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Computer-Aided Design of Lasso-like Self-Assembling Anticancer Peptides with Multiple Functions for Targeted Self-Delivery and Cancer Treatments

ACS Nano. 2022-09; 
Pengfei Pei , Long Chen , Ruru Fan , Xi-Rui Zhou , Shan Feng , Hangrui Liu , Quanqiang Guo , Huiwei Yin , Qiang Zhang , Fude Sun , Liang Peng , Peng Wei , Chengzhi He , Renzhong Qiao , Zai Wang , Shi-Zhong Luo
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Peptide Synthesis All peptides used in this study were synthesized by GenScript Co., Ltd. (Nanjing, China), and the peptide sequences are listed in Table 1. Get A Quote


Anticancer peptides are promising drug candidates for cancer treatment, but the short circulation time and low delivery efficiency limit their clinical applications. Herein, we designed several lasso-like self-assembling anticancer peptides (LASAPs) integrated with multiple functions by a computer-aided approach. Among these LASAPs, LASAP1 (CRGDKGPDCGKAFRRFLGALFKALSHLL, 1-9 disulfide bond) was determined to be superior to the others because it can self-assemble into homogeneous nanoparticles and exhibits improved stability in serum. Thus, LASAP1 was chosen for proving the design idea. LASAP1 can self-assemble into nanoparticles displaying iRGD on the surface because of its amphiphilic structure and accumulate t... More


anticancer peptide; multitargeting; nanoparticle; self-assembling; self-delivery.