Serine protease inhibitors

Details Serine protease inhibitors Serine protease inhibitors

C - Chemistry, Metallurgy

07

K

C07K 19/00 (2006.01) A61K 38/55 (2006.01) C07F 5/04 (2006.01) C07K 1/04 (2006.01) C07K 5/06 (2006.01) C07K 14/81 (2006.01) C07K 14/815 (2006.01) C12N 9/64 (2006.01) C12N 9/68 (2006.01) C12N 9/96 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2258634

Bifunctional serine protease inhibitors and methods of preparing boron- containing peptides are provided. The serine protease inhiitors comprise a catalytic site-directed moiety, which binds to and inhibits the active site of a serine protease, and an exosite associating moiety, which are joined by a connector moiety. The catalytic site directed moiety and the exosite associating moiety are capable of binding simultaneously to a molecule of the serine protease.

L'invention concerne des inhibiteurs bifonctionnels de la sérine protéase et des procédés de préparation de peptides contenant du bore. Ces inhibiteurs comprennent une fraction catalytique dirigée qui se lie au site actif d'une sérine protéase et l'inhibe, et une fraction se liant à un exosite, ces deux fractions étant réunies par une fraction de couplage. La fraction dirigée catalytique et la fraction se liant à un exosite sont capables de se lier simultanément à une molécule de la sérine protéase.

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