Soluble PD-L1 generated by endogenous retroelement exaptation is a receptor antagonist
Immune regulation is a finely balanced process of positive and negative signals. PD-L1 and its receptor PD-1 are critical regulators of autoimmune, antiviral and antitumoural T cell responses.
Kevin W Ng+6 more
doaj +1 more source
Interaction of GABA and Excitatory Amino Acids in the Basolateral Amygdala: Role in Cardiovascular Regulation [PDF]
Activation of the amygdala in rats produces cardiovascular changes that include increases in heart rate and arterial pressure as well as behavioral changes characteristic of emotional arousal.
Cook, Jennifer C.+3 more
core +2 more sources
Involvement of central opiate receptors in modulation of centrally administered oxytocin-induced antinociception [PDF]
Objective(s): Oxytocin is involved in modulation of many brain-mediated functions. In the present study, we investigated the central effects of oxytocin and its receptor antagonist, atosiban on inflammatory pain.
Amir Erfanparast+2 more
doaj +1 more source
Rimegepant, an Oral Calcitonin Gene-Related Peptide Receptor Antagonist, for Migraine.
BACKGROUND Calcitonin gene-related peptide receptor has been implicated in the pathogenesis of migraine. Rimegepant is an orally administered, small-molecule, calcitonin gene-related peptide receptor antagonist that may be effective in acute migraine ...
R. Lipton+9 more
semanticscholar +1 more source
Non-equivalence of key positively charged residues of the free fatty acid 2 receptor in the recognition and function of agonist versus antagonist ligands [PDF]
Short chain fatty acids (SCFAs) are produced in the gut by bacterial fermentation of poorly digested carbohydrates. A key mediator of their actions is the G protein-coupled Free Fatty Acid 2 (FFA2) receptor and this has been suggested as a therapeutic ...
Hansen, Anders Højgaard+6 more
core +1 more source
The relevance of theobromine for the beneficial effects of cocoa consumption
Cocoa consumption began in America and in the mid 16th Century it quickly spread to Europe. Beyond being considered a pleasant habit due to its rich sweet lingering taste, chocolate was considered a good nutrient and even a medicine.
Eva eMartínez-Pinilla+2 more
doaj +1 more source
Chemokine G-protein coupled receptors are validated drug targets for many diseases, including cancer, neurological, and inflammatory disorders. Despite much time and effort spent on therapeutic development, very few chemokine receptor antagonists are ...
Patrick Grudzien+3 more
doaj +1 more source
The Effects of Serotonin Receptor Antagonists on Contraction and Relaxation Responses Induced by Electrical Stimulation in the Rat Small Intestine [PDF]
Background: The main source of 5-HT in body is in enterchromafin cells of intestine, different studies mentioned different roles for endogenous 5-HT and receptors involved and it is not clearified the mechanism of action of endogenous 5-HT. Objectives:
Bianchi C+33 more
core +1 more source
Fluorescent ligand for human progesterone receptor imaging in live cells. [PDF]
We employed molecular modeling to design and then synthesize fluorescent ligands for the human progesterone receptor. Boron dipyrromethene (BODIPY) or tetramethylrhodamine were conjugated to the progesterone receptor antagonist RU486 (Mifepristone ...
Baker, Michael E+5 more
core +1 more source
Perampanel inhibition of AMPA receptor currents in cultured hippocampal neurons. [PDF]
Perampanel is an aryl substituted 2-pyridone AMPA receptor antagonist that was recently approved as a treatment for epilepsy. The drug potently inhibits AMPA receptor responses but the mode of block has not been characterized.
Chen, Chao-Yin+3 more
core +3 more sources