Zirimwabagabo, Jean-Olivier; Jailani, Ameera B. A.; Avgoustou, Paris; Tozer, Matthew J.; Gibson, Karl R.; Glossop, Paul A.; Mills, James E. J.; Porter, Roderick A.; Blaney, Paul; Wang, Ning; Skerry, Timothy M.; Richards, Gareth O.; Harrity, Joseph P. A. published the artcile< Discovery of a First-In-Class Small Molecule Antagonist against the Adrenomedullin-2 Receptor: Structure-Activity Relationships and Optimization>, Product Details of C19H34O2, the main research area is spiroindenepyrrolopyridinyl acylaminoacetamide preparation selective adrenomedullin receptor antagonist antitumor agent; structure spiroindenepyrrolopyridinyl acylaminoacetamide inhibition adrenomedullin receptor selectivity.
Class B G-protein-coupled receptors (GPCRs) remain an underexploited target for drug development. The calcitonin receptor (CTR) family is particularly challenging, as its receptors are heteromers comprising two distinct components: the calcitonin receptor-like receptor (CLR) or calcitonin receptor (CTR) together with one of three accessory proteins known as receptor activity-modifying proteins (RAMPs). CLR/RAMP1 forms a CGRP receptor, CLR/RAMP2 forms an adrenomedullin-1 (AM1) receptor, and CLR/RAMP3 forms an adrenomedullin-2 (AM2) receptor. The CTR/RAMP complexes form three distinct amylin receptors. While the selective blockade of AM2 receptors would be therapeutically valuable, inhibition of AM1 receptors would cause clin. unacceptable increased blood pressure. We report here a systematic study of structure-activity relationships that has led to the development of first-in-class AM2 receptor antagonists such as I. These compounds exhibit therapeutically valuable properties with 1000-fold selectivity over the AM1 receptor. These results highlight the therapeutic potential of AM2 antagonists.
Journal of Medicinal Chemistry published new progress about Adrenomedullin receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study) (AM2 receptors). 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Product Details of C19H34O2.
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