Search results for " receptor"
showing 10 items of 5090 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…
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.
Identificación de TCRs reactivos contra neoantígenos tumorales en muestras de pacientes con CPNM mediante secuenciación de nueva generación. Implicac…
2021
A pesar del éxito de la inmunoterapia con los bloqueantes de los puntos del control inmune (ICBs) en el cáncer de pulmón, el porcentaje de pacientes que se beneficia de este tipo de tratamiento sigue siendo inferior al 30%, por lo que aún es necesario el desarrollo de nuevos posibles biomarcadores para una mejor selección de los pacientes. El objetivo principal del presente trabajo de tesis doctoral es caracterizar el repertorio de la cadena beta del receptor de células T (TCR-β) en sangre periférica y correlacionar con las variables demográficas, clínico-patológicas, predictivas y pronósticas en una cohorte de pacientes con cáncer de pulmón no microcítico (CPNM) en estadios avanzados trata…
Effect of ligand-binding on protein function
2014
Toll Like Receptors as Sensors of the Tumor Microbial Dysbiosis: Implications in Cancer Progression
2021
Microbiota is a complex ecosystem of active microorganisms resident in the body of mammals. Although the majority of these microorganisms resides at the distal gastrointestinal tract, high-throughput DNA sequencing technology have made possible to understand that several other tissues of the human body host their own microbiota, even those once considered sterile, such as lung tissue. These bacterial communities have important functions in maintaining a healthy body state and the host immune system has evolved multiple mechanisms by which maintaining a symbiotic relationship with the microbiota. The maintenance of this dialogue allows the induction of protective responses to pathogens and r…
Synthesis and biological evaluation of the antioxidant properties of new analogues of natural products with piperidine based structure and evaluation…
Targeting the Activin Receptor Signaling to Counteract the Multi-Systemic Complications of Cancer and Its Treatments
2021
Muscle wasting, i.e., cachexia, frequently occurs in cancer and associates with poor prognosis and increased morbidity and mortality. Anticancer treatments have also been shown to contribute to sustainment or exacerbation of cachexia, thus affecting quality of life and overall survival in cancer patients. Pre-clinical studies have shown that blocking activin receptor type 2 (ACVR2) or its ligands and their downstream signaling can preserve muscle mass in rodents bearing experimental cancers, as well as in chemotherapy-treated animals. In tumor-bearing mice, the prevention of skeletal and respiratory muscle wasting was also associated with improved survival. However, the definitive proof tha…
Mast cells as protectors of health.
2019
Mast cells (MCs), which are well known for their effector functions in T(H)2-skewed allergic and also autoimmune inflammation, have become increasingly acknowledged for their role in protection of health. It is now clear that they are also key modulators of immune responses at interface organs, such as the skin or gut. MCs can prime tissues for adequate inflammatory responses and cooperate with dendritic cells in T-cell activation. They also regulate harmful immune responses in trauma and help to successfully orchestrate pregnancy. This review focuses on the beneficial effects of MCs on tissue homeostasis and elimination of toxins or venoms. MCs can enhance pathogen clearance in many bacter…