Synthetic α-l-Threose Nucleic Acids Targeting BcL-2 Show Gene Silencing and in Vivo Antitumor Activity for Cancer Therapy

• DOI: 10.1021/acsami.9b14324
• Publication Date: 2019-09-26T14:18:46Z
• Authors: Fei Wang; Ling Sum Liu; Cia Hin Lau; Tristan Juin Han ...; Dick Yan Tam; Hoi Man Leung; Chung Tin; Pik Kwan Lo
• Keywords: Antisense therapy

We design and synthesize a sequence-defined α-l-threose nucleic acid (TNA) polymer, which is complementary to certain nucleotide sites of target anti-apoptotic proteins, BcL-2 involving in development progression tumors. Compared scramble TNA, anti-BcL-2 TNA significantly suppresses mRNA protein expression cancerous cells shows antitumor activity carcinoma xenografts, resulting suppression tumor cell growth induction death. Together with good biocompatibility, very low toxicity, excellent specificity features, strong binding affinity toward the RNAs, TNAs become new useful biomaterials effective alternatives traditional antisense oligonucleotides including locked acids, morpholino oligomers, peptide acids therapy. conventional cancer therapy such as radiotherapy, surgery, chemotherapy, we anticipate that this TNA-based polymeric system will work effectively shortly start play an important role practical application.