Novel Macrocyclic Antagonists of the CGRP Receptor Part 2: Stereochemical Inversion Induces an Unprecedented Binding Mode.
Sign Up to like & getrecommendations! Published in 2022 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.2c00400
Abstract: The diastereomeric macrocyclic calcitonin gene-related peptide (CGRP) antagonists HTL0029881 (3) and HTL0029882 (4), in which the stereochemistry of a spiro center is reversed, surprisingly demonstrate comparable potency. X-ray crystallographic characterization demonstrates that 3 binds to… read more here.
Keywords: macrocyclic antagonists; receptor part; antagonists cgrp; novel macrocyclic ... See more keywords
Real world considerations for newly approved CGRP receptor antagonists in migraine care
Sign Up to like & getrecommendations! Published in 2022 at "Expert Review of Neurotherapeutics"
DOI: 10.1080/14737175.2022.2049758
Abstract: ABSTRACT Introduction Migraine is the leading cause of years lived with disability in people under 50. Electrophysiological phenomena at the basis of prodromal and headache attack phases and of chronification processes involve calcitonin-gene related peptide… read more here.
Keywords: newly approved; migraine; cgrp receptor; real world ... See more keywords
Mechanistic Investigations Support Liver Safety of Ubrogepant
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DOI: 10.1093/toxsci/kfaa093
Abstract: Abstract Small-molecule calcitonin gene-related peptide (CGRP) receptor antagonists have demonstrated therapeutic efficacy for the treatment of migraine. However, previously investigated CGRP receptor antagonists, telcagepant and MK-3207, were discontinued during clinical development because of concerns about… read more here.
Keywords: cgrp receptor; telcagepant 3207; support liver; mechanistic investigations ... See more keywords
Comparing the Liver Safety Profiles of 4 Next-Generation CGRP Receptor Antagonists to the Hepatotoxic CGRP Inhibitor Telcagepant Using Quantitative Systems Toxicology Modeling
Sign Up to like & getrecommendations! Published in 2022 at "Toxicological Sciences"
DOI: 10.1093/toxsci/kfac051
Abstract: Abstract Calcitonin gene-related peptide (CGRP) signaling inhibitors have shown efficacy in both the acute and preventive treatment of migraine. Telcagepant, a first-generation CGRP receptor antagonist, was effective but failed in clinical trials due to hepatotoxicity.… read more here.
Keywords: generation cgrp; toxicology; generation; cgrp receptor ... See more keywords
Recent advances in targeting calcitonin gene-related peptide for the treatment of menstrual migraine
Sign Up to like & getrecommendations! Published in 2022 at "Medicine"
DOI: 10.1097/md.0000000000029361
Abstract: Abstract Menstrual migraine (MM) has a longer duration and higher drug resistance than non-perimenstrual migraine. Calcitonin gene-related peptide (CGRP) and CGRP receptors are expressed in the peripheral and central nervous systems throughout the trigeminovascular system.… read more here.
Keywords: calcitonin gene; migraine; cgrp; cgrp receptor ... See more keywords
Characterization of transit rates in the large intestine of mice following treatment with a CGRP antibody, CGRP receptor antibody, and small molecule CGRP receptor antagonists
Sign Up to like & getrecommendations! Published in 2022 at "Headache"
DOI: 10.1111/head.14336
Abstract: To characterize the effects of blocking calcitonin gene‐related peptide (CGRP) activity in a mouse model of gastrointestinal transport. read more here.
Keywords: transit rates; characterization transit; cgrp; cgrp receptor ... See more keywords
Blood Pressure in Migraine Patients Treated With Monoclonal Anti-CGRP (receptor) Antibodies: A Prospective Follow-up Study.
Sign Up to like & getrecommendations! Published in 2022 at "Neurology"
DOI: 10.1212/wnl.0000000000201008
Abstract: BACKGROUND AND OBJECTIVES Anti-CGRP (receptor) antibodies are approved as preventive treatment for migraine. Recent concerns have been raised after a retrospective analysis of post-marketing case reports of elevated BP associated with erenumab. In this prospective… read more here.
Keywords: receptor antibodies; cgrp receptor; blood pressure; anti cgrp ... See more keywords
Lipidated Calcitonin Gene-Related Peptide (CGRP) Peptide Antagonists Retain CGRP Receptor Activity and Attenuate CGRP Action In Vivo
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Pharmacology"
DOI: 10.3389/fphar.2022.832589
Abstract: Signaling through calcitonin gene-related peptide (CGRP) receptors is associated with pain, migraine, and energy expenditure. Small molecule and monoclonal antibody CGRP receptor antagonists that block endogenous CGRP action are in clinical use as anti-migraine therapies.… read more here.
Keywords: cgrp; peptide; cgrp action; cgrp receptor ... See more keywords
Gαs-Coupled CGRP Receptor Signaling Axis from the Trigeminal Ganglion Neuron to Odontoblast Negatively Regulates Dentin Mineralization
Sign Up to like & getrecommendations! Published in 2022 at "Biomolecules"
DOI: 10.3390/biom12121747
Abstract: An inflammatory response following dental pulp injury and/or infection often leads to neurogenic inflammation via the axon reflex. However, the detailed mechanism underlying the occurrence of the axon reflex in the dental pulp remains unclear.… read more here.
Keywords: ganglion neuron; cgrp receptor; receptor; mineralization ... See more keywords