Title:
SITE-SELECTIVE ACYL TRANSFER
Document Type and Number:
WIPO Patent Application WO2001085756
Kind Code:
A3
Abstract:
A method for site-selective acyl transfer in or amidation of folded polypeptides and proteins based on the use of a chemical structure element comprising an imidazole function, such as histidine, in position i flanked by at least one functional group to be amidated, such as lysine, in position i+3+4k, where k is an integer equal to or higher than -1, or in position i-4-4n, wherein n is an integer equal to or higher than 0, and at least one activating group, such as serine, in position i+4+4n or i-3-4n, respectively.
Inventors:
BALTZER LARS (SE)
Application Number:
PCT/SE2001/000987
Publication Date:
March 14, 2002
Filing Date:
May 07, 2001
Export Citation:
Assignee:
A & SCIENCE INVEST AB (SE)
BALTZER LARS (SE)
BALTZER LARS (SE)
International Classes:
A61K49/14; C07K1/00; C07K1/06; C07K14/00; C07K1/107; C07K1/113; (IPC1-7): C12N9/10; C07K1/10; C07K14/00
Domestic Patent References:
| WO1997043302A1 | 1997-11-20 | |||
| WO1998055501A1 | 1998-12-10 | |||
| WO2000032623A1 | 2000-06-08 |
Other References:
THOR J. BORGFORD: "Site-directed mutagenesis reveals transition-state stabilization", BIOCHEMISTRY, vol. 26, 1987, pages 7246 - 7249, XP000917994
KERSTIN S. BROO: "Cooperative neucleophilic and general-acid catalysis", J. AM. CHEM. SOC., vol. 120, no. 17, 1998, pages 4063 - 4068, XP002948865
JUN LI: "Conversion of serine-114 to cysteine-114 and the role of the active site nucleophile in acyl transfer by myristol-ACP thioesterase from vibrio harveyi+", BIOCHEMISTRY, vol. 35, no. 31, 1996, pages 9967 - 9973, XP002948866
KERSTIN S. BROO: "Cooperative neucleophilic and general-acid catalysis", J. AM. CHEM. SOC., vol. 120, no. 17, 1998, pages 4063 - 4068, XP002948865
JUN LI: "Conversion of serine-114 to cysteine-114 and the role of the active site nucleophile in acyl transfer by myristol-ACP thioesterase from vibrio harveyi+", BIOCHEMISTRY, vol. 35, no. 31, 1996, pages 9967 - 9973, XP002948866
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