C - Chemistry – Metallurgy – 12 – N
Patent
C - Chemistry, Metallurgy
12
N
C12N 15/11 (2006.01) A61K 38/07 (2006.01) A61K 38/08 (2006.01) A61K 38/10 (2006.01) C07K 1/04 (2006.01) C07K 4/00 (2006.01) C07K 5/10 (2006.01) C07K 7/06 (2006.01) C07K 7/08 (2006.01) C07K 14/81 (2006.01) C07K 16/38 (2006.01) C07K 16/44 (2006.01) C12N 15/10 (2006.01) C12Q 1/37 (2006.01) C12Q 1/42 (2006.01) C12Q 1/48 (2006.01) G01N 33/53 (2006.01)
Patent
CA 2257873
The invention provides substrate substraction libraries and methods of using substrate substraction libraries to identify highly selective substrates for enzymes which use peptides as substrates. In one embodiment, substrates for proteases such as t-PA and u-PA have been identified whose relative reactivities towards the two enzymes vary by a factor of more than 9000. The substrates identified by the present invention are useful for the construction of highly selective enzyme inhibitors.
La présente invention se rapporte à des banques de soustraction de substrats et à des procédés d'utilisation de telles banques pour identifier des substrats hautement sélectifs associés à des enzymes qui utilisent des peptides en tant que substrats. Dans une réalisation, on a identifié des substrats destinés à des protéases du type t-PA et u-PA, les réactivités relatives desdits substrats envers les deux enzymes variant suivant un facteur supérieur à 9000. Les substrats identifiés par la présente invention servent à la fabrication d'inhibiteurs d'enzymes très sélectifs.
Ke Song-Hua
Madison Edwin L.
Fetherstonhaugh & Co.
The Scripps Research Institute
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