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Development of NK3R Antagonists with a Labile Functional Group in the Natural Environment
For development of novel NK3R antagonists with reduced environmental toxicity, a structure-activity relationship study of an NK3R antagonist,...
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A3 Adenosine Receptor Ligands: From Discovery to Clinical Trials
Numerous classes of selective agonists, antagonists, and allosteric modulators of the A3 adenosine receptor (AR) have been reported. The...
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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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Comparative study of interaction energies between αIIbβ3 integrin and the peptidic, peptidomimetic and non-peptidic ligands by quantum mechanics FMO-PIEDA calculations
Integrins belong to a family of cell adhesion receptors. To better understand an adhesion mechanism of integrins, fragmented molecular orbital (FMO)...
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Mechanism of Antagonism: Hyperparasitism and Antibiosis
Government and public concerns about chemicals and their chemical residues including fungicides, bactericides, herbicides, etc. in food and...
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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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Enhancement of Biocontrol Agents Activity by Compatible Treatments Against Postharvest Disease of Fruits
Despite the ability of microbial antagonists to control postharvest spoilage, the looking for the consistently high level of disease control using...
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Solid-State Synthesis of SnO2–Zn2SnO4 Nanocomposite and Its Application for Electrochemical Detection of Cabergoline as Dopamine Receptor Antagonists
AbstractIn the present work, the synthesis of SnO 2 –Zn 2 SnO 4 nanocomposite was fulfilled according to solid-state technique followed by calcination....
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The Therapeutic Potential of 2-{[4-(2-methoxyphenyl)piperazin-1-yl]alkyl}-1H-benzo[d]imidazoles as Ligands for Alpha1-Adrenergic Receptor - Comparative In Silico and In Vitro Study
Adrenergic receptors are among the most studied G protein-coupled receptors. Activation or blockade of these receptors is a major therapeutic...
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New molecular insights into dual inhibitors of tankyrase as Wnt signaling antagonists: 3D-QSAR studies on 4H-1,2,4-triazole derivatives for the design of novel anticancer agents
Genetic mutations in APC or CNTBB1 gene with aberrant canonical Wnt/β-catenin pathway are responsible for more than 90% of colorectal carcinogenesis....
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Next-Generation Therapies for Type 2 Diabetes Mellitus
Type 2 diabetes mellitus (T2DM), which has been considered a pandemic due to its growing pervasiveness in the world population, is associated with...
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Simultaneous Determination of Three 5-HT3 Receptor Antagonists Accompanied by Stability Study Using Thin-Layer Chromatography—Densitometry
A thin-layer chromatographic (TLC)—densitometric method for the separation and simultaneous determination of 3 5-HT 3 receptor antagonists, namely,...
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One class classification for the detection of β2 adrenergic receptor agonists using single-ligand dynamic interaction data
G protein-coupled receptors are involved in many biological processes, relaying the extracellular signal inside the cell. Signaling is regulated by...
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Electronic complementarity permits hindered butenolide heterodimerization and discovery of novel cGAS/STING pathway antagonists
sp 3 -hybridized attached-rings are common motifs in secondary metabolites and represent tetrahedral equivalents to the biaryl substructures that...
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Targeting colorectal cancer with small-molecule inhibitors of ALDH1B1
Aldehyde dehydrogenases (ALDHs) are promising cancer drug targets, as certain isoforms are required for the survival of stem-like tumor cells. We...
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Current Elicitation Strategies for Improving Secondary Metabolites in Medicinal Plants with Antiallergy Properties
In recent decades, there has been a substantial surge in the occurrence of allergic conditions such as rhinitis, asthma, food allergies, and atopic...
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Mass spectrometry captures biased signalling and allosteric modulation of a G-protein-coupled receptor
G-protein-coupled receptors signal through cognate G proteins. Despite the widespread importance of these receptors, their regulatory mechanisms for...
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The impact of ATP-sensitive potassium channel modulation on mitochondria in a Parkinson’s disease model using SH-SY5Y cells depends on their differentiation state
Inward rectifying potassium channels sensitive to ATP levels (KATP) have been the subject of investigation for several decades. Modulators of KATP...
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The Medicinal Chemistry of Glucocorticoid Receptor Modulators
This book covers the design and development of glucocorticoid receptor modulators (GRM) from cortisol to antibody-drug conjugate payloads over the...
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Application of Enzymatic Promiscuity in Pharmaceutical Synthesis: Papain-catalyzed One-pot Synthesis of 1,4-Dihydropyridine Calcium Channel Antagonists and Derivatives
A new method for the synthesis of 1,4-dihydropyridine(1,4-DHP) calcium channel antagonists felodipine, nitrendipine and their derivatives via ...