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http://dx.doi.org/10.1113/jphysiol.1949.sp004445 | DOI Listing |
SLAS Discov
September 2024
Department of Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, Scottsdale, AZ, USA. Electronic address:
Agonists of the secretin receptor have potential applications for diseases of the cardiovascular, gastrointestinal, and metabolic systems, yet no clinically-active non-peptidyl agonists of this receptor have yet been developed. In the current work, we have identified a new small molecule lead compound with this pharmacological profile. We have prepared and characterized a systematic structure-activity series around this thiadiazole scaffold to better understand the molecular determinants of its activity.
View Article and Find Full Text PDFCell Mol Biol Lett
January 2024
Department of Gastroenterology and Hepatology, Erasmus MC University Medical Center, PO Box 2040, 3000CA, Rotterdam, The Netherlands.
Background: Loss of CFTR-dependent anion and fluid secretion in the ducts of the exocrine pancreas is thought to contribute to the development of pancreatitis, but little is known about the impact of inflammation on ductal CFTR function. Here we used adult stem cell-derived cell cultures (organoids) obtained from porcine pancreas to evaluate the effects of pro-inflammatory cytokines on CFTR function.
Methods: Organoids were cultured from porcine pancreas and used to prepare ductal epithelial monolayers.
Acta Pharm Sin B
February 2021
Shanghai Engineering Research Center of ImmunoTherapeutics, School of Pharmacy, Fudan University, Shanghai 201203, China.
Dendritic cell-based cancer vaccines (DC vaccines) have been proved efficient and safe in immunotherapy of various cancers, including melanoma, ovarian and prostate cancer. However, the clinical responses were not always satisfied. Here we proposed a novel strategy to prepare DC vaccines.
View Article and Find Full Text PDFFront Mol Neurosci
January 2021
Laboratory of Endocrine Neurobiology, Institute of Experimental Medicine, Budapest, Hungary.
Rising serum estradiol triggers the surge release of gonadotropin-releasing hormone (GnRH) at late proestrus leading to ovulation. We hypothesized that proestrus evokes alterations in peptidergic signaling onto GnRH neurons inducing a differential expression of neuropeptide-, growth factor-, and orphan G-protein-coupled receptor (GPCR) genes. Thus, we analyzed the transcriptome of GnRH neurons collected from intact, proestrous and metestrous GnRH-green fluorescent protein (GnRH-GFP) transgenic mice using Affymetrix microarray technique.
View Article and Find Full Text PDFJ Struct Biol
June 2021
Laboratory of Biomolecular Research, Paul Scherrer Institut, Förschunggstrasse 111, 5232 Villigen, Switzerland; Department of Biology, ETH Zürich, Wolfgang-Pauli-Strasse 27, Zürich 8093, Switzerland.
G-protein coupled receptors (GPCRs) are among the most versatile signal transducers in the cell. Once activated, GPCRs sample a large conformational space and couple to G-proteins to initiate distinct signaling pathways. The dynamical behavior of GPCR-G-protein complexes is difficult characterize structurally, and it might hinder obtaining routine high-resolution density maps in single-particle reconstructions.
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