In vitro stability of α-helical peptide nucleic acids (αPNAs)

被引:11
作者
Garner, P [1 ]
Sherry, B [1 ]
Moilanen, S [1 ]
Huang, YM [1 ]
机构
[1] Case Western Reserve Univ, Dept Chem, Cleveland, OH 44106 USA
关键词
D O I
10.1016/S0960-894X(01)00422-X
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
alpha -helical peptide nucleic acids (alpha PNAs) are synthetic molecules that merge the a-helix secondary structure of peptides with the codified Watson-Crick base pairing capability of nucleic acids. It is now demonstrated that aPNAs made up of either L- Or D-amino acids are resistant to degradation by the proteases present in human serum. The increased stability of aPNAs towards proteases may be attributable to the presence of unnatural nucleoamino acid residues [-NHCH(CH2OCH2B)CO, where B = thymine or cytosine] since the replacement of these amino acids by serine yields a control peptide that does break down in human serum. The stability of alpha PNAs towards proteases makes them attractive candidates for further development as antisense agents. (C) 2001 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:2315 / 2317
页数:3
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