Search results for "Receptor"
showing 10 items of 6990 documents
Synthesis and Structure-Affinity Relationships of Spirocyclic Benzopyrans with Exocyclic Amino Moiety
2019
σ1 and/or σ2 receptors play a crucial role in pathological conditions such as pain, neurodegenerative disorders, and cancer. A set of spirocyclic cyclohexanes with diverse O-heterocycles and amino moieties (general structure III) was prepared and pharmacologically evaluated. In structure-activity relationships studies, the σ1 receptor affinity and σ1:σ2 selectivity were correlated with the stereochemistry, the kind and substitution pattern of the O-heterocycle, and the substituents at the exocyclic amino moiety. cis-configured 2-benzopyran cis-11b bearing a methoxy group and a tertiary cyclohexylmethylamino moiety showed the highest σ1 affinity ( Ki = 1.9 nM) of this series of compounds. In…
FUNCTIONAL STUDY ON THE ROLE OF TACHYKININS IN COLONIC PERISTALTIC ACTIVITY IN MICE
2009
Because the role of tachykinin receptors in colonic peristalsis remains incompletely understood, we studied the effect of tachykinin receptor antagonists on mouse colonic peristaltic activity. Peristaltic activity was assessed by quantifying the amplitude and interval of distension-induced pressure waves in proximal and distal colon segments of mice using a modified Trendelenburg set-up. We studied the effect of the NK1, NK2 and NK3 tachykinin receptor antagonists RP67580 (2 mM), nepadutant (1 mM) and SR142801 (0.3 mM) respectively. Gradual distension of proximal and distal colon segments induced repetitive rhythmic pressure waves which were blocked by tetrodotoxin (1 mM) and virtually abol…
Expression and characterization of the human sweet taste receptor expressed in a mammalian inducible cell line
2018
International audience; Sweet taste perception is mediated by a heterodimeric receptor composed of the two distinct protein subunits, TAS1R2 and TAS1R3. TAS1R2 and TAS1R3 subunits are members of the small family of class C GPCRs. Class C GPCRs share a large N-terminal domain (NTD) linked to the heptahelical transmembrane domain by a cysteine-rich region. TAS1R2/TAS1R3 is the primary receptor for a diverse range of sweet compounds including natural sugars, sweet amino acids, artificial sweeteners and plant sweet-tasting proteins. In order to understand the molecular mechanisms that govern receptor – ligand interactions and the relative contribution of the two subunits to the detection of swe…
Biomolecular and cellular approaches to study taste receptors
2012
Recombinant expression of the N-terminal domain of human T1R2 taste receptor: interaction with brazzein, a sweet-tasting protein
2014
Interaction of the n-terminal domain of human t1r2 taste receptor with brazzein, a sweet-tasting protein
2015
Brazzein is a small (6.5 kDa) sweet-tasting protein originating from the fruit of Pentadiplandra brazzeana, a plant found in West Africa. Brazzein like all classes of sweet compounds is perceived through the activation of the T1R2/T1R3 heterodimeric sweet-taste receptor. T1R2 and T1R3 subunits are members of the small family of class C G-protein coupled receptors (GPCRs). Class C GPCRs possess a large N-terminal domain (NTD) linked to seven transmembrane domain by a cysteine rich domain (CRD). The NTD of T1R2 (T1R2-NTD) has been shown to contain the primary binding site for most of the sweet ligands. However, brazzein has been shown to require CRD of human T1R3 for receptor activation [1]. …
Expression hétérologue, repliement in vitro et caractérisation biophysique du domaine N-terminal de la sous-unité T1R3 du récepteur humain au goût su…
2010
The sweet taste receptor is a heterodimer composed of two subunits called T1R2 and T1R3. Each subunit belongs to the class C of G protein-coupled receptors and is constituted by a large extracellular N-terminal domain (NTD) linked to the transmembrane domain by a cysteine-rich region. It has been shown that T1R2 and T1R3 NTDs are both able to bind natural sugars and sucralose with distinct affinities and undergo ligand-dependent conformational change (Nie et al., Curr Biol, 2005). However, the binding properties of T1R3 NTD and the relative contribution of the two subunits to the heterodimeric receptor function remained largely unknown. To characterize the binding properties of each subunit…
Role of odorant-binding proteins in Drosophila melanogaster chemosensory perception
2019
Chemoperception is used by animals to detect nutritive food and avoid toxic compounds. It also allows animals to identify suitable ecological niche and mating partners. Like many other insects, Drosophila melanogaster possesses a very sensitive chemosensory ability and can detect and discriminate a wide panel of semiochemicals. Chemosensory detection is mostly mediated by olfactory and gustatory systems involving several multigene chemoreceptor families. Volatile and non-volatile chemical compounds entering the sensory organ (sensillum) must be solubilized before being transported through the hydrophilic sensillum lymph bathing the dendrites of chemosensory neurons. These perireceptor event…
Chemicals and chemoreceptors: ecologically relevant signals driving behavior in Drosophila
2015
Insects encounter a vast repertoire of chemicals in their natural environment, which can signal positive stimuli like the presence of a food source, a potential mate, or a suitable oviposition site as well as negative stimuli such as competitors, predators, or toxic substances reflecting danger. The presence of specialized chemoreceptors like taste and olfactory receptors allows animals to detect chemicals at short and long distances and accordingly, trigger proper behaviors toward these stimuli. Since the first description of olfactory and taste receptors in Drosophila melanogaster 15 years ago, our knowledge on the identity, properties, and function of specific chemoreceptors has increase…
Taste perception: from molecule to eating behaviour
2020
The sense of taste has a role in human nutrition, it help to orient our food choices and avoid the ingestion of toxi compounds. Advances in molecular biology, cell biology an, biochemistry were used to identify and characterize the main taste receptors. The identification of these receptors allow a better understanding of the physiological processes tha govern taste perception. The presence of genetic polymorphisr in these receptors explains interindividual differences in tast perception.