I found the field of Pharmacology & Pharmacy very interesting. Saw the article Identification of Small-Molecule Positive Modulators of Calcitonin-like Receptor-Based Receptors published in 2020. Recommanded Product: Indolin-2-one, Reprint Addresses Hay, DL (corresponding author), Univ Auckland, Sch Biol Sci, Auckland 1010, New Zealand.; Flanagan, JU; Hay, MP; Hay, DL (corresponding author), Univ Auckland, Maurice Wilkins Ctr Mol Biodiscovery, Auckland 1010, New Zealand.; Flanagan, JU; Hay, MP (corresponding author), Univ Auckland, Auckland Canc Soc Res Ctr, Auckland 1023, New Zealand.. The CAS is 59-48-3. Through research, I have a further understanding and discovery of Indolin-2-one
Class B G protein-coupled receptors are highly therapeutically relevant but challenges remain in identifying suitable small-molecule 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-molecule ligands that can modulate these receptors. Here we describe small molecules that are able to positively 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 beta-arrestin recruitment screen, coupled with rounds of medicinal chemistry to improve their activity. Translational potential is shown as the compounds can positively modulate cAMP signaling in a vascular cell line model. Binding experiments do not support an extracellular domain binding site; however, molecular modeling reveals potential allosteric binding sites in multiple receptor regions. These are the first small-molecule positive modulators described for the CLR:RAMP complexes.
Welcome to talk about 59-48-3, If you have any questions, you can contact Hendrikse, ER; Liew, LP; Bower, RL; Bonnet, M; Jamaluddin, MA; Prodan, N; Richards, KD; Walker, CS; Pairaudeau, G; Smith, DM; Rujan, RM; Sudra, R; Reynolds, CA; Booe, JM; Pioszak, AA; Flanagan, JU; Hay, MP; Hay, DL or send Email.. Recommanded Product: Indolin-2-one
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