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US 12,286,480 B2Granted
Modulators of ROR1-ROR2 binding
AssigneeThe Regents of the University of California
InventorsThomas J. Kipps, Jian Yu
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Abstract
Provided herein are, inter alia, methods of identifying agents that are capable of inhibiting the binding (e.g., coupling) between a ROR1 protein and a ROR2 protein. By interfering with ROR1-ROR2 coupling (binding) the agents identified using the methods provided herein inhibit non-canonical Wnt5a signaling. Thus, the agents identified by the methods provided herein may, inter alia, be useful for cancer diagnosis and therapy.
Claims17
A method of identifying an inhibitor of ROR1-ROR2 binding, said method comprising:
- (i) combining a test agent with a ROR1 protein and a ROR2 protein in a reaction vessel;
- (ii) detecting a decrease in binding of said ROR1 protein to said ROR2 protein relative to a standard control;
- and
- (iii) detecting a level of a guanine exchange factor (GEF) protein binding activity to said ROR1 protein or said ROR2 protein in the presence of said test agent, wherein a decreased level of said GEF protein binding activity relative to a standard control indicates said test agent is an inhibitor of ROR1-ROR2 binding;
- and wherein said GEF protein is ARHGEF1, ARHGEF2, or ARHGEF6.
2 more elements
Dependencies are inferred from the claim text.