Results 41 to 50 of about 1,154,493 (312)

Mapping the druggable allosteric space of G-protein coupled receptors: a fragment-based molecular dynamics approach. [PDF]

open access: yes, 2010
To address the problem of specificity in G-protein coupled receptor (GPCR) drug discovery, there has been tremendous recent interest in allosteric drugs that bind at sites topographically distinct from the orthosteric site. Unfortunately, structure-based
Ivetac, Anthony, McCammon, J Andrew
core   +2 more sources

G protein-coupled receptors: structure- and function-based drug discovery

open access: yesSignal Transduction and Targeted Therapy, 2021
As one of the most successful therapeutic target families, G protein-coupled receptors (GPCRs) have experienced a transformation from random ligand screening to knowledge-driven drug design.
Dehua Yang   +14 more
doaj   +1 more source

Engineering of Challenging G Protein-Coupled Receptors for Structure Determination and Biophysical Studies

open access: yesMolecules, 2021
Membrane proteins such as G protein-coupled receptors (GPCRs) exert fundamental biological functions and are involved in a multitude of physiological responses, making these receptors ideal drug targets.
Yann Waltenspühl   +3 more
doaj   +1 more source

N-acetyl-cysteine, a drug that enhances the endogenous activation of group-II metabotropic glutamate receptors, inhibits nociceptive transmission in humans. [PDF]

open access: yes, 2015
Emerging research seeking novel analgesic drugs focuses on agents targeting group-II metabotropic glutamate receptors (mGlu2 and mGlu3 receptors). N-Acetylcysteine (NAC) enhances the endogenous activation of mGlu2/3 receptors by activating the glial ...
BATTAGLIA, Giuseppe   +8 more
core   +1 more source

The effect of combined glutamate receptor blockade in the NTS on the hypoxic ventilatory response in awake rats differs from the effect of individual glutamate receptor blockade. [PDF]

open access: yes, 2014
Ventilatory acclimatization to hypoxia (VAH) increases the hypoxic ventilatory response (HVR) and causes persistent hyperventilation when normoxia is restored, which is consistent with the occurrence of synaptic plasticity in acclimatized animals ...
Carr, John A   +3 more
core   +2 more sources

European Standard Clinical Practice Guideline and EXPeRT Recommendations for the Diagnosis and Management of Gastroenteropancreatic Neuroendocrine Neoplasms in Children and Adolescents

open access: yesPediatric Blood &Cancer, EarlyView.
ABSTRACT Pediatric gastroenteropancreatic neuroendocrine neoplasms (GEP‐NENs) are extremely rare and clinically heterogeneous. Management has largely been extrapolated from adult practice. This European Standard Clinical Practice Guideline (ESCP), developed by the EXPeRT network in collaboration with adult NEN experts, provides (adult) evidence ...
Michaela Kuhlen   +23 more
wiley   +1 more source

SYNERGISM AND DRUG-RECEPTOR

open access: yesJapanese Journal of Pharmacology, 1964
In the study of the drug-receptor interaction, the analysis of the mode of drugantagonism had been the objects of the principal interests, and the drug-synergism had only been remarked in passing (1). Veldstra (2) mentioned the relation between drug receptor and synergism in his extensive review on “Synergism and Potentiation”.
K, TAKAGI, I, TAKAYANAGI
openaire   +3 more sources

Stress-Induced Reinstatement of Drug Seeking: 20 Years of Progress [PDF]

open access: yes, 2015
In human addicts, drug relapse and craving are often provoked by stress. Since 1995, this clinical scenario has been studied using a rat model of stress-induced reinstatement of drug seeking.
A Cippitelli   +291 more
core   +2 more sources

Why and When Are Evidence‐Based Interventions Adopted in Paediatric Supportive Care? A Qualitative Exploration of the Determinants of Photobiomodulation Implementation

open access: yesPediatric Blood &Cancer, EarlyView.
ABSTRACT Background Oral mucositis is a common and debilitating side effect of childhood cancer and stem cell transplant treatments. It affects the quality of life of children and young people (CYP) and places a strain on services. Photobiomodulation is recommended for oral mucositis prevention in international guidance but is poorly implemented in UK ...
Claudia Heggie   +4 more
wiley   +1 more source

The Hippocampus Is the Place to Be: Opioid Receptors and LTP

open access: yesCell Reports, 2019
Nam et al. (2019) genetically modulate the expression of astrocytic μ-opioid receptors to reveal they are necessary for drug-induced conditioned place preference.
Thomas M. Sanderson   +3 more
doaj   +1 more source

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