164
G. Yang and Y. Huang
However, further challenges must be addressed to promote the development of
aptamers for targeted therapy, including better tumor permeability, greater blood
stability, reversibility, lower cost, and so on. In addition, due to the development of
aptamer screening technology, a more diverse set of aptamers are obtained and the
targets are extended widely. However, there were not enough aptamers with stable
and excellent performance can be used. Rational aptamer screening, design, synthesis
and modification techniques need to be further developed to allow aptamers to be
widely utilized as targeted therapeutic agents.
Acknowledgements This work was supported by the National Natural Science Foundation of
China (31871003), the Natural Science Foundation of Guangdong Province (2019A1515010776),
the Beijing Institute of Technology Research Fund Program for Young Scholars and the Fundamental
Research Funds for the Central Universities (3052018065), the Hunan Provincial Natural Science
Foundation of China (2018JJ1019), and the Hu-Xiang Young Talent Program (2018RS3094). The
authors thank Biological & Medical Engineering Core Facilities (Beijing Institute of Technology)
for providing advanced working conditions. Also thanks to Bo Hu and Chunhui Li (Beijing Institute
of Technology) for their manuscript proofreading.
Conflict of Interest The authors declare no competing financial interest.
References
1. Drolet DW, Green LS, Gold L, Janjic N (2016) Fit for the eye: aptamers in ocular disorders.
Nucleic Acid Ther 26(3):127–146
2. Jaffe GJ, Ciulla TA, Ciardella AP, Devin F, Dugel PU, Eandi CM, Masonson H, Mones J,
Pearlman JA, Quaranta-El Maftouhi M, Ricci F, Westby K, Patel SC (2017) Dual antagonism
of PDGF and VEGF in neovascular age-related macular degeneration: a phase IIb, multicenter.
Randomized Controlled Trial Ophthalmol 124(2):224–234
3. Mousa SA, Mousa SS (2010) Current status of vascular endothelial growth factor inhibition
in age-related macular degeneration. BioDrugs 24(3):183–194
4. Barakat MR, Kaiser PK (2009) VEGF inhibitors for the treatment of neovascular age-related
macular degeneration. Expert Opin Investig Drugs 18(5):637–646
5. Chakravarthy U, Adamis AP, Cunningham ET, Jr., Goldbaum M, Guyer DR, Katz B, Patel
M (2006) Neovascularization (V.I.S.I.O.N.) clinical trial group, year 2 efficacy results of
2 randomized controlled clinical trials of pegaptanib for neovascular age-related macular
degeneration. Ophthalmology 113 (9):1508 (e01–e25)
6. Satarug S, Kikuchi M, Wisedpanichkij R, Li B, Takeda K, Na-Bangchang K, Moore MR,
Hirayama K, Shibahara S (2008) Prevention of cadmium accumulation in retinal pigment
epithelium with manganese and zinc. Exp Eye Res 87(6):587–593
7. Siddiqui MA, Keating GM (2005) Pegaptanib: in exudative age-related macular degeneration.
Drugs 65(11):1571–1577. (discussion 1578–1579)
8. Jellinek D, Lynott CK, Rifkin DB, Janjic N (1993) High-affinity RNA ligands to basic fibroblast growth factor inhibit receptor binding. Proc Natl Acad Sci U S A 90(23):11227–11231
9. Jellinek D, Green LS, Bell C, Lynott CK, Gill N, Vargeese C, Kirschenheuter G, McGee DP,
Abesinghe P, Pieken WA et al (1995) Potent 2’-amino-2’-deoxypyrimidine RNA inhibitors
of basic fibroblast growth factor. Biochemistry 34(36):11363–11372
10. Green LS, Jellinek D, Bell C, Beebe LA, Feistner BD, Gill SC, Jucker FM, Janjic N (1995)
Nuclease-resistant nucleic acid ligands to vascular permeability factor/vascular endothelial
growth factor. Chem Biol 2(10):683–695
G. Yang and Y. Huang
However, further challenges must be addressed to promote the development of
aptamers for targeted therapy, including better tumor permeability, greater blood
stability, reversibility, lower cost, and so on. In addition, due to the development of
aptamer screening technology, a more diverse set of aptamers are obtained and the
targets are extended widely. However, there were not enough aptamers with stable
and excellent performance can be used. Rational aptamer screening, design, synthesis
and modification techniques need to be further developed to allow aptamers to be
widely utilized as targeted therapeutic agents.
