Results 171 to 180 of about 121,181 (303)
Analysis of equilibrium binding of an orthosteric tracer and two allosteric modulators - Fig 8
, 2019 Comparison of competition and allosteric interaction between modulators A and B. Simulation of tracer binding (ordinate) in the presence two allosteric modulators A and B each binding to its own allosteric site (yellow line) or competing for the same ...
Esam E. El-Fakahany (339452) +3 more
core +1 more source
Precision Chemistry for Protein Lysine Modification
Chemistry – A European Journal, EarlyView.Selective modification of lysine residues is challenging due to their similar intrinsic reactivity. Inspired by enzymatic recognition, ligand‐guided electrophiles enable site‐selective labeling and functionalization, while ligand‐guided catalyses achieve regioselective installation of bio‐relevant post‐translational modifications.
Mayu Onoda, Motomu Kanai
wiley +1 more source
A hybrid indoloquinolizidine peptide as allosteric modulator of dopamine D1 receptors
, 2013 et al.The indoloquinolizidine-peptide 28 [(3S,12bR)-N-((S)-1-((S)-1-((S)-2- carbamoylpyrrolidin-1-yl)-3-(4-fluorophenyl)-1-oxopropan-2-ylamino) -4-cyclohexyl-1-oxobutan-2-yl)-1,2,3,4,6,7,12,12b-octahydroindolo[2,3-a] quinolizine-3-carboxamide], a ...
Albericio, Fernando +3 more
core +1 more source
Chemistry – A European Journal, EarlyView.A modular, de novo α/β‐peptide design strategy allows fine‐tuning of ligand properties, resulting in multivalent ligands that simultaneously target separate binding sites on the protein surface. ABSTRACT Protein‐protein interactions that regulate gene expression in the nucleus are increasingly recognized as potential therapeutic targets but present ...
Márk V. Tresztián +4 more
wiley +1 more source
PLoS BiologyP2X receptors are ATP-gated cation channels, and the P2X3 subtype plays crucial roles in peripheral sensory neurons, including in chronic pain and chronic cough.
Zhixuan Zhao +10 more
doaj +1 more source
Long-term α5 GABA A receptor negative allosteric modulator treatment reduces NMDAR-mediated neuronal excitation and maintains basal neuronal inhibition. [PDF]
Neuropharmacology, 2023 Nuwer JL, Povysheva N, Jacob TC.
europepmc +1 more source
Natural Negative Allosteric Modulators of 5-HT₃ Receptors.
Molecules (Basel, Switzerland), 2019 Chemotherapy-induced nausea and vomiting (CINV) remain the most common and devastating side-effects associated with cancer chemotherapy. In recent decades, several lines of research emphasize the importance of 5-hydroxytryptamine3 (5-HT3; serotonin) receptors in the pathogenesis and treatment of CINV.
Lina T, Al Kury +3 more
openaire +1 more source
A Systematic Review on Disease‐Modifying Therapies in Parkinsonian Disorders
Clinical Pharmacology &Therapeutics, EarlyView.Parkinsonian disorders, including Parkinson's disease, Lewy body dementia, multiple system atrophy, and progressive supranuclear palsy, are progressive neurodegenerative conditions with no treatment options to slow disease progression. This systematic review provides an overview of evidence of disease‐modifying therapies that have been evaluated in ...
Pepijn P.N.M. Eijsvogel +3 more
wiley +1 more source
Changes in social, sexual, and hedonic behaviors in rats in response to stress and restoration by a negative allosteric modulator of α5-subunit containing GABA receptor. [PDF]
Behav Brain Res, 2023 Bailey AM +6 more
europepmc +1 more source
Clinical Pharmacology &Therapeutics, EarlyView.One‐third of epilepsy patients remain treatment‐resistant, underscoring the need for novel anti‐seizure medications (ASMs) and reliable biomarkers of central target engagement. Cortical hyperexcitability is a hallmark of epilepsy, making excitability a valuable pharmacodynamic biomarker for early‐phase drug development supporting go/no‐go decision ...
Catherine M. E. de Cuba +7 more
wiley +1 more source