Hepatitis c virus ns5b polymerase inhibitor binding pocket

C - Chemistry – Metallurgy – 07 – K

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C07K 14/18 (2006.01) C12N 9/12 (2006.01)

Patent

CA 2522574

The HCV NS5B polymerase, when complexed with certain inhibitors, adopts a confirmation in which the finger loop region defined by amino acid residues 18 to 35 is displaced to expose a binding pocket defined generally by amino acid residues 392, 393, 395, 396, 399, 424, 425, 428, 429, 492, 493, 494, 495, 496, 500 and 503. This newly exposed binding pocket defines a novel target in the search of further chemical entities which are capable of binding to HCV NS5B and modulating, or preferably inhibiting, the polymerase activity of HCV NS5B.

La polymérase NS5B du VHC, lorsqu'elle est complexée avec certains inhibiteurs, adopte une conformation dans laquelle la région boucle du doigt définie par les restes d'acide aminé 18 à 35 est déplacée de manière qu'une poche de liaison définie généralement par les restes d'acide aminés, 392, 393, 395, 396, 399, 424, 425, 428, 429, 492, 493, 494, 495, 496, 500 et 503 soit exposée. Cette poche récemment exposée définit une nouvelle cible dans la recherche d'autres entités chimiques capables de se lier à NS5B du VHC et de moduler ou de préférence d'inhiber l'activité de polymérase de NS5B de VHC.

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