Reagents and models for detecting endogenous GLP1R and GIPR

J Ast, J Broichhagen, DJ Hodson - EBioMedicine, 2021 - thelancet.com
Abstract Glucagon-like peptide-1 receptor (GLP1R) agonists target the GLP1R, whereas
dual GLP1R/gastric inhibitory polypeptide receptor (GIPR) agonists target both the GLP1R …

Emerging modes of regulation of neuromodulatory G protein-coupled receptors

AJ Gonzalez-Hernandez, H Munguba, J Levitz - Trends in Neurosciences, 2024 - cell.com
In the nervous system, G protein-coupled receptors (GPCRs) control neuronal excitability,
synaptic transmission, synaptic plasticity, and, ultimately, behavior through spatiotemporally …

N-Methyl deuterated rhodamines for protein labelling in sensitive fluorescence microscopy

K Roßmann, KC Akkaya, P Poc, C Charbonnier… - Chemical …, 2022 - pubs.rsc.org
Rhodamine fluorophores are setting benchmarks in fluorescence microscopy. Herein, we
report the deuterium (d12) congeners of tetramethyl (silicon) rhodamine, obtained by …

Revealing the tissue-level complexity of endogenous glucagon-like peptide-1 receptor expression and signaling

J Ast, D Nasteska, NHF Fine, DJ Nieves… - Nature …, 2023 - nature.com
The glucagon-like peptide-1 receptor (GLP1R) is a class BG protein-coupled receptor
(GPCR) involved in glucose homeostasis and food intake. GLP1R agonists (GLP1RA) are …

DFT‐Guided Discovery of Ethynyl‐Triazolyl‐Phosphinates as Modular Electrophiles for Chemoselective Cysteine Bioconjugation and Profiling

CE Stieger, Y Park, MAR de Geus… - Angewandte Chemie …, 2022 - Wiley Online Library
We report the density functional theory (DFT) guided discovery of ethynyl‐triazolyl‐
phosphinates (ETPs) as a new class of electrophilic warheads for cysteine selective …

Peptide-coated polycaprolactone-benzalkonium chloride nanocapsules for targeted drug delivery to the pancreatic β-cell

J Collins, JM Barra, K Holcomb, A Ocampo… - ACS Applied Bio …, 2024 - ACS Publications
Targeting current therapies to treat or prevent the loss of pancreatic islet β-cells in Type 1
Diabetes (T1D) may provide improved efficacy and reduce off-target effects. Current efforts …

[HTML][HTML] GLP1R and GIPR expression and signaling in pancreatic alpha cells, beta cells and delta cells

AH Shilleh, K Viloria, J Broichhagen, JE Campbell… - Peptides, 2024 - Elsevier
Abstract Glucagon-like peptide-1 receptor (GLP1R) and glucose-dependent insulinotropic
polypeptide receptor (GIPR) are transmembrane receptors involved in insulin, glucagon and …

Multicolor, Cell-Impermeable, and High Affinity BACE1 Inhibitor Probes Enable Superior Endogenous Staining and Imaging of Single Molecules

F Stockinger, P Poc, A Möhwald, S Karch… - Journal of Medicinal …, 2024 - ACS Publications
The prevailing but not undisputed amyloid cascade hypothesis places the β-site of APP
cleaving enzyme 1 (BACE1) center stage in Alzheimer′ s Disease pathogenesis. Here, we …

DFT‐basierte Entdeckung von Ethynyl‐Triazolyl‐Phosphinaten als modulare Elektrophile für die chemoselektive Cystein‐Biokonjugation und Profilierung

CE Stieger, Y Park, MAR de Geus, D Kim… - Angewandte …, 2022 - Wiley Online Library
Wir berichten über eine Dichtefunktionaltheorie (DFT)‐basierte Entdeckung von Ethinyl‐
Triazolyl‐Phosphinaten (ETP) als eine neue Klasse elektrophiler Verbindungen für die …

Dynamic regulation of pancreatic β cell function and gene expression by the SND1 coregulator in vitro

S Kanojia, RK Davidson, JM Conley, J Xu, M Osmulski… - Islets, 2023 - Taylor & Francis
The pancreatic β cell synthesizes, packages, and secretes insulin in response to glucose-
stimulation to maintain blood glucose homeostasis. Under diabetic conditions, a subset of β …