US 7,572,884 B2
Method for making acylated polypeptides
Thomas Hoeg-Jensen, Klampenborg (Denmark); Michi Egel-Mitani, Vedbaek (Denmark); Per Balschmidt, Espergaerde (Denmark); Jan Markussen, Herlev (Denmark); and Ivan Diers, Vaerlose (Denmark)
Assigned to Novo Nordisk A/S, Bagsvaerd (Denmark)
Filed on Jul. 28, 2005, as Appl. No. 11/191,574.
Application 11/191574 is a continuation of application No. 10/205270, filed on Jul. 24, 2002, abandoned.
Claims priority of provisional application 60/310952, filed on Aug. 08, 2001.
Claims priority of application No. 2001 01140 (DK), filed on Jul. 24, 2001.
Prior Publication US 2005/0272125 A1, Dec. 08, 2005
Int. Cl. A61K 38/00 (2006.01); A61K 38/04 (2006.01)
U.S. Cl. 530—345  [530/330; 530/329; 530/324; 514/2; 514/12] 6 Claims
 
1. A method for making GLP-1 or a GLP-1 analogue comprising at least one lysine residue being acylated in its ε-amino group, said method comprising the following steps:
(i) culturing a host cell comprising a polynucleotide sequence encoding a precursor molecule of the GLP-1 or GLP-1 analogue under suitable conditions for expression of the precursor molecule said precursor molecule comprising an N-terminal extension capable of protecting the GLP-1 or GLP-1 analogue against proteolytic degradation, said N-terminal extension comprising: i) a sequence of Glu-Glu-Ala-Glu(SEQ ID NO:27), and ii) a cleavage site positioned at its C-terminal end for cleavage from the GLP-1 or GLP-1 analogue, wherein the cleavage site is not a Lys;
(ii) separating the expressed precursor from the culture broth;
(iii) acylating the ε-amino group of at least one lysine residue in the desired polypeptide;
(iv) removing the N-terminal extension by chemical and/or enzymatic cleavage and isolating the acylated polypeptide by suitable means,
wherein said GLP-1 or GLP-1 analogue is a peptide of GLP-1(7-36) or GLP-1(7-37).