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1.
Annu Rev Biochem ; 88: 383-408, 2019 06 20.
Artículo en Inglés | MEDLINE | ID: mdl-30939043

RESUMEN

The cellular thermal shift assay (CETSA) is a biophysical technique allowing direct studies of ligand binding to proteins in cells and tissues. The proteome-wide implementation of CETSA with mass spectrometry detection (MS-CETSA) has now been successfully applied to discover targets for orphan clinical drugs and hits from phenotypic screens, to identify off-targets, and to explain poly-pharmacology and drug toxicity. Highly sensitive multidimensional MS-CETSA implementations can now also access binding of physiological ligands to proteins, such as metabolites, nucleic acids, and other proteins. MS-CETSA can thereby provide comprehensive information on modulations of protein interaction states in cellular processes, including downstream effects of drugs and transitions between different physiological cell states. Such horizontal information on ligandmodulation in cells is largely orthogonal to vertical information on the levels of different proteins and therefore opens novel opportunities to understand operational aspects of cellular proteomes.


Asunto(s)
Desarrollo de Medicamentos/métodos , Proteoma/metabolismo , Ensayo de Cambio de Movilidad Electroforética , Humanos , Ligandos , Espectrometría de Masas , Unión Proteica , Proteoma/química , Proteómica
2.
Pancreas ; 42(1): 123-9, 2013 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-22850623

RESUMEN

OBJECTIVES: The anti-inflammatory effects of O-1602 and cannabidiol (CBD), the ligands of G protein-coupled receptor 55 (GPR55), on experimental acute pancreatitis (AP) were investigated. METHODS: Acute pancreatitis was induced in C57BL mice by intraperitoneal injection of 50 µg/kg cerulein hourly, with a total of 6 times. Drugs (O-1602, 10 mg/kg, or CBD, 0.5 mg/kg) were given by intraperitoneal injection 2 times at 30 minutes before the first injection and immediately before the fifth cerulein injection. At 3 hours after the last injection, the blood, the lungs, and the pancreas were harvested for the pancreatic enzyme activity, myeloperoxidase activity, and pro-inflammatory cytokines measurement; and the expressions of GPR55 mRNA and protein in the pancreas were detected. RESULTS: Cannabidiol or O-1602 treatment significantly improved the pathological changes of mice with AP and decreased the enzyme activities, IL-6 and tumor necrosis factor α; levels, and the myeloperoxidase activities in plasma and in the organ tissues. G protein-coupled receptor 55 mRNA and protein expressed in the pancreatic tissue, and the expressions were decreased in the mice with AP, and either CBD or O-1602 attenuated these changes to a certain extent. CONCLUSION: Cannabidiol and O-1602 showed anti-inflammatory effects in mice with AP and improved the expression of GPR55 in the pancreatic tissue as well.


Asunto(s)
Antiinflamatorios/farmacología , Cannabidiol/análogos & derivados , Ceruletida , Páncreas/efectos de los fármacos , Pancreatitis/prevención & control , Enfermedad Aguda , Amilasas/sangre , Animales , Antiinflamatorios/administración & dosificación , Western Blotting , Cannabidiol/administración & dosificación , Cannabidiol/farmacología , Modelos Animales de Enfermedad , Inmunohistoquímica , Mediadores de Inflamación/sangre , Inyecciones Intraperitoneales , Interleucina-6/sangre , Lipasa/sangre , Pulmón/efectos de los fármacos , Pulmón/metabolismo , Ratones , Ratones Endogámicos C57BL , Páncreas/metabolismo , Páncreas/patología , Pancreatitis/sangre , Pancreatitis/inducido químicamente , Pancreatitis/patología , Peroxidasa/sangre , ARN Mensajero/metabolismo , Reacción en Cadena en Tiempo Real de la Polimerasa , Receptores de Cannabinoides/efectos de los fármacos , Receptores de Cannabinoides/genética , Receptores de Cannabinoides/metabolismo , Reacción en Cadena de la Polimerasa de Transcriptasa Inversa , Factores de Tiempo , Factor de Necrosis Tumoral alfa/sangre
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