Conserved class B GPCR activation by a biased intracellular agonist
LH Zhao, Q He, Q Yuan, Y Gu, X He, H Shan, J Li… - Nature, 2023 - nature.com
Class B G-protein-coupled receptors (GPCRs), including glucagon-like peptide 1 receptor
(GLP1R) and parathyroid hormone 1 receptor (PTH1R), are important drug targets …
(GLP1R) and parathyroid hormone 1 receptor (PTH1R), are important drug targets …
Deciphering the role of glycosaminoglycans in GPCR signaling
S Savransky, AD White, JP Vilardaga - Cellular Signalling, 2024 - Elsevier
G protein-coupled receptors (GPCR) and glycosaminoglycans (GAGs) are two essential
components of the cell surface that regulate physiological processes in the body. GPCRs …
components of the cell surface that regulate physiological processes in the body. GPCRs …
Molecular recognition of two endogenous hormones by the human parathyroid hormone receptor-1
LH Zhao, Q Yuan, A Dai, X He, C Chen… - Acta Pharmacologica …, 2023 - nature.com
Parathyroid hormone (PTH) and PTH-related peptide (PTHrP) are two endogenous
hormones recognized by PTH receptor-1 (PTH1R), a member of class BG protein-coupled …
hormones recognized by PTH receptor-1 (PTH1R), a member of class BG protein-coupled …
Hormone Analogues with Unique Signaling Profiles from Replacement of α-Residue Triads with β/γ Diads
R Gibadullin, TW Kim, LML Tran… - Journal of the American …, 2023 - ACS Publications
We have applied an underexplored backbone modification strategy to generate new
analogues of peptides that activate two clinically important class B1 G protein-coupled …
analogues of peptides that activate two clinically important class B1 G protein-coupled …
Impact of secretin receptor homo-dimerization on natural ligand binding
KG Harikumar, SJ Piper, A Christopoulos… - Nature …, 2024 - nature.com
Class BG protein-coupled receptors can form dimeric complexes important for high potency
biological effects. Here, we apply pharmacological, biochemical, and biophysical techniques …
biological effects. Here, we apply pharmacological, biochemical, and biophysical techniques …
Backbone Modification Provides a Long-Acting Inverse Agonist of Pathogenic, Constitutively Active PTH1R Variants
Parathyroid hormone 1 receptor (PTH1R) plays a key role in mediating calcium homeostasis
and bone development, and aberrant PTH1R activity underlies several human diseases …
and bone development, and aberrant PTH1R activity underlies several human diseases …
Harnessing Aromatic‐Histidine Interactions through Synergistic Backbone Extension and Side Chain Modification
Peptide engineering efforts have delivered drugs for diverse human diseases. Side chain
alteration is among the most common approaches to designing new peptides for specific …
alteration is among the most common approaches to designing new peptides for specific …