Method of screening binding of a compound to a receptor

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

Reexamination Certificate

Rate now

  [ 0.00 ] – not rated yet Voters 0   Comments 0

Details

C435S007930, C530S350000

Reexamination Certificate

active

07081346

ABSTRACT:
Disclosed is a method of measuring affinity of a test compound for a receptor protein. The method includes the steps of providing a receptor-ligand complex comprising a receptor and a quinoxaline derivative ligand bound thereto; then contacting the receptor-ligand complex with a test compound, thereby yielding a receptor-test compound complex and an amount of free quinoxaline derivative; and then measuring the amount of the free quinoxaline derivative generated as a result of the previous step. In this fashion, the affinity of the test compound for the receptor can be determined.

REFERENCES:
patent: 3992378 (1976-11-01), St. Clair et al.
patent: 4812458 (1989-03-01), Honore et al.
patent: 5208145 (1993-05-01), Rogers
patent: 2002/0006925 (2002-01-01), Pei et al.
patent: 2451049 (1976-04-01), None
patent: 2847285 (1980-05-01), None
patent: 45/25387 (1970-08-01), None
patent: 91909 (1975-02-01), None
patent: WO 01/79181 (2001-04-01), None
Madden et al., J. Biol. Chem. 276: 37821-37826, 2001.
Long et al., (1990) Effect of 6-cyano-2,3-dihydroxy-7-nitro-quinoxaline (CNQX) on dorsal root-, NMDA, kainate- and quisqualate-mediated depolarization of rat motoneurons in vitro,Br. J. Pharmacol., 100:850.
Nakanishi, (1992) Molecular diversity of glutamate receptors and implications for brain functions,Science, 258:597.
Armstrong, N. & Gouaux, E. (2000) Mechanisms for activation and antagonism of an AMPA-sensitive glutamate receptor: crystal structures of the FluR2 ligand binding core,Neuron, 28:165-181.
Boulter, J. et al., (1990) Molecular cloning and functional expression of glutamate receptor subunit genes,Science, 249:1033-1037.
Chen, G.Q. & Gouaux, E. (1997) Overexpression of a glutamate receptor (GluR2) ligand binding domain inEscherichia coli: application of a novel protein folding screen,Proc. Natl. Acad. Sci. USA, 94:13431-13436.
Gill et al., (1992) The neuroprotective actions of 2,3-dihydroxy-6-nitro-7 sulfamoylbenzo-(f)-quinoxaline (NBQX) in a rat focal ischaemia model,Brain Res., 580:35.
Hollman, M., O'Shea-Greenfield, A., Rodgers, S.W. & Heinemann, S. (1989) Cloning by functional expression of a member of the glutamate receptor family,Nature, 342:643-648.
Hollman, M. & Heinemann, S. (1994) Cloned Glutamate receptors,Annu, Rev. Neurosci., 17:31-108.
Honoré et al., (1988) Quinoxalinediones: potent competitive non-NMDA glutamate receptor antagonists,Science, 241:701.
Ichord, R.N., Johnston, M.V. & Traystman, R.J. (2001) MK801 decreases glutamate release and oxidative metabolism during hypoglycemic coma in piglets,Brain Res. Dec. Brain Res., 128:139-148.
Keinänen, K. et al., (1990) A family of AMPA-selective glutamate receptors,Science249:556-560.
King et al., (1992) Antagonism of synaptic potentials in ventral horn neurons by 6-cyano-7nitroquinoxaline-2,3-dione: a study in the rat spinal cord in vitro,Br. J. Pharmacol., 107:375.
Knöpfel et al., (1995) Metabrotropic glutamate receptors: novel targets for drug development,J. Med. Chem., 38:1417.
Namba et al, (1994) Antiepileptogenic and anticonvulsant effects of NBQX, a selective AMPA receptor antagonist, in the rat kindling model of epilepsy,Brain Res., 638:36.
Pin and Duvoisin, (1995) The metabotropic glutamate receptors: structure and functions,Neuropharmacology, 34:1.
Pringle, A.K., Self, J. & Iannotti, F. (2000) Reducing conditions produce a loss of neuroprotective efficacy of competitive but not non-competitive antagonists in a model of NMDA-mediated excitotoxicity in organotypic hippocampal slice cultures,Acta. Neurchir. Suppl., 76:79-80.
Rao, V.L., Fogan, A., Todd, K.G., Bowen, K.K. & Dempsey, R.J. (2001) Neuroprotection by memantine, a non-competitive NMDA receptor antagonist after traumatic brain injury in rats,Brain Res., 911:96-100.
Saito et. al., (1967) Chemical Studies on Riboflavin and Related Compounds. I. Oxidation of Quinoxaline-2,3-diols as a Possible Model for the Biological Decomposition of Riboflavin,Biochemistry, 6(11):3602-3608.
Sheardown et al., (1993) The pharmacology of AMPA receptors and their antagonists,Stroke 24, Suppl. I, 146.
Uchida, K. et al., (2001) Dizocilpine but not ketamine reduces the volume of ischaemic damage after acute subdural haemotama in the rat,Eur. J. Anaesthesiol., 18:295-302.
Watkins et al., (1990) Structure-activity relationships in the development of excitatory amino acid receptor agonists and competitive antagonists,TiPS, 11:25.
Wisden, W. & Seeburg, P.H., (1993) Mammalian ionotropic glutamate receptors,Curr. Opin. Neurobio. 3:291-298.
Yoneda, Y. et al., (2001) Synthesis of diaminobutane derivatives as potent CA(2+)- permeable AMPA receptor antagonists,Bioorg. Med. Chem. Lett., 11:2663-2666.
Zeman and Lodge, (1992) Pharmacological characterization of non-NMDA glutamate subtypes of glutamate receptors in the neonatal rat hemisected spinal cord in vitro,Br. J. Pharmacol., 106:367.

LandOfFree

Say what you really think

Search LandOfFree.com for the USA inventors and patents. Rate them and share your experience with other people.

Rating

Method of screening binding of a compound to a receptor does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Method of screening binding of a compound to a receptor, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Method of screening binding of a compound to a receptor will most certainly appreciate the feedback.

Rate now

     

Profile ID: LFUS-PAI-O-3605286

  Search
All data on this website is collected from public sources. Our data reflects the most accurate information available at the time of publication.