Patent ID: 11857600
Assignee: GPCR THERAPEUTICS, INC.
Field: Pharmaceuticals (Chemistry)
Classification: CPC A  C | IPC A  C

Claim 3:
4. The method of claim 2, wherein the CXCR4-HRH1 heteromer has two or more of the following characteristics:
1. the CXCR4-HRH1 heteromer components in a cancer cell colocalize and physically interact, either directly or via intermediate proteins acting as conduits for allosterism, as determined via one or more of the following: a co-internalization assay, a colocalization assay, in situ hybridization, immunohistochemistry, immunoelectron microscopy, a proximity-based assay, a co-immunoprecipitation assay, enzyme-linked immunosorbent assay (ELISA), flow cytometry, RNAseq, qRT-PCR, microarray, or a fluorescent animal assay;
2. an enhanced amount of calcium mobilization such that:
a) either CXCR4 or HRH1 in an individual protomer context in a cancer cell, upon co-stimulation with CXCL12 and a selective HRH1 agonist, results in a calcium mobilization amount that is equal to or less than the sum of calcium mobilization amounts resulting from single agonist stimulation with either the CXCL12 or the HRH1 agonist; and
b) the CXCR4-HRH1 heteromer exhibits an enhanced calcium mobilization upon co-stimulation with the CXCL12 and the selective HRH1 agonist relative to the sum of calcium mobilization amounts resulting from single agonist stimulation with either the CXCL12 or the selective HRH1 agonist;
as determined via a calcium mobilization assay; or

3. a CXCR4-HRH1 heteromer-selective reagent:
a) alters heteromer-specific properties of the CXCR4-HRH1 heteromer in the cancer cell;
b) alters heteromer-specific function of the CXCR4-HRH1 heteromer in the cancer cell;
c) alters heteromer-specific properties of the cancer cell containing the CXCR4-HRH1 heteromer; or
d) decreases cancer progression of the cancer cell containing the CXCR4-HRH1 heteromer.