Mrg receptor modulators
AssigneeBayer Pharma Aktiengesellschaft
InventorsStefan GOLZ, Sina MICUS
Life of this patent
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Abstract
The present invention is in the field of molecular biology, more particularly, the present invention relates to drug screening, assay development and identification and use of modulators for G-protein coupled receptor/ligand pair MRGX2/CXCL14 within drug discovery.
Claims20
A method of screening for an antagonist of a Mrg receptor comprising the steps of
- a. contacting a test compound with a Mrg receptor polypeptide in the presence of a CXCL14 polypeptide,
- b. detecting binding of a CXCL14 polypeptide to said Mrg receptor polypeptide in the presence of said test compound,
- c. contacting CXCL14 with a Mrg receptor polypeptide in the absence of said test compound, and
- d. detecting binding of a CXCL14 polypeptide to said Mrg receptor polypeptide in the absence of said test compound.
A method of screening for an antagonist of a Mrg receptor comprising the steps of
- a. determining the activity of a Mrg receptor polypeptide in the presence of a CXCL14 polypeptide, and
- b. determining the activity of a Mrg receptor polypeptide in the presence of a CXCL14 polypeptide and a test compound.
A method of screening for an agonist of a Mrg receptor comprising the steps of
- a. generating a CXCL14 variant by replacing one or more amino acids of a CXCL14 polypeptide by another naturally or non-naturally occurring amino acid, and
- b. determining the activity of a Mrg receptor polypeptide in the presence of a CXCL14 variant.
An antagonist of CXCL14 activation of a Mrg receptor as a medicament.
A peptide comprised in the group of peptides consisting of fragment 1 (SEQ ID NO:
- 12), fragment 2 (SEQ ID NO:
- 13), fragment 4 (SEQ ID NO:
- 15), fragment 5 (SEQ ID NO:
- 16), fragment 9 (SEQ ID NO:
- 20), fragment 10 (SEQ ID NO:
- 21), and fragment 11 (SEQ ID NO:
- 22);
- or a variant thereof.
Dependencies are inferred from the claim text.