Search Results - "Lu, Jenny Ying Lin"
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G-protein-coupled receptor 35 is a target of the asthma drugs cromolyn disodium and nedocromil sodium
Published in Pharmacology (01-01-2010)“…We report that the asthma drugs cromolyn disodium and nedocromil sodium are potent G-protein-coupled receptor 35 (GPR35) agonists. We utilized calcium flux and…”
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AMG 837: a novel GPR40/FFA1 agonist that enhances insulin secretion and lowers glucose levels in rodents
Published in PloS one (08-11-2011)“…Agonists of GPR40 (FFA1) have been proposed as a means to treat type 2 diabetes. Through lead optimization of a high throughput screening hit, we have…”
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The psoriasis drug monomethylfumarate is a potent nicotinic acid receptor agonist
Published in Biochemical and biophysical research communications (31-10-2008)“…Nicotinic acid has been used for several decades to treat dyslipidemia. In mice, the lipid-lowing effect of nicotinic acid is mediated by the Gi coupled…”
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Discovery and Optimization of Substituted 1-(1-Phenyl-1H-pyrazol-3-yl)methanamines as Potent and Efficacious Type II Calcimimetics
Published in Journal of medicinal chemistry (12-11-2009)“…Our efforts to discover potent, orally bioavailable type II calcimimetic agents for the treatment of secondary hyperparathyroidism focused on the development…”
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Effect of the calcimimetic R-568 [3-(2-chlorophenyl)-N-((1R)-1-(3-methoxyphenyl)ethyl)-1-propanamine] on correcting inactivating mutations in the human calcium-sensing receptor
Published in The Journal of pharmacology and experimental therapeutics (01-12-2009)“…Over 257 mutations in the human calcium-sensing receptor (hCaSR) gene have been reported. Heterozygous inactivating mutations can result in familial…”
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AMG 837: A potent, orally bioavailable GPR40 agonist
Published in Bioorganic & medicinal chemistry letters (15-01-2012)“…The discovery that certain long chain fatty acids potentiate glucose stimulated insulin secretion through the previously orphan receptor GPR40 sparked interest…”
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Metabolism-guided discovery of a potent and orally bioavailable urea-based calcimimetic for the treatment of secondary hyperparathyroidism
Published in Bioorganic & medicinal chemistry letters (15-12-2013)“…A series of urea based calcimimetics was optimized for potency and oral bioavailability. Crucial to this process was overcoming the poor pharmacokinetic…”
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The discovery of an orally efficacious positive allosteric modulator of the calcium sensing receptor containing a dibenzylamine core
Published in Bioorganic & medicinal chemistry letters (15-09-2010)“…Compound 22 suppressed plasma PTH levels relative to vehicle when dosed orally in a rat pharmacodynamic model. The discovery of a series of novel and orally…”
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Discovery of a calcimimetic with differential effects on parathyroid hormone and calcitonin secretion
Published in The Journal of pharmacology and experimental therapeutics (01-06-2011)“…Calcimimetics are positive allosteric modulators to the calcium-sensing receptor (CaSR). Activation of the CaSR inhibits the secretion of parathyroid hormone…”
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