Abstract
Aptamers are nucleic acids referred to as chemical antibodies as they bind to their specific targets with high affinity and selectivity. They are selected via an iterative process known as ‘selective evolution of ligands by exponential enrichment’ (SELEX). Aptamers have been developed against numerous cancer targets and among them, many tumor cell-membrane protein biomarkers. The identification of aptamers targeting cell-surface proteins has mainly been performed by two different strategies: protein- and cell-based SELEX, when the targets used for selection were proteins and cells, respectively. This review aims to update the literature on aptamers targeting tumor cell surface protein biomarkers, highlighting potentials, pitfalls of protein- and cell-based selection processes and applications of such selected molecules. Aptamers as promising agents for diagnosis and therapeutic approaches in oncology are documented, as well as aptamers in clinical development.
Highlights
Nucleic acid aptamers are single stranded DNA or RNA molecules
Doxorubicin, a chemotherapeutic agent extensively used in the treatment of various cancers, has often been used as a drug non-covalently conjugated to aptamers containing CG/GC sequences or covalently conjugated to aptamer through a functional linker [87]
This study showed a low level of activity of AS1411 in patients with metastatic RRC
Summary
Nucleic acid aptamers are single stranded DNA (ssDNA) or RNA molecules. They are selected through a fully in vitro well-established iterative process known as ‘selective evolution of ligands by exponential enrichment’ (SELEX) [1,2,3]. Identification of aptamers is more complex for cell-surface proteins which activities depend on their conformation and on their cellular environment than for non-amphipatic molecules. This review will focus on the main selection strategies which have been used to identify aptamers to tumor cell-surface proteins, highlighting differences, success, and limitations of the SELEX processes. Involved in cell growth and migration, tumor invasion, metastasis and angiogenesis. Implicated in tumor cell adhesion to vascular endothelium, migration, proliferation of cancer cells and step of metastasis formation. EGFR is a receptor tyrosine kinase expressed at the surface of cell. Co-stimulatory receptor implicated in survival and expansion of activated T cells. Implicated in survival and in suppressor activity of myeloid derived suppressor cells Member of the immunoglobulin-like super family. Role in mRNA stabilization (example: role in stabilization of bcl-2 mRNA in human leukemia)
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