Abstract
The arrival of the monoclonal antibody (mAb) technology in the 1970s brought with it the hope of conquering cancers to the medical community. However, mAbs, on the whole, did not achieve the expected wonder in cancer therapy although they do have demonstrated successfulness in the treatment of a few types of cancers. In 1990, another technology of making biomolecules capable of specific binding appeared. This technique, systematic evolution of ligands by exponential enrichment (SELEX), can make aptamers, single-stranded DNAs or RNAs that bind targets with high specificity and affinity. Aptamers have some advantages over mAbs in therapeutic uses particularly because they have little or no immunogenicity, which means the feasibility of repeated use and fewer side effects. In this review, the general properties of the aptamer, the advantages and limitations of aptamers, the principle and procedure of aptamer production with SELEX, particularly the undergoing studies in aptamers for cancer therapy, and selected anticancer aptamers that have entered clinical trials or are under active investigations are summarized.
Highlights
The advent of the technology of using B lymphocyte hybridomas to produce monoclonal antibodies in the 1970s gave the medical world a ray of hope to conquer cancers because monoclonal antibody (mAb) are capable of binding to target molecules, such as tumor antigens and carrying cytotoxic agents selectively to cancer cells, which means effective destruction of cancer cells with minimum damage to normal cells
This paper summarizes the general properties of the aptamer, the advantages and limitations of aptamers compared with mAbs, the principle and procedure of aptamer production with systematic evolution of ligands by exponential enrichment (SELEX), () the undergoing investigations into aptamer’s applications in cancer treatment, and selected aptamers that have entered clinical trials or are under active investigation for cancer therapy
Other nanoparticle–aptamer conjugates that have been reported far include: conjugating the anti-CD44 aptamer to liposomes loaded with siRNA for gene silencing in CD44-expressing tumor cells in vivo [142], mucin1 aptamer-conjugated chitosan nanoparticles loaded with docetaxel and cMET siRNA that was delivered into mucin1 positive SKBR3 breast cancer cells [143], LA1 aptamer-conjugated grapefruit-derived nanovectors harboring Dox and P-glycoprotein siRNA that could be internalized into multidrug resistance LoVo colon cancer cells [144], self-assembled DNA nanostructures (DNA nanoprisms) decorated with therapeutic siRNAs targeting the GTPase Rab26 and MUC-1 aptamers that target non-small cell lung cancer [145], and paclitaxel-encapsulated PEGylated PLGA nanoparticles that were surface-functionalized with the heparanase aptamers targeting triple-negative breast cancers [146]
Summary
The advent of the technology of using B lymphocyte hybridomas to produce monoclonal antibodies (mAbs) in the 1970s gave the medical world a ray of hope to conquer cancers because mAbs are capable of binding to target molecules, such as tumor antigens and carrying cytotoxic agents selectively to cancer cells, which means effective destruction of cancer cells with minimum damage to normal cells. There has already been an aptamer called Macugen (Pegaptanib Sodium Injection) being approved by the US Food and Drug Administration (FDA) for therapeutic application. This aptamer targets vascular endothelial growth factor (VEGF) and is used for the treatment of age-related macular degeneration (AMD) [5]. This paper summarizes the general properties of the aptamer, the advantages and limitations of aptamers compared with mAbs, the principle and procedure of aptamer production with SELEX, () the undergoing investigations into aptamer’s applications in cancer treatment, and selected aptamers that have entered clinical trials or are under active investigation for cancer therapy
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