Method of screening for GPR40 ligands

Chemistry: molecular biology and microbiology – Measuring or testing process involving enzymes or... – Involving antigen-antibody binding – specific binding protein...

Reexamination Certificate

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C435S007200

Reexamination Certificate

active

10451007

ABSTRACT:
Methods of screening for ligands of the GPR40 receptor are provided, including methods utilizing fatty acid GPR40 ligands.

REFERENCES:
patent: 0849361 (1998-06-01), None
patent: WO 0022129 (2000-04-01), None
patent: WO 0244362 (2002-06-01), None
Briscoe et al., The orphan G protein-coupled receptor GPR40 is activated by medium and long chain fatty acids. J. Biol. Chem. 278:11303-11311, 2003.
Itoh et al., Free fatty acids regulate insulin secretion from pancreatic beta cells through GPR40. Nature 422:173-176, 2003.
Sawzdargo et al., “A cluster of four novel human G protein-coupled receptor genes occurring in close proximity to CD22 gene on chromosome 19Q13.1,”Biochemical and Biophysical Research Communications239:543-547 (1997).
Sharif et al., “A high-throughput system for the evaluation of protein kinase C inhibitors based on ELK1 transcriptional activation in human astrocytoma cells,”International Journal of Oncology, Editorial Academy of the International Journal of Oncology14(2):326-335 (Feb. 1999).
Stables et al., “Development of a dual glow-signal firefly and renilla luciferase assay reagent for the analysis of G-protein coupled receptor signalling,”Journal of Receptor and Signal Transduction Research19(1-4):395-410 (1999).
Database EMBL ′Online!, Mar. 20, 2000, Database accession No. AW583167 abstract.
Database WPI, Section Ch, Week 200249, Derwent Publications, AN 2002-463740 & WO0244362 abstract.
Tseng et al., “Role of regulator of G protein signaling in desensitization of the glucose-dependent insulinotropic peptide receptor,”Endocrinology139(11):4470-4475 (Nov. 1998).
Warnotte et al., “Unbound rather than total concentration and saturation rather than unsaturation determine the potency of fatty acids on insulin secretion,”Molecular and Cellular Endocrinology153(1-2):147-153 (Jul. 1999).

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