: CONNECT WITH US Twitter: LinkedIn: Facebook: Instagram: ABOUT NANOME Website: Step into Nanome and experience the world at the molecular level. From drug discovery to chemistry class, Nanome is a powerful tool for research and education. Visualize, design, and simulate chemical compounds, proteins, and nucleic acids like never before. Collaborate remotely in real-time, save workspaces, and share. Leading pharmaceutical and biotech companies use Nanome to accelerate drug discovery and collaborate with distributed teams across the globe. Educators at top universities use Nanome to teach chemistry in virtual reality, allowing students to explore shapes of proteins and drug compounds and to learn how these structures explain function. Be sure to also check out our blockchain platform, Matryx, which will serve as the backend IP tracking mechanism for Nanome. More info at
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