14 Perspectives of Aptamers for Medical Applications
447
Therefore, when the aptamer is tested in a laboratory environment, it should be
considered how to adapt to the human body environment when used in vivo, especially
the application of aptamer for targeted therapy and in vivo dynamic monitoring.
In short, as an emerging tool, aptamers have great potential in clinical applications.
Reasonable aptamer screening, appropriate aptamer modification, and conjugation
with multiple biological materials to enhance the facility are options for aptamers
in the future which will surely provide many possibilities for its applications in real
clinical scenarios. However, except for the opportunities, aptamers are also facing
challenges due to their limitations. Realizing the clinical transformation of aptamers
necessitates more research efforts and preclinical practices to overcome the problem
during the process from laboratory transform to clinical application. Nevertheless,
a large number of experimental studies and limited successful cases still give us
solidconfidence in the clinical application of aptamers in the near future.
References
1. Geiger A, Burgstaller P, von der Eltz H, Roeder A, Famulok M (1996) RNA aptamers that
bind L-arginine with sub-micromolar dissociation constants and high enantioselectivity. Nucl
Acids Res 24(6):1029–1036. https://doi.org/10.1093/nar/24.6.1029
2. Sassanfar M, Szostak JW (1993) An RNA motif that binds ATP. Nature 364(6437):550–553.
https://doi.org/10.1038/364550a0
3. Chen L, Rashid F, Shah A, Awan HM, Wu M, Liu A, Wang J, Zhu T, Luo Z, Shan G (2015)
The isolation of an RNA aptamer targeting to p53 protein with single amino acid mutation.
Proc Natl Acad Sci U S A 112(32):10002–10007. https://doi.org/10.1073/pnas.1502159112
4. Wu L, Zhu L, Huang M, Song J, Zhang H, Song Y, Wang W, Yang C (2019) Aptamer-based
microfluidics for isolation, release and analysis of circulating tumor cells. TrAC Trends Anal
Chem 117:69–77. https://doi.org/10.1016/j.trac.2019.05.003
5. Zhu G, Chen X (2018) Aptamer-based targeted therapy. Adv Drug Deliv Rev 134:65–78.
https://doi.org/10.1016/j.addr.2018.08.005
6. Pagratis NC, Bell C, Chang YF, Jennings S, Fitzwater T, Jellinek D, Dang C (1997) Potent 2 -
amino-, and 2 -fluoro-2 -deoxyribonucleotide RNA inhibitors of keratinocyte growth factor.
Nat Biotechnol 15(1):68–73. https://doi.org/10.1038/nbt0197-68
7. Shaw JP, Kent K, Bird J, Fishback J, Froehler B (1991) Modified deoxyoligonucleotides
stable to exonuclease degradation in serum. Nucl Acids Res 19(4):747–750. https://doi.org/
10.1093/nar/19.4.747
8. Monia BP, Johnston JF, Sasmor H, Cummins LL (1996) Nuclease resistance and antisense
activity of modified oligonucleotides targeted to Ha-ras. J Biol Chem 271(24):14533–14540.
https://doi.org/10.1074/jbc.271.24.14533
9. Liu Y, Kuan CT, Mi J, Zhang X, Clary BM, Bigner DD, Sullenger BA (2009) Aptamers
selected against the unglycosylated EGFRvIII ectodomain and delivered intracellularly reduce
membrane-bound EGFRvIII and induce apoptosis. Biol Chem 390(2):137–144. https://doi.
org/10.1515/bc.2009.022
10. Point of Care Diagnostics Market by Product (Glucose, Infectious Disease (Hepatitis
C, Influenza, Respiratory), Coagulation), Platform (Microfluidics, Immunoassays),
Mode (Prescription & OTC), End-User (Hospitals, Home Care) -Global Forecast
to 2024. https://www.marketsandmarkets.com/Market-Reports/point-of-care-diagnostic-mar
ket-106829185.html
11. Kropff J, Choudhary P, Neupane S, Barnard K, Bain SC, Kapitza C, Forst T, Link M, Dehennis
A, DeVries JH (2017) Accuracy and longevity of an implantable continuous glucose sensor in
447
Therefore, when the aptamer is tested in a laboratory environment, it should be
considered how to adapt to the human body environment when used in vivo, especially
the application of aptamer for targeted therapy and in vivo dynamic monitoring.
