• Publications
  • Influence
Structural mechanism of ligand activation in human calcium-sensing receptor
Human calcium-sensing receptor (CaSR) is a G-protein-coupled receptor (GPCR) that maintains extracellular Ca2+ homeostasis through the regulation of parathyroid hormone secretion. It functions as aExpand
  • 96
  • 12
  • PDF
The S100B/RAGE Axis in Alzheimer's Disease
Increasing evidence suggests that the small EF-hand calcium-binding protein S100B plays an important role in Alzheimer's disease. Among other evidences are the increased levels of both S100B and itsExpand
  • 58
  • 7
  • PDF
Autocrine selection of a GLP-1R G-protein biased agonist with potent antidiabetic effects
Glucagon-like peptide-1 (GLP-1) receptor (GLP-1R) agonists have emerged as treatment options for type 2 diabetes mellitus (T2DM). GLP-1R signals through G-protein-dependent, and G-protein-independentExpand
  • 54
  • 3
Development of a high-throughput screening-compatible cell-based functional assay to identify small molecule probes of the galanin 3 receptor (GalR3).
The galanin 3 receptor (GalR3) belongs to the large G protein-coupled receptor (GPCR) family of proteins. GalR3 and two other closely related receptors, GalR1 and GalR2, together with theirExpand
  • 9
  • 2
Structural basis for auxiliary subunit KCTD16 regulation of the GABAB receptor
  • Hao Zuo, I. Glaaser, +12 authors Q. Fan
  • Chemistry, Medicine
  • Proceedings of the National Academy of Sciences
  • 10 April 2019
Significance Human GABAB receptor inhibits the activity of neurons in the brain. Malfunction of the receptor is associated with various neurological and mood disorders, including spasticity,Expand
  • 8
  • 1
GABAB receptor allosteric modulators exhibit pathway‐dependent and species‐selective activity
Positive modulation of the GABAB receptor (GABABR) represents a potentially useful therapeutic approach for the treatment of nicotine addiction. The positive allosteric modulators (PAMs) of GABABRExpand
  • 8
  • 1
O-GlcNAc engineering of GPCR peptide-agonists improves their stability and in vivo activity.
Peptide agonists of GPCRs and other receptors are powerful signaling molecules with high potential as biological tools and therapeutics, but they are typically plagued by instability and shortExpand
  • 2
  • 1
Different potencies of angiotensin receptor blockers at suppressing adrenal β-Arrestin1-dependent post-myocardial infarction hyperaldosteronism.
Aldosterone is 1 of the various hormones with detrimental functions for the failing heart, whose circulating levels are elevated post-myocardial infarction (MI) and in patients with chronic heartExpand
  • 28
  • PDF
Suppression of adrenal βarrestin1-dependent aldosterone production by ARBs: head-to-head comparison
The known angiotensin II (AngII) physiological effect of aldosterone synthesis and secretion is mediated by either Gq/11 proteins or βarrestin1 (βarr1), both of which can couple to its type 1Expand
  • 29
Structure–activity relationship study of angiotensin II analogs in terms of β‐arrestin‐dependent signaling to aldosterone production
The known angiotensin II (AngII) physiological effect of aldosterone synthesis and secretion induction, a steroid hormone that contributes to the pathology of postmyocardial infarction (MI) heartExpand
  • 16