Site-selective acyl transfer

Details Site-selective acyl transfer Site-selective acyl transfer

2007-06-12

2007-06-12

Nashed, Nashaat T. (Department: 1656)

Chemistry: natural resins or derivatives; peptides or proteins;

Peptides of 3 to 100 amino acid residues

C530S350000

Reexamination Certificate

active

10258445

ABSTRACT:
A method for site-selective acyl transfer in 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 lysinc, 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.

REFERENCES:
patent: 6171819 (2001-01-01), Ahlberg et al.
patent: WO 97/43302 (1997-11-01), None
patent: WO 98/55501 (1998-12-01), None
patent: WO 00/32623 (2000-06-01), None
Biochemistry 1987, “Site-Directed Mutagenesis Reveals Transition-State Stabilization” Thor J. Borgford, Abstract, p. 7247 col. 2 line 23—p. 7249 col. 2 line 27.
J. Am. Chem. Soc. 1998, “Cooperative Neucleophilic and General-Acid Catalysis”, Kerstin S. Broo, Abstract, p. 4063 col. 2 line 5-15, p. 4064 col. 2 line 32—p. 4067 col. 2 line 14.
Biochemistry 1996, “Conversion of Serine-114 to Cysteine-114 and the Role of the Active Site Nucleophile in Acyl Transfer by Myristol-ACP Thioesterase fromVibrio harveyi+”, Jun Li, Abstract, p. 9968 col. 1 line 25-35, p. 9971 col. 1 line 32—p. 9972 col. 2 line 15.

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