# US 8,568,997 B2 · Detection system and uses therefor > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 8,568,997 B2 - Document ID: US8568997B2 - Status: Granted - Kind: B2 - Application number: 13/608,855 - Filed: 2012-09-10 - Published: 2013-03-14 - Granted: 2013-10-29 - Earliest claimed: 2006-11-10 - Assignees: Dimerix Bioscience Pty Ltd. - Applicants: Kevin Donald George Pfleger; Ruth Marie Seeber; Heng Boon See; Karin Ann Eidne - Inventors: Kevin Donald George Pfleger; Ruth Marie Seeber; Heng Boon See; Karin Ann Eidne - Web page: https://patentgrep.com/patent/US8568997B2 ## CPC - G01N 33/542: with steric inhibition or signal modification, e.g. fluorescent quenching - A61P 3/04: Anorexiants; Antiobesity agents - A61P 25/00: Drugs for disorders of the nervous system - A61P 25/08: Antiepileptics; Anticonvulsants - A61P 25/16: Anti-Parkinson drugs - A61P 25/18: Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia - A61P 25/22: Anxiolytics - A61P 25/24: Antidepressants - A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia - A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 - G01N: INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES (measuring or testing apparatus or processes other than immunoassay, involving enzymes or microorganisms C12M, C12Q) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS ## Abstract A system for the detection of molecular associations, the system comprising: i) a first agent, comprising a first interacting group coupled to a first reporter component; ii) a second agent, comprising a second interacting group coupled to a second reporter component; iii) a third agent, comprising a third interacting group; iv) a modulator; and v) a detector; wherein proximity of the first and second reporter components generates a signal capable of detection by the detector; and wherein the modulator modulates the association of the second interacting group with the third interacting group; such that monitoring the signal generated by proximity of the first and second reporter components by the detector constitutes monitoring the association of the first and third agents. ## Claims ### Claim 1 A kit for determining whether and/or the extent to which a test compound interacts with a second receptor when the second receptor is associated with a first receptor, wherein the first receptor is different from the second receptor, the kit comprising: (a) a first receptor coupled to a first reporter component; (b) an interacting group coupled to a second reporter component; and (c) a second receptor capable of associating with the interacting group, wherein proximity of the first and second reporter components generates a signal, wherein the test compound is capable of modulating association of the interacting group with the second receptor by interacting with the second receptor, either alone, or simultaneously with the first receptor. ### Claim 2 (depends on 1) The kit according to claim 1, wherein the test compound is an agonist of the second receptor when the second receptor is associated with the first receptor and in increase in the signal determination of the extent to which the test compound is an agonist of the second receptor when the second receptor is associated with the first receptor. ### Claim 3 (depends on 1) The kit according to claim 1, wherein the test compound is an antagonist or a partial agonist of the second receptor when the second receptor is associated with the first receptor, wherein the kit further comprises: (d) an agonist of the second receptor; and wherein decrease in the signal is a determination of the extent to which the test compound is an antagonist or a partial agonist of the second receptor when the second receptor is associated with the first receptor. ### Claim 4 (depends on 1) The kit according to claim 1, wherein the test compound is an inverse agonist of the second receptor when the second receptor is associated with the first receptor, wherein the second receptor is a constitutively active receptor, and wherein a decrease in the signal is a determination of the extent to which the test compound is an inverse agonist of the second receptor when the second receptor is associated with the first receptor. ### Claim 5 (depends on 1) The kit according to claim 1, wherein the test compound exhibits first receptor/second receptor hetero-dimer/-oligomer selective activity, wherein the test compound interacts with the second receptor while the second receptor is associated with the first receptor; and wherein the signal is a determination of the extent to which the test compound interacts with the second receptor in the absence of the first receptor, such that a test compound that exhibits greater affinity and/or potency and/or efficacy when interacting with the second receptor while the second receptor is associated with the first receptor is selective for the first receptor/second receptor hetero-dimer/-oligomer. ### Claim 6 (depends on 1) The kit according to claim 1, wherein the test compound exhibits first receptor/second receptor hetero-dimer/-oligomer selective antagonism or partial agonism, wherein kit further comprises: (d) an agonist of the first receptor, the second receptor and/or the first protein/second receptor hetero-dimer/-oligomer; and wherein a decrease in the signal is a determination of the extent to which the test compound is an antagonist or partial agonist of the first receptor/second hetero-dimer/-oligomer. ### Claim 7 (depends on 6) The kit according to claim 6, wherein the test compound is an antagonist or partial agonist of the first receptor/second receptor hetero-dimer/-oligomer, and wherein the signal is a determination of the extent to which the test compound interacts with the second receptor in the absence of the first receptor, such that a test compound that exhibits greater antagonistic or partial agonistic properties when interacting with the first receptor/second receptor hetero-dimer/-oligomer is selective for the first receptor/second receptor hetero-dimer/-oligomer. ### Claim 8 (depends on 1) The kit according to claim 1, wherein the test compound exhibits first receptor/second receptor hetero-dimer/-oligomer selective inverse agonism, wherein the second receptor is constitutively active, and wherein a decrease in the signal is a determination of the extent to which the test compound is an inverse agonist of the first receptor/second receptor hetero-dimer/-oligomer. ### Claim 9 (depends on 1) The kit according to claim 1, wherein the test compound is an inverse agonist of the first receptor/second receptor hetero-dimer/-oligomer, and wherein the signal is a determination of the extent to which the test compound is an inverse agonist of the first receptor in the absence of the second receptor, and of the second receptor in the absence of the first receptor, such that a test compound that exhibits greater inverse agonistic properties when interacting with the first receptor/second receptor hetero-dimer/-oligomer is selective for the first receptor/second receptor hetero-dimer/-oligomer. ### Claim 10 A kit for screening a test compound for selective activity against a heterodimer of a first receptor and a second receptor, the kit comprising: (a) the test compound at increasing concentrations, and (b) a system comprising: (i) a first receptor coupled to a first reporter component; (ii) an interacting group coupled to a second reporter component; and (iii) a second receptor, wherein the second receptor is different from the first receptor; the second receptor capable of associating with the interacting group, wherein proximity of the first and second reporter components generates a signal, wherein the test compound is capable of modulating the association of the interacting group with the second receptor by interacting with the second receptor, either alone, or simultaneously with the first receptor, wherein the signal is a determination of whether the test compound modulates the association of the interacting group with the second receptor at each concentration to produce a dose-response curve, and wherein a Hill slope of the dose-response curve in excess of 1 indicates interaction of the test compound with the hetero-dimer.