Method for the production of cyclic molecules

C - Chemistry – Metallurgy – 12 – P

Patent

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C12P 21/00 (2006.01) A61K 38/12 (2006.01) C07K 1/107 (2006.01) C07K 5/12 (2006.01) C07K 7/06 (2006.01) C07K 7/50 (2006.01) C07K 7/64 (2006.01)

Patent

CA 2574733

The invention relates to a method for creating a cyclic form of peptides and proteins, in which method linear thioesters act as substrates. The cyclic formation is catalysed by thioesterase domains of NRPS or PKS cyclases. The inventive substrates consist of a linear peptide, to which a charge-stabilised aromatic, heteroaromatic or araliphatic leaving group is bonded. Said substrates permit high yields and reaction speeds of linear peptides that were created in cyclic form in prior art to be obtained and also permit the creation of a cyclic form for those peptides, for which such a process was previously impossible.

La présente invention concerne un procédé pour rendre cycliques des peptides et des protéines, dans lequel des thioesters linéaires servent de substrats. La mise sous forme de cyclique est catalysée par des domaines de thioestérase de cyclases NRPS ou PKS. Les substrats de l'invention consistent en un peptide linéaire auquel est lié un groupe partant aromatique, hétéroaromatique ou araliphatique. Ces substrats permettent d'obtenir des rendements élevés et des vitesses réactionnelles élevées des peptides linéaires qui pouvaient être rendus cycliques grâce aux procédés de l'état de la technique, et l'invention rend possible en outre la mise sous forme cyclique de peptides qui ne pouvaient l'être dans l'état de la technique.

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