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Crystal structure of adenosine A2A receptor in complex with clinical candidate Etrumadenant reveals unprecedented antagonist interaction
The G s protein-coupled adenosine A 2A receptor (A 2A AR) represents an emerging drug target for cancer immunotherapy. The clinical candidate...
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Exploring the interaction mechanism between antagonist and the jasmonate receptor complex by molecular dynamics simulation
Jasmonates induce the protein–protein interaction between the F-box protein CORONATINE INSENSITIVE 1 (COI1) and jasmonate ZIM-domain proteins (JAZs)...
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Structural basis of TRPV3 inhibition by an antagonist
The TRPV3 channel plays vital roles in skin physiology. Dysfunction of TRPV3 causes skin diseases, including Olmsted syndrome. However, the lack of...
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Pharmacophore-based virtual screening from phytocannabinoids as antagonist r-CB1
Search for new pharmacological alternatives for obesity is based on the design and development of compounds that can aid in weight loss so that they...
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Economical Voltammetric Sensor for Sensitive Rapid Determination of Ondansetron in the Presence of Opioid Antagonist Naltrexone
The electrochemical actions of ondansetron (OND) were investigated on the modified electrode with Polyvinyl Pyrollidone (PVP) and multi-walled carbon...
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Antagonist action of Lactobacillus acidophilus against pathogenic strains in goat milk yogurt
Contamination by pathogenic bacteria is the major cause of foodborne diseases, which is an international public health issue. Probiotics added to...
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Development of Polar Organic Mode Chromatographic Method by Polysaccharide-Based Immobilized Chiral Selector and Validation for the Determination of the Enantiopurity of Novel Mineralocorticoid Receptor Antagonist Atropisomer–Esaxerenone
Esaxerenone is a new nonsteroidal mineralocorticoid receptor antagonist utilized to treat high blood pressure. Chemically, esaxerenone is a pyrrole...
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Insights from molecular docking and molecular dynamics on the potential of vitexin as an antagonist candidate against lipopolysaccharide (LPS) for microglial activation in neuroinflammation
BackgroundNeuroinflammation has been identified to be the key player in most neurodegenerative diseases. If neuroinflammation is left to be...
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In silico docking and ADME study of deketene curcumin derivatives (DKC) as an aromatase inhibitor or antagonist to the estrogen-alpha positive receptor (Erα+): potent application of breast cancer
Regardless of many extensive studies, hormonal-based breast cancer is the most common cause of cancer-related mortality of females worldwide. Indeed,...
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Synthesis, molecular modeling and functional evaluation of a GnRH antagonist
In the present study, a series of novel Trp-Pro-Val containing peptides were prepared via solid-phase synthesis, and their structures were cyclized...
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Synthesis and single-molecule imaging reveal stereospecific enhancement of binding kinetics by the antitumour eEF1A antagonist SR-A3
Ternatin-family cyclic peptides inhibit protein synthesis by targeting the eukaryotic elongation factor-1α. A potentially related cytotoxic natural...
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Synthesis of the Neurokinin 1 Receptor Antagonist (+)-L-733,060 by Jacobsen’s Hydrolytic Kinetic Resolution
AbstractEnantioselective synthesis of the neurokinin 1 receptor antagonist (+)-L-733,060 has been achieved using Jacobsen’s hydrolytic kinetic...
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Integrated In Silico-In Vitro Identification and Optimization of Bone Morphogenic Protein-2 Armpit Epitope as Its Antagonist Binding Site
Bone morphogenic protein-2 (BMP-2) is the most documented member of BMP family and plays a crucial role in bone formation and growth. In this study,...
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Antagonist Impact of Selenium-Based Nanoparticles Against Mycobacterium tuberculosis
One of the cardinal causes of global deaths from a single-point infectious agent has been reported to be tuberculosis (or TB). At present times, the...
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Hyaluronic acid-FGF2-derived peptide bioconjugates for suppression of FGFR2 and AR simultaneously as an acne antagonist
Acne is a chronic skin condition that has serious consequences for mental and social well-being because it frequently occurs on the face. Several...
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Distinct binding mode of BAFF antagonist antibodies belimumab and tabalumab, analyzed by computer simulation
B cell-activating factor (BAFF) can bind with specific receptors to activate signalling pathways associated with the B cell activation. Belimumab and...
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Effect of Interleukin 1 Receptor Antagonist Gene on Stable Expression Bone Marrow Mesenchymal Stem Cells and Early Aseptic Loosening of Hip Prosthesis of Mouse
The research aimed to investigate the diagnostic value of Interleukin 1 receptor antagonist (IL-1Ra) in the early aseptic loosening of hip prosthesis...
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Synthesis and muscarinic acetylcholine receptor (mAChR) antagonist activity of substituted piperazine-triazoles
This study describes synthesis of a series of piperazine-triazole derivatives and their ex vivo evaluation for preliminary muscarinic acetylcholine...
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Determination of neuropeptide Y Y1 receptor antagonist BIBP 3226 and evaluation of receptor expression based on liquid chromatography coupled with tandem mass spectrometry
Neuropeptide Y (NPY) is a peptide widely distributed throughout the body that is involved in various physiological processes, including the...
