Synthesis of the Proteinase Inhibitor LEKTI Domain 6 by the Fragment Condensation Method and Regioselective Disulfide Bond Formation

被引：15
|
作者：
Vasileiou, Zoe [1 ]
Barlos, Kostas K. [1 ]
Gatos, Dimitrios [1 ]
Adermann, Knut [2 ]
Deraison, Celine [3 ]
Barlos, Kleomenis [1 ]
机构：
[1] Univ Patras, Dept Chem, GR-26010 Patras, Greece
[2] Pharis Biotec GmbH, D-30625 Hannover, Germany
[3] INSERM, U563, F-3130 Toulouse, France
来源：
BIOPOLYMERS | 2010年 / 94卷 / 03期
关键词：
fragment condensation; LEKTI domain 6; peptides; proteinase inhibitor; solid-phase synthesis; PROTECTED PEPTIDE-FRAGMENTS; NATIVE CHEMICAL LIGATION; LARGE-SCALE MANUFACTURE; SOLID-PHASE; UNPROTECTED PEPTIDES; IODINE OXIDATION; CYANOGEN-BROMIDE; SIDE REACTION; SERINE; CLEAVAGE;
D O I：
10.1002/bip.21376
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
Proteinase inhibitors are of high pharmaceutical interest and are drug candidates for a variety of indications. Specific kallikrein inhibitors are important for their antitumor activity and their potential application to the treatment of skin diseases. In this study we describe the synthesis of domain 6 of the kallikrein inhibitor Lympho-Epithilial Kazal-Type Inhibitor (LEKTI) by the fragment condensation method and site-directed cystine bridge formation. To obtain the linear LEKTI precursor, the condensation was best performed in solution, coupling the protected fragment 1-22 to 23-68. This method yielded LEKTI domain 6 of high purity and equipotent to the recombinantly produced peptide. (C) 2010 Wiley Periodicals, Inc. Biopolymers (Pept Sci) 94: 339-349, 2010.
引用
收藏
页码：339 / 349
页数：11
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