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Radiolabeled Integrin αvβ3 Antagonists as Radiopharmaceuticals for Tumor Radiotherapy
Integrins are a family of proteins that facilitate cellular adhesion to and migration on the extracellular matrix proteins found in intercellular...
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Two-point immobilization of M3 muscarinic receptor: a method for recognizing receptor antagonists in natural products
In the investigation of active ingredients from natural products, current technologies relying on drug–target affinity recognition analysis face...
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Molecular Mechanism of Action of GPR91 Agonists and Antagonists: Insights from Molecular Dynamics Simulation
G protein-coupled receptor 91 (GPR91) has garnered widespread attention as a prospective therapeutic target for metabolic diseases. However, no...
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Adenosine A2A Receptor Antagonists: Chemistry, SARs, and Therapeutic Potential
Many physiological processes are modulated by the naturally occurred nucleoside adenosine after interaction with four G-protein-coupled receptor...
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DeepAR: a novel deep learning-based hybrid framework for the interpretable prediction of androgen receptor antagonists
Drug resistance represents a major obstacle to therapeutic innovations and is a prevalent feature in prostate cancer (PCa). Androgen receptors (ARs)...
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Synthesis of 3,4-dihydropyrimido[1,2-a]benzimidazoles, promising CRF1 receptor antagonists
The influence of conditions on the course of the reactions between 1,2-diaminoimidazole and N -arylmaleimides was studied. It was shown that,...
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Computational prediction of analog compounds of the membrane protein MCHR1 antagonists ALB-127158 and KRX-104130
Obesity, which is already pervasive throughout the world, endangers public health by raising the prevalence of metabolic disorders and making their...
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Microbial Antagonists from Different Environments Used in the Biocontrol of Plant Pathogens
The control of plant diseases is generally done with the application of synthetic pesticides; however, their use causes problems of environmental...
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Structures of the human cholecystokinin receptors bound to agonists and antagonists
Cholecystokinin receptors, CCK A R and CCK B R, are important neurointestinal peptide hormone receptors and play a vital role in food intake and appetite...
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ATP-competitive partial antagonists of the IRE1α RNase segregate outputs of the UPR
The unfolded protein response (UPR) homeostatically matches endoplasmic reticulum (ER) protein-folding capacity to cellular secretory needs. However,...
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Bacterial Antagonists: Effective Tools for the Management of Postharvest Diseases in Fruits, Vegetables, and Food Grains
Microorganisms play an important role in our daily life through their presence in human intestine to the microbial flora of the earth. Fresh produce...
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Design and synthesis of novel tetrahydrofuran cyclic urea derivatives as androgen receptor antagonists
AbstractIn order to improve the antiproliferative activity of androgen receptor (AR) antagonists, which used clinically for the treatment of prostate...
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Structure–Activity Relationships for Development of Neurokinin-3 Receptor Antagonists Reducing Environmental Impact
This book explores the possible development of neurokinin-3 receptor (NK3R) antagonists with reduced environmental impact.Pharmaceuticals are used to...
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Antibodies expand the scope of angiotensin receptor pharmacology
G-protein-coupled receptors (GPCRs) are key regulators of human physiology and are the targets of many small-molecule research compounds and...
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A combined structure-based pharmacophore modeling and 3D-QSAR study on a series of N-heterocyclic scaffolds to screen novel antagonists as human DHFR inhibitors
Dihydrofolate reductase (DHFR) is an essential enzyme that participates in folate metabolism and purine and thymidylate synthesis in cell...
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Drug design of new 5-HT6 antagonists: a QSAR study of arylsulfonamide derivatives
Several studies underscore that the 5-hydroxytryptamine subtype 6 (5-HT 6 ) receptor is intrinsically related to the onset of Alzheimer’s disease and...
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5-Alkylamino-7-aminoazolo[1,5-a]pyrimidine-6-carbonitriles: synthetic strategies and anticancer activity in vitro
The design of novel antagonists for adenosine A 2a receptor (A 2a AR) is a promising strategy for the development of new-generation anticancer agents....
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Development of NK3R Antagonists with a Degradable Scaffold in the Natural Environment: Identification of NK3R Antagonists with a Decomposable Core Structure by Scaffold Hop**
For development of novel NK3R antagonists with less environmental toxicity, a series of heterocyclic scaffolds for the triazolopiperazine...
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Adenosine Receptor Ligands, Probes, and Functional Conjugates: A 20-Year History of Pyrazolo[4,3-e][1,2,4]Triazolo[1,5-c]Pyrimidines (PTP)
Adenosine receptors are G protein-coupled receptors (GPCRs) involved in several processes in the human body. Their involvement in pathologies like...
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6-Hydrazinonicotinamide Derivatives as Bifunctional Coupling Agents for 99mTc-Labeling of Small Biomolecules
99mTc-labeled small biomolecules are a class of receptor-based, target specific radiopharmaceuticals for the detection of various diseases, such as...