Probing Biochemical Mechanisms of Action of Muscarinic M3 Receptor Antagonists with Label-Free Whole Cell Assays

2012 ◽  
Vol 84 (19) ◽  
pp. 8232-8239 ◽  
Author(s):  
Huayun Deng ◽  
Chaoming Wang ◽  
Ming Su ◽  
Ye Fang
Keyword(s):  
Mechanisms Of Action ◽  
Label Free ◽  
Receptor Antagonists ◽  
Whole Cell ◽  
Cell Assays ◽  
M3 Receptor ◽  
Biochemical Mechanisms

Label-free whole-cell assays: expanding the scope of GPCR screening

2010 ◽  
Vol 15 (17-18) ◽  
pp. 704-716 ◽  
Author(s):  
Clay W Scott ◽  
Matthew F. Peters
Keyword(s):  
Label Free ◽  
Whole Cell ◽  
Cell Assays

scholarly journals Label-Free Whole Cell Biosensing for High-Throughput Discovery of Activators and Inhibitors Targeting G Protein-Activated Inwardly Rectifying Potassium Channels

ACS Omega ◽  
2018 ◽  
Vol 3 (11) ◽  
pp. 14814-14823 ◽  
Author(s):  
Katrin M. Krebs ◽  
Eva M. Pfeil ◽  
Katharina Simon ◽  
Manuel Grundmann ◽  
Felix Häberlein ◽  
...  
Keyword(s):  
Potassium Channels ◽  
G Protein ◽  
High Throughput ◽  
Label Free ◽  
Whole Cell ◽  
Inwardly Rectifying Potassium Channels ◽  
Inwardly Rectifying

Proglucagon-Derived Peptides: Mechanisms of Action and Therapeutic Potential

Physiology ◽  
2005 ◽  
Vol 20 (5) ◽  
pp. 357-365 ◽  
Author(s):  
Elaine M Sinclair ◽  
Daniel J. Drucker
Keyword(s):  
Type 2 Diabetes ◽  
Human Disease ◽  
Clinical Relevance ◽  
Therapeutic Potential ◽  
Mechanisms Of Action ◽  
Receptor Antagonists ◽  
Glucagon Receptor ◽  
Receptor Agonists ◽  
Glucagon Like Peptide

Glucagon is used for the treatment of hypoglycemia, and glucagon receptor antagonists are under development for the treatment of type 2 diabetes. Moreover, glucagon-like peptide (GLP)-1 and GLP-2 receptor agonists appear to be promising therapies for the treatment of type 2 diabetes and intestinal disorders, respectively. This review discusses the physiological, pharmacological, and therapeutic actions of the proglucagon-derived peptides, with an emphasis on clinical relevance of the peptides for the treatment of human disease.

scholarly journals Constitutive activity of the metabotropic glutamate receptor 2 explored with a whole-cell label-free biosensor

2018 ◽  
Vol 152 ◽  
pp. 201-210 ◽  
Author(s):  
Maarten L.J. Doornbos ◽  
Ilse Van der Linden ◽  
Liesbeth Vereyken ◽  
Gary Tresadern ◽  
Adriaan P. IJzerman ◽  
...  
Keyword(s):  
Glutamate Receptor ◽  
Metabotropic Glutamate Receptor ◽  
Constitutive Activity ◽  
Label Free ◽  
Whole Cell ◽  
Metabotropic Glutamate

Increasing the throughput of label-free cell assays to study the activation of G-protein-coupled receptors by using a serial agonist exposure protocol

2019 ◽  
Vol 11 (3) ◽  
pp. 99-108 ◽  
Author(s):  
J A Stolwijk ◽  
M Skiba ◽  
C Kade ◽  
G Bernhardt ◽  
A Buschauer ◽  
...  
Keyword(s):  
G Protein ◽  
Free Cell ◽  
G Protein Coupled Receptors ◽  
Label Free ◽  
Cell Assays ◽  
G Protein Coupled

scholarly journals A label-free optical whole-cell Escherichia coli biosensor for the detection of pyrethroid insecticide exposure

2019 ◽  
Vol 9 (1) ◽  
Author(s):  
Pinpunya Riangrungroj ◽  
Candace Spier Bever ◽  
Bruce D. Hammock ◽  
Karen M. Polizzi
Keyword(s):  
Escherichia Coli ◽  
Pyrethroid Insecticide ◽  
Label Free ◽  
Whole Cell ◽  
Insecticide Exposure

Concentration of glucocorticoid receptor sites in normal human lymphocytes.

1986 ◽  
Vol 32 (1) ◽  
pp. 80-83 ◽  
Author(s):  
A E Steiner ◽  
J L Wittliff
Keyword(s):  
Glucocorticoid Receptor ◽  
Human Lymphocytes ◽  
Normal Subjects ◽  
Mean Value ◽  
Whole Cell ◽  
Receptor Sites ◽  
Human T Cells ◽  
Cell Assays ◽  
Normal Human ◽  
The Mean

Abstract We used a whole-cell glucocorticoid receptor assay to examine characteristics of the glucocorticoid receptor in the lymphocytes of normal human donors. We measured binding of [3H]dexamethasone to the lymphocytes of four different donors on several different occasions; the variation about the mean for the assays was +/- 15%. Whole-cell assays in 15 normal subjects showed a mean value of 6.18 fmol/10(6) cells or 3722 sites per cell, with a somewhat higher level in men (7.67 fmol/10(6) cells, or 4620 sites per cell) than women (4.48 fmol/10(6) cells, or 2698 sites per cell). We saw no correlation between donor age and receptor values, in either group. Assays in which we used [3H]prednisolone demonstrated similar binding properties as with [3H]dexamethasone. The mean glucocorticoid receptor value for normal human T-cells from three donors was 2.52 fmol/10(6) cells, or 1518 sites per cell.

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