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公开(公告)号：EP1079859A1
公开(公告)日：2001-03-07
申请号：EP99924431.2
申请日：1999-05-21
发明人： BRIESEWITZ, Roger , CRABTREE, Gerald, R. , WANDLESS, Thomas , RAY, Gregory, Thomas , VOGEL, Kurt, William
IPC分类号： A61K39/385
CPC分类号： C12N9/90 , A61K38/00 , A61K47/54 , A61K47/552 , C07K5/1027 , C07K7/06 , C07K2319/00 , Y10S530/812
摘要： The disclosed invention describes bifunctional conjugates of the form Z-L-X, where Z is a ligand that binds to a specific protein, X is a drug moiety (e.g. antimicrobial agent, etc.), and L is an optional linker. The design of the conjugate is such that upon entering a cell, the ligand Z can bind to its receptor protein (if such a receptor protein is present) and the drug's effectiveness is thereby enhanced or inhibited, depending on the nature of Z's receptor.
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2.发明公开BIFUNCTIONAL MOLECULES AND THEIR USE IN THE DISRUPTION OF PROTEIN-PROTEIN INTERACTIONS 审中-公开双功能分子及其用途蛋白 - 蛋白相互作用的销毁
公开(公告)号：EP1230353A1
公开(公告)日：2002-08-14
申请号：EP00980512.8
申请日：2000-11-17
CPC分类号： A61K47/62
摘要： 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.
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3.发明公开BIFUNCTIONAL MOLECULES HAVING MODULATED PHARMACOKINETIC PROPERTIES AND THERAPIES BASED THEREON 审中-公开用调制的药代动力学特性和基于事实的治疗双功能分子
公开(公告)号：EP1229793A1
公开(公告)日：2002-08-14
申请号：EP00983722.0
申请日：2000-11-17
IPC分类号： A01N61/00 , A61K38/00 , A61K38/43 , C12N11/00 , C12N11/02 , C07K1/00 , C07K17/00 , C07K17/02 , C07K17/06
摘要： Bifunctional molecules and methods for their use are provided. The subject bifunctional molecules are conjugates of a drug moiety and a pharmacokinetic modulating moiety, where these two moieties are optionally joined by a linking group. The bifunctional molecules are further characterized in that they exhibit at least one modulated pharmacokinetic property upon administration to a host as compared to a free drug control. The subject bifunctional molecules find use in a variety of therapeutic applications.
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