Publications by authors named "Chuan-Cheng Yang"
Structural basis of ligand recognition and activation of the histamine receptor family.
Nat Commun
September 2024
Article Synopsis
- - Histamine plays a key role in various bodily functions like allergic reactions, wakefulness, and gastric acid secretion, and it works through four different histamine receptors.
- - The study analyzes 9 cryo-electron microscopy structures of these receptors bound to different G protein types and agonists, revealing important details about how histamine binds and the nuanced differences in receptor interactions.
- - Findings include specific motifs for ligand recognition and key residues for selectivity, providing a framework for designing targeted drugs that can effectively interact with these histamine receptors.
Adhesion G protein-coupled receptors (aGPCRs) constitute an evolutionarily ancient family of receptors that often undergo autoproteolysis to produce α and β subunits. A tethered agonism mediated by the 'Stachel sequence' of the β subunit has been proposed to have central roles in aGPCR activation. Here we present three cryo-electron microscopy structures of aGPCRs coupled to the G heterotrimer.
View Article and Find Full Text PDFLigand recognition and allosteric regulation of DRD1-Gs signaling complexes.
Cell
February 2021
Dopamine receptors, including D1- and D2-like receptors, are important therapeutic targets in a variety of neurological syndromes, as well as cardiovascular and kidney diseases. Here, we present five cryoelectron microscopy (cryo-EM) structures of the dopamine D1 receptor (DRD1) coupled to Gs heterotrimer in complex with three catechol-based agonists, a non-catechol agonist, and a positive allosteric modulator for endogenous dopamine. These structures revealed that a polar interaction network is essential for catecholamine-like agonist recognition, whereas specific motifs in the extended binding pocket were responsible for discriminating D1- from D2-like receptors.
View Article and Find Full Text PDF