Recombinant onconase, and chemical conjugates and fusion...

C - Chemistry – Metallurgy – 12 – N

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C12N 15/55 (2006.01) A61K 38/46 (2006.01) C07K 16/46 (2006.01) C07K 19/00 (2006.01) C12N 9/22 (2006.01) C12N 15/62 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2323631

Recombinantly-produced Onconase molecules and fusion proteins containing the same are disclosed. The recombinantly-produced Onconase molecule has the sequence of native Onconase, retains the proper folding of native Onconase and has cytotoxic activity similar to that of Onconase purified from oocytes of Rana pipiens. cDNA coding for Onconase is extended by one triplet which codes for N-formyl-methionine. When expressed recombinantly, the mutant Onconase has N-formyl-methionine as the N-terminal amino acid, and glutaminyl as the penultimate N-terminal residue. Following expression, the N-formyl methionine residue is cleaved and the penultimate glutaminyl residues are cyclized to produce Onconase with an N-terminal pyroglutamate residue, and hence the same structure and function as native Onconase.

L'invention concerne des molécules d'Onconase produites par recombinaison et des protéines de fusion contenant ces molécules. La molécule d'Onconase produite par recombinaison comporte une séquence d'Onconase native, conserve le repliement approprié de l'Onconase native et manifeste une activité cytotoxique semblable à celle de l'Onconase purifiée à partir des oocites de Rana pipiens. Le codage d'ADNc pour l'Onconase est élargi d'un triplet qui code pour N-formyl-méthionine. Exprimée par recombinaison, l'Onconase mutante possède N-formyl-méthionine en qualité d'acide aminé et glutaminyle en qualité de dernier résidu N-terminal. Après l'expression, le résidu N-formyl-méthionine est clivé et les derniers résidus de glutamynile sont cyclisées pour produire une Onconase avec un résidu de pyroglutamate N-terminale, qui possède, par conséquent, la même structure et les mêmes fonctions que l'Onconase native.

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