Design, synthesis and efficacy of novel G protein-coupled receptor kinase 2 inhibitors(527 views) Carotenuto A, Cipolletta E, Gomez-Monterrey I, Sala M, Vernieri E, Limatola A, Bertamino A, Musella S, Sorriento D, Grieco P, Trimarco B, Novellino E, Iaccarino G, Campiglia P
Keywords: Cardiovascular System, Cyclic Peptides, Grk2 Inhibitors, Nmr Conformational Analysis, Cyclopeptide, G Protein Coupled Receptor Kinase 2, G Protein Coupled Receptor Kinase 2 Inhibitor, Lactam Derivative, Protein Serine Threonine Kinase Inhibitor, Unclassified Drug, Article, Controlled Study, Drug Conformation, Drug Design, Drug Efficacy, Drug Potency, Drug Selectivity, Drug Synthesis, Enzyme Inhibition, Enzyme Structure, Human, Human Cell, Nuclear Magnetic Resonance Spectroscopy, Nuclear Overhauser Effect, Peptide Library, Protein Structure, 7-Pentamethyldihydro Benzofuran-5-Sulfonyl, 2-(1h-Benzotriazole-1-Yl)-1, 3-Tetramethyluronium Hexafluoro-Phosphate, 9-Fluorenyl-Methoxycarbonyl, Adenosine Triphosphate, Cyclic Adenosine Monophosphate, Dichloromethane, Dipea, Dodecylphosphocholine, Egta, Electrospray Ionization, Ethylene Diamine Tetraacetic Acid, Ethylene Glycol Tetraacetic Acid, Fmoc, Hbtu, Liquid Chromatography Quadrupole Mass Spectrometry, N-Diisopropylethyl-Amine, N-Dimethylformamide, N-Hydroxy-Benzotriazole, Pr(3)sih Or Tis, Reversed-Phase High Performance Liquid Chromatography, Rp-Hplc, Structure-Activity Relationship, Trifluoroacetic Acid, Triisopropylsilane, Trityl, Dose-Response Relationship, G-Protein-Coupled Receptor Kinase 2, Models, Molecular, Protein Kinase Inhibitors,
Affiliations: *** IBB - CNR ***
Dipartimento di Farmacia Federico II, University of Naples, Italy
Dipartimento di Scienze Biomediche Avanzate Federico II, University of Naples, Italy
Dipartimento di Medicina e Chirurgia, University of Salerno, Italy
IRCCS Multimedica, Milano, Italy
Pharmaceutical Science, University of Salerno, Salerno, Italy
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Design, synthesis and efficacy of novel G protein-coupled receptor kinase 2 inhibitors