Process for the deacylation of cyclic lipopeptides

Details Process for the deacylation of cyclic lipopeptides Process for the deacylation of cyclic lipopeptides

C - Chemistry, Metallurgy

12

N

C12N 9/80 (2006.01) C07K 7/56 (2006.01) C12N 1/20 (2006.01) C12P 21/04 (2006.01)

Patent

CA 2248348

There is provided a cyclic lipopeptide acylase which is capable of deacylating the acyl side chain of a cyclic lipopeptide compound, e.g. Substance FR901379 or its analog, of the following general formula [ I] with effectiveness as well a method of producing a cyclic peptide compound which comprises using the acylase. (see above formula) [wherein R1 is acyl; R2 is hydroxy or acyloxy; R3 is hydrogen or hydroxy; R4 is hydrogen or hydroxy; R5 is hydrogen or hydroxysulfonyloxy; and R6 is hydrogen or carbamoyl.]

Cette invention concerne une acylase de lipopeptide cyclique qui permet d'éliminer efficacement une chaîne latérale acyle d'un lipopeptide cyclique. D'une manière plus spécifique, cette invention concerne l'élément FR901379 correspondant à la formule générale (I) où R<1> représente acyle, R<2> représente hydroxy ou acyloxy, R<3> représente hydrogène ou hydroxy, R<4> représente hydrogène ou hydroxy, R<5> représente hydrogène ou hydroxysulfonyloxy, et R<6> représente hydrogène ou carbamoyle. Cette invention concerne également des analogues de l'élément FR901379, ainsi qu'un processus de préparation d'un peptide cyclique à l'aide de l'acylase.

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