Molecularly Engineering Triptolide with Aptamers for High Specificity and Cytotoxicity for Triple-Negative Breast Cancer

Abstract

Triple-negative breast cancer (TNBC) lacks three important receptors, ER, PR, and HER2. It is more aggressive and more likely to relapse after treatment, thus has been identified as one of the most malignant breast cancer types. The development of efficient targeted TNBC therapy is an important research topic in TNBC treatment. We report the development of a new aptamer–drug conjugate (ApDC), AS1411–triptolide conjugate (ATC), as targeted therapy for the treatment of TNBC with high efficacy. The conjugate possesses excellent specificity and high cytotoxicity against the MDA-MB-231 cell line. The advantages of our newly invented ATC are further highlighted by its excellent in vivo anti-TNBC efficacy and negligible side effects toward healthy organs.

Triple-Negative Breast Cancer: A Review of Conventional and Advanced Therapeutic Strategies

“…Various aptamers have been developed for therapy in TNBC; for example, the aptamer 5TR1 pursues the molecular target MUC1 which is a tumor protein in MDA-MB-231, the researchers have conjugated 5TR1 to Doxorubicin to make it more specific and avoid the known side effects such as cardiotoxicity [147]. He et al have reported aptamer-drug conjugate (ApDC), AS1411-triptolide conjugate (ATC) for TNBC therapeutics with higher efficacies [148]. Nanomedicine is advancing rapidly, and now researchers have focused on combining all the technologies mentioned above (siRNA, miRNA, aptamers) by loading them into nanoparticles that pursue the CD-44 receptor characteristic of TNBC pluripotent cells [149].…”

In Situ Silver-based Electrochemical Bioreactor In Vivo

“…Aptamer-mediated targeting assay in vitro AS1411 speci cally targets nucleolin, which is overexpressed by many tumors [30][31][32] . Therefore, we investigated the internalization of AS1411-CS/rGO/Ag + -DNA into HepG2 cells, which overexpress nucleolin.…”

Rational design of aqueous conjugated polymer nanoparticles as potential theranostic agents of breast cancer

“…44,45 Generally, most breast cancer diagnoses are related to luminal tumors, 20% relates to those that overexpress HER2, while only 15% refers to TNBC subtype. 44 Even though the percentage of TNBC tumors among all breast cancer cases is relatively low, they represent the most aggressive phenotype 46 with the highest rate of metastasis to other healthy organs, high proliferative index, high recurrence rate (o5 years), 47 and a worse prognosis. 48 Nowadays, the most common treatments for TNBC patients include surgery, radiotherapy and chemotherapy.…”

“…48 Nowadays, the most common treatments for TNBC patients include surgery, radiotherapy and chemotherapy. 46,49 During the last few years, CPNs have been reported as promising materials in photodynamic therapy of breast cancers. [49][50][51] In this contribution, we performed in vitro studies in order to evaluate the cytotoxicity effects of the T2fQf and T2fQ2f (chemical structures on Fig.…”