# US 2017/0283872 A1 · Compositions and methods for enhancing odorant receptor activity

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- Number: US 2017/0283872 A1
- Document ID: US20170283872A1
- Status: Published application
- Kind: A1
- Application number: 15/477,873
- Filed: 2017-04-03
- Published: 2017-10-05
- Earliest claimed: 2009-12-04
- Assignees: Duke University
- Applicants: Duke University
- Inventors: Hiroaki Matsunami; Yun Li
- Web page: https://patentgrep.com/patent/US20170283872A1

## CPC

- C12Q 1/6881: for tissue or cell typing, e.g. human leukocyte antigen [HLA] probes
- C07K 14/70571: {for neuromediators, e.g. serotonin receptor, dopamine receptor}
- C12Q 2600/136: Screening for pharmacological compounds
- C12Q 2600/156: Polymorphic or mutational markers
- C12Q: MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS (immunoassay G01N33/53); COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
- C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00)

## Abstract

The present invention relates to polypeptides capable of modulating odorant receptor activation. In particular, the present invention provides polypeptides (e.g., type 3 muscarinic actetylcholine receptor M3) capable of enhancing odorant receptor activation. The present invention further provides assays for the detection of ligands specific for various odorant receptors. Additionally, the present invention provides methods of screening for polypeptide polymorphisms and mutations associated with odorant receptor activation (e.g., polymorphisms and mutations associated with muscarinic actetylcholine receptor polypeptides (e.g., M1, M2, M3, M4, M5)), as well as methods of screening for therapeutic agents, ligands, and modulators of such proteins.

## Claims

### Claim 1

A method for identifying an odorant receptor ligand, comprising:
a) providing
i) a cell comprising an odorant receptor, wherein said cell further comprises a heterologous nucleic acid encoding a polypeptide comprising an amino acid sequence that is at least 80% identical to SEQ ID No. 3, wherein said polypeptide is capable of promoting odorant receptor activity;
ii) at least one test compound;
b) exposing said test compound to said cell; and
c) detecting the activity of said odorant receptor.

### Claim 2 (depends on 1)

The method of claim 1, wherein said cell expresses an RTP1S polypeptide.

### Claim 3 (depends on 1)

The method of claim 1, wherein said at least one test compound comprises more than one test compound.

### Claim 4 (depends on 1)

The method of claim 1, wherein said detecting comprises detecting a reporting agent.

### Claim 5 (depends on 1)

The method of claim 1, wherein said odorant receptor is a human odorant receptor.

### Claim 6 (depends on 1)

The method of claim 1, wherein said test compound is an odoriferous molecule.

### Claim 7 (depends on 1)

The method of claim 1, wherein said odorant receptor is a murine odorant receptor.

### Claim 8 (depends on 1)

The method of claim 1, wherein said odorant receptor is a synthetic odorant receptor.

### Claim 9 (depends on 1)

The method of claim 1, wherein said at least one test compound is exposed in the presence of a reference compound previously identified as a ligand for said odorant receptor.

### Claim 10 (depends on 1)

The method of claim 1, wherein said at least one test compound corresponds to a mixture of different test compounds.

### Claim 11 (depends on 1)

The method of claim 1, further comprising the step of d) detecting the presence or absence of an odorant receptor ligand based upon said activity.

### Claim 12 (depends on 1)

The method of claim 1, wherein said exposing said test compound to said cell occurs in a setting selected from the group consisting of an in vitro setting, an in vivo setting, an in vitro setting, and an ex vivo setting.

### Claim 13

A method for identifying an odorant receptor ligand, comprising:
a) providing
i) a cell comprising an odorant receptor, wherein said cell further comprises a polypeptide comprising an amino acid sequence that is at least 80% identical to SEQ ID No. 9, wherein said polypeptide is capable of promoting odorant receptor activity;
ii) at least one test compound;
b) exposing said test compound to said cell; and
c) detecting the activity of said odorant receptor.

### Claim 14 (depends on 13)

The method of claim 13, wherein said cell expresses an RTP1S polypeptide.

### Claim 15 (depends on 13)

The method of claim 13, wherein said at least one test compound comprises more than one test compound.

### Claim 16 (depends on 13)

The method of claim 13, wherein said detecting comprises detecting a reporting agent.

### Claim 17 (depends on 13)

The method of claim 13, wherein said odorant receptor is a human odorant receptor.

### Claim 18 (depends on 13)

The method of claim 13, wherein said test compound is an odoriferous molecule.

### Claim 19 (depends on 13)

The method of claim 13, wherein said odorant receptor is a murine odorant receptor.

### Claim 20 (depends on 13)

The method of claim 13, wherein said odorant receptor is a synthetic odorant receptor.

### Claim 21 (depends on 13)

The method of claim 13, wherein said at least one test compound is exposed in the presence of a reference compound previously identified as a ligand for said odorant receptor.

### Claim 22 (depends on 13)

The method of claim 13, wherein said at least one test compound corresponds to a mixture of different test compounds.

### Claim 23 (depends on 13)

The method of claim 13, further comprising the step of d) detecting the presence or absence of an odorant receptor ligand based upon said activity.

### Claim 24 (depends on 13)

The method of claim 13, wherein said exposing said test compound to said cell occurs in a setting selected from the group consisting of an in vitro setting, an in vivo setting, an in vitro setting, and an ex vivo setting.
