268
Q. Lv et al.
9.8 Conclusion and Perspectives
Aptamers have been identified and selected against a huge quantity of cancer targets
over the past three decades, and a great progress has been made in their variety,
affinity, and chemical diversity. The classic process for new aptamers discovery and
validation depended on the SELEX technique seems too tedious with low efficiency.
The automated systems address one promising solution to this obstacle, which could
finish successful selection in less than one week [168]. In recent years, in silico postSELEX screening has been proved as another powerful tool to offer aptamers with
higher affinity [169, 170]. In practical applications, aptamers are required to have
a picomolar-ranged binding affinity, abundant chemical diversity, and explicit good
pharmacological behavior (as pharmacokinetics, pharmacodynamics, and cytotoxicity). More importantly, the effects of aptamers on the regulation of normal gene
expression in the natural eukaryotic system should be carefully confirmed.
It is well known that early diagnosis of cancer could effectively benefit to low
mortality rate through proving accurate judgment of disease development and giving
early intervention to treatment. By serving as a recognition element, aptamers have
been employed in many analysis methods for early cancer diagnosis. However, most
aptamer-based techniques still remain at the proof-of-concept level. The commercialization of these novel detection techniques suffers from the complexity of clinical
samples and the above-mentioned limitations. Nevertheless, the unique advantages
of aptamer molecules provide a strong incentive toward extending their use in more
fields, including the clinical application in early diagnosis and therapeutics. From
what has been discussed in this chapter, it is reasonable to believe that aptamers could
rise to be powerful members in imaging, cancer diagnosis, and therapy in the near
future.
References
1. Bray F, Ferlay J, Soerjomataram I, Siegel RL, Torre LA, Jemal A (2018) Global cancer
statistics 2018: GLOBOCAN estimates of incidence and mortality worldwide for 36 cancers
in 185 countries. CA-Cancer J Clin 68(6):394–424
2. Hassan EM, Willmore WG, DeRosa MC (2016) Aptamers: promising tools for the detection
of circulating tumor cells. Nucleic Acid Ther 26(6):335–347
3. Hanahan D, Weinberg Robert A (2011) Hallmarks of cancer: the next generation. Cell
144(5):646–674
4. Zichi D, Eaton B, Singer B, Gold L (2008) Proteomics and diagnostics: llet’s Get Specific,
again. Curr Opin Chem Biol 12(1):78–85
5. Shigdar S, Qiao L, Zhou S-F, Xiang D, Wang T, Li Y, Lim LY, Kong L, Li L, Duan W (2013)
RNA aptamers targeting cancer stem cell marker CD133. Cancer Lett 330(1):84–95
6. Tuerk C, Gold L (1990) Systematic evolution of ligands by exponential enrichment: RNA
ligands to bacteriophage T4 DNA polymerase. Science 249(4968):505–510
7. Stoltenburg R, Reinemann C, Strehlitz B (2007) SELEX-A (r)evolutionary method to generate
high-affinity nucleic acid ligands. Biomol Eng 24(4):381–403
8. Keefe AD, Pai S, Ellington A (2010) Aptamers as therapeutics. Nat Rev Drug Discov
9(7):537–550
Q. Lv et al.
9.8 Conclusion and Perspectives
Aptamers have been identified and selected against a huge quantity of cancer targets
over the past three decades, and a great progress has been made in their variety,
affinity, and chemical diversity. The classic process for new aptamers discovery and
validation depended on the SELEX technique seems too tedious with low efficiency.
The automated systems address one promising solution to this obstacle, which could
finish successful selection in less than one week [168]. In recent years, in silico postSELEX screening has been proved as another powerful tool to offer aptamers with
higher affinity [169, 170]. In practical applications, aptamers are required to have
a picomolar-ranged binding affinity, abundant chemical diversity, and explicit good
pharmacological behavior (as pharmacokinetics, pharmacodynamics, and cytotoxicity). More importantly, the effects of aptamers on the regulation of normal gene
expression in the natural eukaryotic system should be carefully confirmed.
It is well known that early diagnosis of cancer could effectively benefit to low
mortality rate through proving accurate judgment of disease development and giving
early intervention to treatment. By serving as a recognition element, aptamers have
been employed in many analysis methods for early cancer diagnosis. However, most
aptamer-based techniques still remain at the proof-of-concept level. The commercialization of these novel detection techniques suffers from the complexity of clinical
samples and the above-mentioned limitations. Nevertheless, the unique advantages
of aptamer molecules provide a strong incentive toward extending their use in more
fields, including the clinical application in early diagnosis and therapeutics. From
what has been discussed in this chapter, it is reasonable to believe that aptamers could
rise to be powerful members in imaging, cancer diagnosis, and therapy in the near
future.
References
1. Bray F, Ferlay J, Soerjomataram I, Siegel RL, Torre LA, Jemal A (2018) Global cancer
statistics 2018: GLOBOCAN estimates of incidence and mortality worldwide for 36 cancers
in 185 countries. CA-Cancer J Clin 68(6):394–424
2. Hassan EM, Willmore WG, DeRosa MC (2016) Aptamers: promising tools for the detection
of circulating tumor cells. Nucleic Acid Ther 26(6):335–347
3. Hanahan D, Weinberg Robert A (2011) Hallmarks of cancer: the next generation. Cell
144(5):646–674
4. Zichi D, Eaton B, Singer B, Gold L (2008) Proteomics and diagnostics: llet’s Get Specific,
again. Curr Opin Chem Biol 12(1):78–85
5. Shigdar S, Qiao L, Zhou S-F, Xiang D, Wang T, Li Y, Lim LY, Kong L, Li L, Duan W (2013)
RNA aptamers targeting cancer stem cell marker CD133. Cancer Lett 330(1):84–95
6. Tuerk C, Gold L (1990) Systematic evolution of ligands by exponential enrichment: RNA
ligands to bacteriophage T4 DNA polymerase. Science 249(4968):505–510
7. Stoltenburg R, Reinemann C, Strehlitz B (2007) SELEX-A (r)evolutionary method to generate
high-affinity nucleic acid ligands. Biomol Eng 24(4):381–403
8. Keefe AD, Pai S, Ellington A (2010) Aptamers as therapeutics. Nat Rev Drug Discov
9(7):537–550