Patent ID: 8957024
Filing Date: 2015-02-17
Classification: A61K,A61P,C07K

Abstract:
1. A method for inhibiting opioid-induced internalization of gastrin-releasing peptide receptor (GRPR) in a neuron expressing GRPR in a subject, the method comprising administering to the subject a composition comprising a cell-penetrating peptide fused to the C-terminus of an agent that inhibits the interaction of GRPR with μ opioid receptor 1D (MOR1D), wherein the agent consisting of at least 5 and up to 22 contiguous amino acids of SEQ ID NO: 245 (EHPSTANTVDRTNHQRNEEPSS) wherein the at least 5 contiguous amino acids are selected from the group consisting of SEQ ID NO: 22 (RNEEP), SEQ ID NO: 25 (NEEPS) and SEQ ID NO: 28 (EEPSS), such that the agent inhibits opioid-induced internalization of GRPR by inhibiting the interaction of GRPR with MOR1D, and wherein the cell-penetrating peptide is selected from the group consisting of SEQ ID NO: 549, SEQ ID NO: 550, SEQ ID NO: 551, SEQ ID NO: 552, SEQ ID NO: 553, SEQ ID NO: 554, SEQ ID NO: 555, SEQ ID NO: 556, SEQ ID NO: 557, SEQ ID NO: 558, SEQ ID NO: 559, SEQ ID NO: 560, SEQ ID NO: 561, SEQ ID NO: 562, SEQ ID NO: 563, SEQ ID NO: 564, SEQ ID NO: 565, SEQ ID NO: 566 and SEQ ID NO: 567.