Πλοήγηση ανά Θέμα "ligand binding"
Αποτελέσματα 1-7 από 7
-
Desensitization of cAMP accumulation via human β3-adrenoceptors expressed in human embryonic kidney cells by full, partial, and biased agonists
(2019)β3-Adrenoceptors couple not only to cAMP formation but, at least in some cell types, also to alternative signaling pathways such as phosphorylation of extracellular signal-regulated kinase (ERK). β3-Adrenoceptor agonists ... -
Functional expression of mammalian opioid receptors in insect cells and high-throughput screening platforms for receptor ligand mimetics
(2005)Lepidopteran cell lines have been engineered to constitutively express high levels of mouse δ opioid receptors either alone or in combination with human Gα16 protein. Biochemical and pharmacological studies demonstrate ... -
Nanomolar Inhibitors of Glycogen Phosphorylase Based on β- D -Glucosaminyl Heterocycles: A Combined Synthetic, Enzyme Kinetic, and Protein Crystallography Study
(2017)Aryl substituted 1-(β-d-glucosaminyl)-1,2,3-triazoles as well as C-β-d-glucosaminyl 1,2,4-triazoles and imidazoles were synthesized and tested as inhibitors against muscle and liver isoforms of glycogen phosphorylase (GP). ... -
Phytogenic polyphenols as glycogen phosphorylase inhibitors: The potential of triterpenes and flavonoids for glycaemic control in type 2 diabetes
(2017)Glycogen phosphorylase (GP) is a validated pharmaceutical target for the development of antihyperglycaemic agents. Phytogenic polyphenols, mainly flavonoids and pentacyclic triterpenes, have been found to be potent inhibitors ... -
Rapid effects of 17β-estradiol and progesterone on sheep visceral and parietal pleurae via a nitric oxide pathway
(2002)We investigated the effects of 17β-estradiol and progesterone on transepithelial electrical resistance (R TE) in sheep visceral and parietal pleurae. Specimens of intact pleurae from adult female sheep were used. The samples ... -
Sex hormone binding globulin of the plasma: Towards understanding of a new regulatory system in steroid hormone action
(1999)Sex hormone binding globulin (SHBG) is a protein that circulates in the plasma of many species and binds with high affinity to sex steroids in the human and primates, while it is androgen-binding protein in many animals ... -
Synthetic flavonoid derivatives targeting the glycogen phosphorylase inhibitor site: QM/MM-PBSA motivated synthesis of substituted 5,7-dihydroxyflavones, crystallography, in vitro kinetics and ex-vivo cellular experiments reveal novel potent inhibitors
(2020)Glycogen phosphorylase (GP) is an important target for the development of new anti-hyperglycaemic agents. Flavonoids are novel inhibitors of GP, but their mode of action is unspecific in terms of the GP binding sites ...