Genetically Encoded Photo-cross-linkers Map the Binding Site of an Allosteric Drug on a G Protein-Coupled Receptor [PDF]
, 2012 G protein-coupled receptors (GPCRs) are dynamic membrane proteins that bind extracellular molecules to transduce signals. Although GPCRs represent the largest class of therapeutic targets, only a small percentage of their ligand-binding sites are ...
Abrol, Ravinder +5 more
core +1 more source
The Role of the Apelin/APJ System in the Regulation of Liver Disease
Frontiers in Pharmacology, 2017 Apelin is an endogenous peptide that is a ligand for the APJ receptor (angiotensin II receptor like-1, AT-1). The apelin/APJ system is distributed in diverse periphery organ tissues.
Wei-Dong Chen +4 more
doaj +1 more source
Analgesia induced by the epigenetic drug, L-acetylcarnitine, outlasts the end of treatment in mouse models of chronic inflammatory and neuropathic pain [PDF]
, 2017 Background: L-acetylcarnitine, a drug marketed for the treatment of chronic pain, causes analgesia by epigenetically up-regulating type-2 metabotropic glutamate (mGlu2) receptors in the spinal cord.
Battaglia, Giuseppe +10 more
core +1 more source
mGluR5 antagonism inhibits cocaine reinforcement and relapse by elevation of extracellular glutamate in the nucleus accumbens via a CB1 receptor mechanism. [PDF]
, 2018 Metabotropic glutamate receptor 5 (mGluR5) antagonism inhibits cocaine self-administration and reinstatement of drug-seeking behavior. However, the cellular and molecular mechanisms underlying this action are poorly understood.
Bi, Guo-Hua +9 more
core +2 more sources
eLife, 2020 By analyzing and simulating inactive conformations of the highly homologous dopamine D2 and D3 receptors (D2R and D3R), we find that eticlopride binds D2R in a pose very similar to that in the D3R/eticlopride structure but incompatible with the D2R ...
J Robert Lane +10 more
doaj +1 more source
Caenorhabditis elegans muscle Cys-loop receptors as novel targets of terpenoids with potential anthelmintic activity [PDF]
, 2019 The anthelmintic treatment of nematode infections remains the pillar of worm control in both human and veterinary medicine. Since control is threatened by the appearance of drug resistant nematodes, there is a need to develop novel compounds, among which
Bouzat, Cecilia Beatriz +2 more
core +1 more source
Drug‐resistant epilepsy: Drug target hypothesis and beyond the receptors
Epilepsia Open, 2022 Epilepsy is a chronic neurological disorder that affects more than 50 million people worldwide. Despite a recent introduction of antiseizure drugs for the treatment of epileptic seizures, one‐third of these patients suffer from drug‐resistant epilepsy ...
Daniel Fonseca‐Barriendos +5 more
doaj +1 more source
Interplay of miRNAs and Canonical Wnt Signaling Pathway in Hepatocellular Carcinoma
Frontiers in Pharmacology, 2018 Hepatocellular carcinoma is one of the leading causes of cancer death worldwide and the activation of canonical Wnt signaling pathway is universal in hepatocellular carcinoma patients.
Xiaobo Nie +5 more
doaj +1 more source
Dopamine-D1 and δ-opioid receptors co-exist in rat striatal neurons [PDF]
, 2006 Cocaine’s enhancement of dopaminergic neurotransmission in the mesolimbic pathway plays a critical role in the initial reinforcing properties of this drug. However, other neurotransmitter systems are also integral to the addiction process.
Ambrose-Lanci, L. M. +3 more
core +2 more sources
Fluoxetine: a case history of its discovery and preclinical development [PDF]
, 2014 Introduction: Depression is a multifactorial mood disorder with a high prevalence worldwide. Until now, treatments for depression have focused on the inhibition of monoaminergic reuptake sites, which augment the bioavailability of monoamines in the CNS ...
Bel N +20 more
core +2 more sources