Aptamer-Drug Conjugation (ApDC)

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As a leading service provider focused on drug development, BOC Sciences has been supporting customers at the forefront of drug conjugation. Building drug conjugates facilitates the selective delivery of toxic therapeutic cargos to diseased cells. Among them, nucleic acid aptamers are one of the scaffolds that have received the most attention. We provide aptamer-drug conjugation services to meet your unique project needs. Our scientific team will work with you to create a scope of work to complete the project on time and within specifications.

Find out more with Drug Conjugation Services.

Introduction

Nucleic acid aptamers are short, single-stranded oligonucleotides (DNA or RNA molecules) with a stable 3D structure, also known as “chemical antibodies”, which could be used as potential drug-delivery vehicles and are able to bind to a molecular target through secondary or tertiary conformation. The targets of aptamers range from small molecules and proteins to intact cells.

Advantages of aptamers served as targeting ligands:

  • Small size
  • High chemical stability
  • Facile chemical modification
  • Low immunogenicity
  • Rapid tissue penetration
Aptamer NameTargetsApplicationAptamer NameTargetsApplication
CD4RORγtGene therapyaptPD-L1PD-L1Mammary cancer, immunotherapy
sgc8PTK7Gene therapyAptCTLA-4CTLA-4Immunotherapy
Zy1SMMC-7721Liver cancerMUC-1MCF-7Mammary cancer
SL₂-BHep G2Liver cancerCL4EGFRMammary cancer
RNV-L7LDL-RLiver cancerS30CD33Leukemia
G12msiGPC3Liver cancerGL44U-87 MGRadiotherapy
CD28Apt7B16Skin cancerAS1411NucleolinMammary cancer, skin cancer, photothermal therapy
P19PANC-1Pancreatic cancerapt4-1BB4-1BBImmunotherapy
TR14hTfR2Pancreatic cancerMP7PD-1Immunotherapy
AP-1CD133Anaplastic thyroid carcinomaTIM3AptTIM-3Immunotherapy
AptABCG2ABCG2Mammary cancerApt1, Apt2, Apt4, Apt5LAG3Immunotherapy
APTA12NucleolinMammary cancerRCA IICD40Immunotherapy

Table 1. Examples of aptamers selected with potential for targeted therapy (Liu, 2022)

Aptamer-drug conjugates (ApDCs) have been developed for targeted therapy. An ApDC typically consists of three molecular parts: a ligand (aptamer), a linker, and a warhead (drug). In these conjugates, aptamers specifically recognize diseases-associated biomarkers to deliver conjugated drugs to target cells or/and tissues. The chemical stability and simplicity of chemical modification of aptamers allow these to be easily combined with many warheads, such as chemotherapeutics, nucleic acids, proteins, photosensitizers, etc.

Aptamer binding to targets Fig 1. Aptamer binding to targets (Liu, 2022)

Our Services

  • Exponential enrichment (SELEX) method for screening aptamers.
  • Chemical modification or insertion of drug molecules into DNA structures for aptamer drug conjugation.
  • Adjustment for payload/drug load (proportion of drug part carried by a single ApDC unit).
  • Increasement of the number of aptamer units on a single ApDC structure for improving aptamer targeting efficiency.
Aptamer-Drug ConjugatesAptamersTherapeutic Cargoes
Aptamer-chemotherapeutic conjugatessgc8, AS1411, A10, APTChemotherapeutics
Aptamer-nucleic acid conjugatesA10, CH6, Anti-gp120siRNA
Aptamer-protein/peptide conjugatesGS24Enzymes
Aptamer-photosensitizer conjugatesAIR-3A, sgc8, TD05, AS1411Photosensitizers
Aptamer-photothermal agent conjugatessgc8photothermal agents

Table 2. Examples of aptamer-drug conjugates

Applications of ApDC

ApDCs can be used in the treatment of various diseases. Combined with aptamer, the diagnosis and treatment of diseases can effectively avoid the problems of low diagnostic sensitivity in vivo, large side effects of drugs, difficult tumor monitoring and so on. With the continuous development of aptamers, ApDC with different target sites are more and more widely used.

ApDCs are used for targeting drug delivery in chemotherapy, gene therapy, immunotherapy, photodynamic therapy and photothermal therapy for the treatment of various cancers such as liver, ovarian, skin, prostate, breast, pancreatic and anaplastic thyroid cancers, as well as acquired immunodeficiency syndrome. In addition, aptamer conjugates can be extended to other types of metal-organic framework (MOF) nanomaterials, and conjugates with targeted therapeutic and imaging capabilities can be developed for cancer cell detection and imaging.

Our Advantages

  • Different ApDC structures and batch development experience
  • Various conjugation methods through chemical modification or molecular engineering
  • A wide range of characteristic analysis
  • People and suites that specialize in ApDC development, manufacturing, and testing
  • Data analysis, detailed report with results and discussion
  • Cost-effective and high-quality products

References

  1. Zhu, G., Niu, G., and Chen, X., Aptamer–Drug Conjugates, Bioconjug Chem., 2015, 26(11): 2186-2197.
  2. Liu, P., et al., Aptamer-drug conjugates: New probes for imaging and targeted therapy, Biosens. Bioelectron., 2022, 10, 100126.

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