摘要:
The invention relates to a method for evaluation of a compound-target interaction in vivo, comprising the steps of administering the compound to an animal, taking a body fluid sample of the animal, determining the concentration of the compound in the body fluid sample, taking a cellular sample of the animal containing the target, preparing a protein preparation of said cellular sample, providing an immobilised ligand capable of binding to the target, contacting the protein preparation with the immobilised ligand under conditions allowing the formation of a complex between the immobilised ligand and the target, determining the amount of complexes formed in step, and correlating the amount of complexes with the concentration of the compound in the body fluid sample.
摘要:
The present invention relates to a process for the isolation and identification of pharmaceutically relevant target compounds (TC) from a sample, said sample being derived from a living organism, wherein said target compound(s) bind(s) to a compound of interest (COI) under physiological conditions, said compound of interest (COI) being associated with a given impaired condition or disease. This process involves the isolation and the purification of the complex(es) formed by the compound. The present invention also relates to a process for the identification of a pharmaceutically effective compound useful for preventing and/or treating a given impaired condition or disease, wherein said compound is identified by its binding to a relevant target compound (TC) that has been identified and isolated according to the above mentioned process. Furthermore, the present application concerns a process for the identification of new uses (i.e. medical indications) of an active agent involving identifying diseases associated with the binding partner(s) of the active agent.
摘要:
The present invention relates to methods for the characterization of enzymes or of enzyme-compound complexes, wherein the enzyme is obtained from a protein preparation with the help of at least one broad spectrum ligand immobilized on a solid support and wherein the enzyme is characterized by mass spectrometry. These methods are useful for the screening of non-immobilized compound libraries, selectivity profiling of lead compounds and mechanism of action studies in living cells.
摘要:
The present invention relates to methods for the identification and characterization (e.g. selectivity profiling) of HDAC interacting compounds using protein preparations derived from cells endogenously expressing HDACs or cell preparations containing said HDACs.