Lifting the lid on GPCRs: the role of extracellular loops

M Wheatley, D Wootten, MT Conner… - British journal of …, 2012 - Wiley Online Library
GPCRs exhibit a common architecture of seven transmembrane helices (TMs) linked by
intracellular loops and extracellular loops (ECLs). Given their peripheral location to the site …

Allostery and biased agonism at class BG protein-coupled receptors

D Wootten, LJ Miller, C Koole, A Christopoulos… - Chemical …, 2017 - ACS Publications
Class BG protein-coupled receptors (GPCRs) respond to paracrine or endocrine peptide
hormones involved in control of bone homeostasis, glucose regulation, satiety, and gastro …

Cryo-EM structure of an activated VIP1 receptor-G protein complex revealed by a NanoBiT tethering strategy

J Duan, D Shen, XE Zhou, P Bi, Q Liu, Y Tan… - Nature …, 2020 - nature.com
Vasoactive intestinal polypeptide receptor (VIP1R) is a widely expressed class BG protein-
coupled receptor and a drug target for the treatment of neuronal, metabolic, and …

Structure of class B GPCR corticotropin-releasing factor receptor 1

K Hollenstein, J Kean, A Bortolato, RKY Cheng… - Nature, 2013 - nature.com
Structural analysis of class B G-protein-coupled receptors (GPCRs), cell-surface proteins
that respond to peptide hormones, has been restricted to the amino-terminal extracellular …

Polar transmembrane interactions drive formation of ligand-specific and signal pathway-biased family BG protein-coupled receptor conformations

D Wootten, J Simms, LJ Miller… - Proceedings of the …, 2013 - National Acad Sciences
Recently, the concept of ligand-directed signaling—the ability of different ligands of an
individual receptor to promote distinct patterns of cellular response—has gained much …

Dynamics of GLP-1R peptide agonist engagement are correlated with kinetics of G protein activation

G Deganutti, YL Liang, X Zhang, M Khoshouei… - Nature …, 2022 - nature.com
The glucagon-like peptide-1 receptor (GLP-1R) has broad physiological roles and is a
validated target for treatment of metabolic disorders. Despite recent advances in GLP-1R …

Calcitonin and calcitonin receptor‐like receptors: common themes with family B GPCRs?

J Barwell, JJ Gingell, HA Watkins… - British journal of …, 2012 - Wiley Online Library
The calcitonin receptor (CTR) and calcitonin receptor‐like receptor (CLR) are two of the 15
human family B (or Secretin‐like) GPCRs. CTR and CLR are of considerable biological …

Cryo-electron microscopy structure of the glucagon receptor with a dual-agonist peptide

R Chang, X Zhang, A Qiao, A Dai, MJ Belousoff… - Journal of Biological …, 2020 - ASBMB
Unimolecular dual agonists of the glucagon (GCG) receptor (GCGR) and glucagon-like
peptide-1 receptor (GLP-1R) are a new class of drugs that are potentially superior to GLP …

[HTML][HTML] Key interactions by conserved polar amino acids located at the transmembrane helical boundaries in Class B GPCRs modulate activation, effector specificity …

D Wootten, CA Reynolds, KJ Smith, JC Mobarec… - Biochemical …, 2016 - Elsevier
Class B GPCRs can activate multiple signalling effectors with the potential to exhibit biased
agonism in response to ligand stimulation. Previously, we highlighted key TM domain polar …

Similarity between class A and class B G-protein-coupled receptors exemplified through calcitonin gene-related peptide receptor modelling and mutagenesis studies

S Vohra, B Taddese, AC Conner… - Journal of The …, 2013 - royalsocietypublishing.org
Modelling class B G-protein-coupled receptors (GPCRs) using class A GPCR structural
templates is difficult due to lack of homology. The plant GPCR, GCR1, has homology to both …