In short, as an emerging tool, aptamers have great potential in clinical applications.
Reasonable aptamer screening, appropriate aptamer modification, and conjugation
with multiple biological materials to enhance the facility are options for aptamers
in the future which will surely provide many possibilities for its applications in real
clinical scenarios. However, except for the opportunities, aptamers are also facing
challenges due to their limitations. Realizing the clinical transformation of aptamers
necessitates more research efforts and preclinical practices to overcome the problem
during the process from laboratory transform to clinical application. Nevertheless,
a large number of experimental studies and limited successful cases still give us
solidconfidence in the clinical application of aptamers in the near future.
References
1. Geiger A, Burgstaller P, von der Eltz H, Roeder A, Famulok M (1996) RNA aptamers that
bind L-arginine with sub-micromolar dissociation constants and high enantioselectivity. Nucl
Acids Res 24(6):1029–1036. https://doi.org/10.1093/nar/24.6.1029
2. Sassanfar M, Szostak JW (1993) An RNA motif that binds ATP. Nature 364(6437):550–553.
https://doi.org/10.1038/364550a0
3. Chen L, Rashid F, Shah A, Awan HM, Wu M, Liu A, Wang J, Zhu T, Luo Z, Shan G (2015)
The isolation of an RNA aptamer targeting to p53 protein with single amino acid mutation.
Proc Natl Acad Sci U S A 112(32):10002–10007. https://doi.org/10.1073/pnas.1502159112
4. Wu L, Zhu L, Huang M, Song J, Zhang H, Song Y, Wang W, Yang C (2019) Aptamer-based
microfluidics for isolation, release and analysis of circulating tumor cells. TrAC Trends Anal
Chem 117:69–77. https://doi.org/10.1016/j.trac.2019.05.003
5. Zhu G, Chen X (2018) Aptamer-based targeted therapy. Adv Drug Deliv Rev 134:65–78.
https://doi.org/10.1016/j.addr.2018.08.005
6. Pagratis NC, Bell C, Chang YF, Jennings S, Fitzwater T, Jellinek D, Dang C (1997) Potent 2 -
amino-, and 2 -fluoro-2 -deoxyribonucleotide RNA inhibitors of keratinocyte growth factor.
Nat Biotechnol 15(1):68–73. https://doi.org/10.1038/nbt0197-68
7. Shaw JP, Kent K, Bird J, Fishback J, Froehler B (1991) Modified deoxyoligonucleotides
stable to exonuclease degradation in serum. Nucl Acids Res 19(4):747–750. https://doi.org/
10.1093/nar/19.4.747
8. Monia BP, Johnston JF, Sasmor H, Cummins LL (1996) Nuclease resistance and antisense
activity of modified oligonucleotides targeted to Ha-ras. J Biol Chem 271(24):14533–14540.
https://doi.org/10.1074/jbc.271.24.14533
9. Liu Y, Kuan CT, Mi J, Zhang X, Clary BM, Bigner DD, Sullenger BA (2009) Aptamers
selected against the unglycosylated EGFRvIII ectodomain and delivered intracellularly reduce
membrane-bound EGFRvIII and induce apoptosis. Biol Chem 390(2):137–144. https://doi.
org/10.1515/bc.2009.022
10. Point of Care Diagnostics Market by Product (Glucose, Infectious Disease (Hepatitis
C, Influenza, Respiratory), Coagulation), Platform (Microfluidics, Immunoassays),
Mode (Prescription & OTC), End-User (Hospitals, Home Care) -Global Forecast
to 2024. https://www.marketsandmarkets.com/Market-Reports/point-of-care-diagnostic-mar
ket-106829185.html
11. Kropff J, Choudhary P, Neupane S, Barnard K, Bain SC, Kapitza C, Forst T, Link M, Dehennis
A, DeVries JH (2017) Accuracy and longevity of an implantable continuous glucose sensor in