Method for Identifying Modulators of Gamma Secretase or Notch

• Main Authors: CHURCHER IAN, NANTHAKUMAR CARMEL BEULIN, SIMPSON PETER BRIAN
• Format: Patent
• Language: English
• Published: 16.09.2010
• Subjects: BEER; BIOCHEMISTRY; CHEMISTRY; COMBINATORIAL CHEMISTRY; COMPOSITIONS OR TEST PAPERS THEREFOR; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL ORENZYMOLOGICAL PROCESSES; ENZYMOLOGY; HUMAN NECESSITIES; HYGIENE; INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIRCHEMICAL OR PHYSICAL PROPERTIES; LIBRARIES, e.g. CHEMICAL LIBRARIES, IN SILICOLIBRARIES; MEASURING; MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEICACIDS OR MICROORGANISMS; MEDICAL OR VETERINARY SCIENCE; METALLURGY; MICROBIOLOGY; MUTATION OR GENETIC ENGINEERING; PHYSICS; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; PROCESSES OF PREPARING SUCH COMPOSITIONS; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS; SPIRITS; TESTING; VINEGAR; WINE

The present invention relates to methods for high throughput screening to identify selective modulators of γ-secretase. Such modulators selectively block γ-secretase activity without affecting Notch cleavage and signaling. Said methods employ the use of high content screening methodologies to measure and quantify the translocation of the Notch intracellular domain (NICD) between the nucleus and cytoplasm in cells and the activation of Notch.