Active site inactivators

Details Active site inactivators Active site inactivators

C - Chemistry, Metallurgy

12

N

C12N 9/50 (2006.01) C12N 9/99 (2006.01) C12Q 1/34 (2006.01) C12Q 1/37 (2006.01) C12Q 1/42 (2006.01) C12Q 1/44 (2006.01) G01N 24/08 (2006.01)

Patent

CA 2444209

A method for identifying active site inhibitors of scission enzyme that cleaves the backbones or side groups of peptides, and for using the resultant inactivators to inhibit the target scission enzyme. Kinetic assays are employed to identify peptide substrates that tightly bind to the active site of the target protease but that are not easily cleaved. These noncleavable but tightly binding substrates are optionally structurally modified to yield inhibitory compounds with optimized properties. Additionally these substrates exhibit apparent specificity for a transition state or ground state configuration of the protease.

L'invention concerne une méthode d'identification d'inhibiteurs de site actif d'enzyme de scission clivant les squelettes ou groupes latéraux de peptides, et d'utilisation des inactivateurs obtenus pour inhiber l'enzyme de scission cible. Des dosages cinétiques sont utilisés pour identifier des substrats peptidiques se fixant étroitement au site actif de la protéase cible mais qui ne sont pas clivés facilement. Ces substrats non clivables mais à liaison étroite sont modifiés facultativement structuralement afin de produire des composés inhibiteurs aux propriétés optimisées. De plus, ces substrats présentent une spécificité apparente pour une configuration d'état de transition ou d'état fondamental de la protéase.

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