Characterization of substrates and inhibitors of the human heterodimeric transporter 4F2hc-LAT1 using purified protein and the scintillation proximity radioligand binding assay [PDF]
Frontiers in Physiology, 2023 Amino acids have diverse and essential roles in many cellular functions such as in protein synthesis, metabolism and as precursors of different hormones.
Satish Kantipudi +2 more
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A radioligand binding assay for the insulin-like growth factor 2 receptor. [PDF]
PLoS ONE, 2020 Insulin-like growth factors 2 and 1 (IGF2 and IGF1) and insulin are closely related hormones that are responsible for the regulation of metabolic homeostasis, development and growth of the organism.
Pavlo Potalitsyn +7 more
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Fully Automated Radioligand Binding Filtration Assay for Membrane-Bound Receptors [PDF]
BioTechniques, 2002 Here we describe a fully automated, hands-free radioligand filtration binding assay for dopamine D3 receptors. Three separate instruments were linked in tandem to perform the following operations: The Genmate and Genesis were linked to perform liquid ...
A. Shrikhande +6 more
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Novel 2-substituted-5-(4-chloro-2-phenoxy)phenyl-1,3,4-oxadiazole derivatives, ligands of GABAA/benzodiazepine receptor complex [PDF]
EXCLI Journal : Experimental and Clinical Sciences, 2023 Agonists of Benzodiazepine (BZD) receptor are exhaustively used in the control of muscle spasms, seizure, anxiety, and insomnia. BZDs have some unwanted effects; therefore, the development of new BZD receptor agonists with better efficacy and fewer ...
Elham Rezaee +7 more
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Methods for assessing binding of a small-molecule radioligand to soluble enzyme isocitrate dehydrogenase 1 variants [PDF]
EJNMMI Radiopharmacy and ChemistryBackground Isocitrate dehydrogenase 1 (IDH1) is a cytosolic NADP+-dependent enzyme involved in cellular redox homeostasis and 2-oxoglutarate (2-OG) metabolism.
Winnie Deuther-Conrad +3 more
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Pharmaceuticals, 2022 Hepsin, a cell surface serine protease, is a potential biomarker for the detection of prostate cancer due to its high expression in prostate cancer but not in normal prostate.
Ji-Hun Park +7 more
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Journal of Pharmacological Sciences, 2022 The present study aimed to characterize and compare β-adrenoceptors in the rat bladder with those in the heart and lungs of SD rats (8–10 weeks old) using subtype-selective agonists and antagonists in a radioligand binding assay with (-)-[125I ...
Shizuo Yamada +4 more
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Cells, 2022 Chemokine receptors are extensively involved in a broad range of physiological and pathological processes, making them attractive drug targets. However, despite considerable efforts, there are very few approved drugs targeting this class of seven ...
Stefanie Alexandra Eberle +1 more
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Machine Learning for Discovery of New ADORA Modulators
Frontiers in Pharmacology, 2022 Adenosine (ADO) is an extracellular signaling molecule generated locally under conditions that produce ischemia, hypoxia, or inflammation. It is involved in modulating a range of physiological functions throughout the brain and periphery through the ...
Ana C. Puhl +3 more
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Dopamine transporter interaction with blockers and transportable substrates: insights from kinetics study [PDF]
Proceedings of the Estonian Academy of Sciences, 2023 Competition kinetic analysis was performed to examine the interaction mechanism of the dopamine transporter with dopamine, (S)-amphetamine, and cocaine, which play a central role in drug abuse phenomena connected with the dopaminergic system.
Vladimir Stepanov
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