Acknowledgements This work was supported by the National Natural Science Foundation of
China (31871003), the Natural Science Foundation of Guangdong Province (2019A1515010776),
the Beijing Institute of Technology Research Fund Program for Young Scholars and the Fundamental
Research Funds for the Central Universities (3052018065), the Hunan Provincial Natural Science
Foundation of China (2018JJ1019), and the Hu-Xiang Young Talent Program (2018RS3094). The
authors thank Biological & Medical Engineering Core Facilities (Beijing Institute of Technology)
for providing advanced working conditions. Also thanks to Bo Hu and Chunhui Li (Beijing Institute
of Technology) for their manuscript proofreading.
Conflict of Interest The authors declare no competing financial interest.
References
1. Drolet DW, Green LS, Gold L, Janjic N (2016) Fit for the eye: aptamers in ocular disorders.
Nucleic Acid Ther 26(3):127–146
2. Jaffe GJ, Ciulla TA, Ciardella AP, Devin F, Dugel PU, Eandi CM, Masonson H, Mones J,
Pearlman JA, Quaranta-El Maftouhi M, Ricci F, Westby K, Patel SC (2017) Dual antagonism
of PDGF and VEGF in neovascular age-related macular degeneration: a phase IIb, multicenter.
Randomized Controlled Trial Ophthalmol 124(2):224–234
3. Mousa SA, Mousa SS (2010) Current status of vascular endothelial growth factor inhibition
in age-related macular degeneration. BioDrugs 24(3):183–194
4. Barakat MR, Kaiser PK (2009) VEGF inhibitors for the treatment of neovascular age-related
macular degeneration. Expert Opin Investig Drugs 18(5):637–646
5. Chakravarthy U, Adamis AP, Cunningham ET, Jr., Goldbaum M, Guyer DR, Katz B, Patel
M (2006) Neovascularization (V.I.S.I.O.N.) clinical trial group, year 2 efficacy results of
2 randomized controlled clinical trials of pegaptanib for neovascular age-related macular
degeneration. Ophthalmology 113 (9):1508 (e01–e25)
6. Satarug S, Kikuchi M, Wisedpanichkij R, Li B, Takeda K, Na-Bangchang K, Moore MR,
Hirayama K, Shibahara S (2008) Prevention of cadmium accumulation in retinal pigment
epithelium with manganese and zinc. Exp Eye Res 87(6):587–593
7. Siddiqui MA, Keating GM (2005) Pegaptanib: in exudative age-related macular degeneration.
Drugs 65(11):1571–1577. (discussion 1578–1579)
8. Jellinek D, Lynott CK, Rifkin DB, Janjic N (1993) High-affinity RNA ligands to basic fibroblast growth factor inhibit receptor binding. Proc Natl Acad Sci U S A 90(23):11227–11231
9. Jellinek D, Green LS, Bell C, Lynott CK, Gill N, Vargeese C, Kirschenheuter G, McGee DP,
Abesinghe P, Pieken WA et al (1995) Potent 2’-amino-2’-deoxypyrimidine RNA inhibitors
of basic fibroblast growth factor. Biochemistry 34(36):11363–11372
10. Green LS, Jellinek D, Bell C, Beebe LA, Feistner BD, Gill SC, Jucker FM, Janjic N (1995)
Nuclease-resistant nucleic acid ligands to vascular permeability factor/vascular endothelial
growth factor. Chem Biol 2(10):683–695
