Process for the modulation of the antagonistic activity of a...

C - Chemistry – Metallurgy – 07 – K

Patent

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C07K 16/00 (2006.01) A61K 39/395 (2006.01) A61P 35/00 (2006.01) C07K 16/28 (2006.01) C07K 16/46 (2006.01)

Patent

CA 2744065

The present disclosure relates to the antibody engineering field and, more particularly, to a process for the screen-ing of antibodies and/or the modulation of the agonistic/antagonistic activity of antibodies. More particularly, the disclosure con-cerns a process of improving the antagonistic activity of a monoclonal antibody directed against a specific target molecule, or a divalent functional fragment or derivative thereof, said antibody being capable of inhibiting one or more of the biological activities of said target molecule, wherein said process comprises a stage of reconfiguration of the hinge region consisting of a modification of the amino acid sequence of said hinge region by the deletion, the addition or the substitution of at least one amino acid. The disclosure also relates to polypeptides useful for such a modulation method and the obtained antibodies.

L'invention a trait au domaine de l'ingénierie des anticorps et plus particulièrement à un procédé de criblage d'anticorps et/ou de modulation de l'activité agoniste ou antagoniste d'anticorps, et plus particulièrement encore à un procédé améliorant l'activité antagoniste d'un anticorps monoclonal dirigé contre une molécule cible spécifique ou contre l'un de ses fragments fonctionnels divalents ou l'un de ses dérivés, ledit anticorps étant capable d'inhiber une ou plusieurs des activités biologiques de ladite molécule cible, et ledit procédé comportant une étape de reconfiguration de la région charnière, consistant à modifier la séquence d'acides aminés de ladite région par suppression, addition ou substitution d'au moins un acide aminé. L'invention porte également sur des polypeptides utilisables dans ladite méthode de modulation, et sur les anticorps ainsi obtenus.

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