role of helicity on the anticancer mechanism of action of cationic-helical peptides角色上的螺旋性抗癌cationic-helical肽的作用机制.pdfVIP

Int. J. Mol. Sci. 2012, 13, 6849-6862; doi:10.3390/ijm OPEN ACCESS International Journal of Molecular Sciences ISSN 1422-0067 /journal/ijms Article Role of Helicity on the Anticancer Mechanism of Action of Cationic-Helical Peptides Yi-Bing Huang 1, Li-Yan He 1, Hong-Yu Jiang 2,* and Yu-Xin Chen 1,* 1 Key Laboratory for Molecular Enzymology and Engineering of the Ministry of Education, Jilin University, Changchun 130012, China; E-Mails: huangyibing@ (Y.-B.H.); heliyan415@163.com (L.-Y.H.) 2 The First Hospital, Jilin University, Changchun 130021, China * Authors to whom correspondence should be addressed; E-Mails: jiang_hy@ (H.-Y.J.); chen_yuxin@ (Y.-X.C.); Tel.: +86-431(H.-Y.J.); +86-431(Y.-X.C.); Fax: +86-431(H.-Y.J.); +86-431(Y.-X.C.). Received: 20 April 2012; in revised form: 19 May 2012 / Accepted: 22 May 2012 / Published: 5 June 2012 Abstract: In the present study, the 26-residue amphipathic α-helical peptide A12L/A20L (Ac-KWKSFLKTFKSLKKTVLHTLLKAISS-amide) with strong anticancer activity and specificity was used as the framework to study the effects of helicity of α-helical anticancer peptides on biological activities. Helicity was systematically modulated by introducing D-amino acids to replace the original L-amino acids on the non-polar face or the polar face of the helix. Peptide helicity was measured by circular dichroism spectroscop