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1. (WO2001036612) BIFUNCTIONAL MOLECULES AND THEIR USE IN THE DISRUPTION OF PROTEIN-PROTEIN INTERACTIONS

Pub. No.:    WO/2001/036612    International Application No.:    PCT/US2000/031695
Publication Date: Sat May 26 01:59:59 CEST 2001 International Filing Date: Sat Nov 18 00:59:59 CET 2000
IPC: A61K 47/48
Applicants: THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITY
CRABTREE, Gerald, R.
STANKUNAS, Kryn
BRIESEWITZ, Roger
WANDLESS, Thomas
Inventors: CRABTREE, Gerald, R.
STANKUNAS, Kryn
BRIESEWITZ, Roger
WANDLESS, Thomas
Title: BIFUNCTIONAL MOLECULES AND THEIR USE IN THE DISRUPTION OF PROTEIN-PROTEIN INTERACTIONS
Abstract:
Bifunctional inhibitor molecules and methods for their use in the inhibition of protein-protein interactions are provided. The subject bifunctional inhibitor molecules are conjugates of a target protein ligand and a blocking protein ligand, where these two moieties are optionally joined by a linking group. In the subject methods, an effective amount of the bifunctional inhibitor molecule is administered to a host in which the inhibition of a protein-protein interaction is desired. The bifunctional inhibitor molecule simultaneously binds to its corresponding target and blocking proteins to produce a tripartite complex that inhibits the target protein-protein interaction. The subject methods and compositions find use in a variety of applications, including therapeutic applications.