METHOD TO IDENTIFY LIGANDS FOR SIGMA-1 RECEPTORS

• Main Authors: CIRUELA ALFÉREZ, Francisco, BURGUEÑO-HURTADO, Javier, VELA HERNÁNDEZ, José Miguel
• Format: Patent
• Language: English; French; German
• Published: 07.12.2016
• Subjects: BEER; BIOCHEMISTRY; CHEMISTRY; COMPOSITIONS THEREOF; CULTURE MEDIA; ENZYMOLOGY; INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIRCHEMICAL OR PHYSICAL PROPERTIES; MEASURING; METALLURGY; MICROBIOLOGY; MICROORGANISMS OR ENZYMES; MUTATION OR GENETIC ENGINEERING; ORGANIC CHEMISTRY; PEPTIDES; PHYSICS; PROPAGATING, PRESERVING OR MAINTAINING MICROORGANISMS; SPIRITS; TESTING; VINEGAR; WINE

An assay for identifying ligands of the à 1 receptor based on a fusion protein comprising the à 1 receptor flanked by two fluorophores, so that said fluorophores are capable of producing constitutive FRET when no ligand is bound to the à 1 receptor. The fusion protein of the invention also allows the simultaneous determination whether the newly determined ligand is an agonist or an antagonist. Said fusion protein has been expressed in a cell, giving rise to a new cellular model useful for identifying à 1 receptor ligands, and additionally for discriminating between agonists and antagonists.