Hendrikse, Erica R.; Liew, Lydia P.; Bower, Rebekah L.; Bonnet, Muriel; Jamaluddin, Muhammad A.; Prodan, Nicole; Richards, Keith D.; Walker, Christopher S.; Pairaudeau, Garry; Smith, David M.; Rujan, Roxana-Maria; Sudra, Risha; Reynolds, Christopher A.; Booe, Jason M.; Pioszak, Augen A.; Flanagan, Jack U.; Hay, Michael P.; Hay, Debbie L. published the artcile< Identification of Small-Molecule Positive Modulators of Calcitonin-like Receptor-Based Receptors>, Name: 3-Methoxy-2-methylbenzaldehyde, the main research area is adrenomedullin CLR calcitonin peptide RAMP allosteric modulator GPCRs.
Class B G protein-coupled receptors are highly therapeutically relevant but challenges remain in identifying suitable small-mol. drugs. The calcitonin-like receptor (CLR) in particular is linked to conditions such as migraine, cardiovascular disease, and inflammatory bowel disease. The CLR cannot act as a cell-surface receptor alone but rather must couple to one of three receptor activity-modifying proteins (RAMPs), forming heterodimeric receptors for the peptides adrenomedullin and calcitonin gene-related peptide. These peptides have extended binding sites across their receptors. This is one reason why there are few small-mol. ligands that can modulate these receptors. Here we describe small mols. that are able to pos. modulate the signaling of the CLR with all three RAMPs but are not active at the related calcitonin receptor. These compounds were selected from a β-arrestin recruitment screen, coupled with rounds of medicinal chem. to improve their activity. Translational potential is shown as the compounds can pos. modulate cAMP signaling in a vascular cell line model. Binding experiments do not support an extracellular domain binding site; however, mol. modeling reveals potential allosteric binding sites in multiple receptor regions. These are the first small-mol. pos. modulators described for the CLR:RAMP complexes.
ACS Pharmacology & Translational Science published new progress about Adrenomedullin receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 56724-03-9 belongs to class ethers-buliding-blocks, and the molecular formula is C9H10O2, Name: 3-Methoxy-2-methylbenzaldehyde.
Referemce:
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Ether | (C2H5)2O – PubChem