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Review
. 2022 Jul 29;12(8):1056.
doi: 10.3390/biom12081056.

Aptamers as Theragnostic Tools in Prostate Cancer

Carlos David Cruz-Hernández  1 , Griselda Rodríguez-Martínez  1 , Sergio A Cortés-Ramírez  1 , Miguel Morales-Pacheco  1 , Marian Cruz-Burgos  1 , Alberto Losada-García  1 , Juan Pablo Reyes-Grajeda  2 , Imelda González-Ramírez  3 , Vanessa González-Covarrubias  4 , Ignacio Camacho-Arroyo  5 , Marco Cerbón  5 , Mauricio Rodríguez-Dorantes  1
Affiliations
Review

Aptamers as Theragnostic Tools in Prostate Cancer

Carlos David Cruz-Hernández et al. Biomolecules. .

Abstract

Despite of the capacity that several drugs have for specific inhibition of the androgen receptor (AR), in most cases, PCa progresses to an androgen-independent stage. In this context, the development of new targeted therapies for prostate cancer (PCa) has remained as a challenge. To overcome this issue, new tools, based on nucleic acids technology, have been developed. Aptamers are small oligonucleotides with a three-dimensional structure capable of interacting with practically any desired target, even large targets such as mammalian cells or viruses. Recently, aptamers have been studied for treatment and detection of many diseases including cancer. In PCa, numerous works have reported their use in the development of new approaches in diagnostics and treatment strategies. Aptamers have been joined with drugs or other specific molecules such as silencing RNAs (aptamer-siRNA chimeras) to specifically reduce the expression of oncogenes in PCa cells. Even though these studies have shown good results in the early stages, more research is still needed to demonstrate the clinical value of aptamers in PCa. The aim of this review was to compile the existing scientific literature regarding the use of aptamers in PCa in both diagnosis and treatment studies. Since Prostate-Specific Membrane Antigen (PSMA) aptamers are the most studied type of aptamers in this field, special emphasis was given to these aptamers.

Keywords: PCa diagnosis; PCa treatment; Prostate-Specific Antigen (PSA); Prostate-Specific Membrane Antigen (PSMA); aptamers; prostate cancer.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Schematic representation of unfolded, folded, and binding of aptamers to a target molecule. (A) Unfolded single strand aptamer. (B) Folding of the aptamer by base pairing and tertiary interactions. (C) Final structure of the aptamer capable of binding to a specific target molecule.
Figure 2
Figure 2
General scheme of the aptamer selection process and possible structural modifications. 1. The 5′ end PEGylation for resisting renal clearance. 2. Nucleobase modification for improving binding affinity and specificity. 3. Phosphodiester backbone modifications for resisting nuclease degradation. 4. Modifications on the sugar ring for resisting nuclease degradation. 5. The 3′ end-capping strategy resisting nuclease degradation. 6. The mirror image L-deoxyoligonucleotide resisting nuclease degradation. In the cell-SELEX process, green cells represent the non-desired cells used for the negative selection step and magenta cells represent the target cells required for the positive selection.
Figure 3
Figure 3
Aptamers in cancer research. (A) Yearly trend of published articles reporting the application of aptamers in cancer research. (B) Proportion of types of cancer in which aptamers are most frequently used for therapeutic or diagnostic purposes.
Figure 4
Figure 4
Aptamer publications in PCa research. (A) Yearly trend of published articles reporting the use of aptamers in PCa. (B) Proteins used as targets of the aptamers in PCa research. Blue bars represent the number of articles using aptamers directed against each protein in diagnosis, whereas yellow bars refer to articles using aptamers in PCa therapy. PCA3 = prostate-cancer-associated 3; Muc1 = mucin 1; EpCAM = epithelial cellular adhesion molecule; PAP = prostatic acid phosphatase; SIRT-6 = sirtuin 6; CD133 = prominin-1; ATP5B = ATP synthase F1 subunit beta; HRE = hormone response element; STAT5 = signal transducer and activator of transcription 5A.
Figure 5
Figure 5
Scheme depicting some applications of aptamers in the diagnosis and treatment of PCa. (A) Aptamers can be coupled to radioligands and siRNA to specifically deliver the siRNA in PSMA+ cells. The inclusion of the technetium radionuclide (99mTc) allows the use of this aptamer in either therapeutic or diagnostic purposes. (B) Aptamers may improve the diagnosis imaging by implementing the semiconductor and nanocrystals technology known as quantum dots. (C) Aptamers can be modified with thiol groups to give them greater stability. (D) Aptamers can be used as aptasensors on gold electrode surfaces to recognize molecular targets. (E) Conjugates with aptamers are anchored to nanoparticles for systemic delivery of drugs. (F) Aptamers are used in therapy as chimeras apt-siRNA, apt-saRNA, apt-shRNA, apt-drugs, or apt-liposome by directly targeting the tumor. (G) Aptamers can be modified with 2′ fluoropyrimidine to increase stability.
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Grants and funding

This research was funded by CONACYT (Grant number A1-S-26446).