Molecular selection, modification and development of therapeutic oligonucleotide aptamers

Yuanyuan Yu, Chao Liang, Quanxia Lv, Defang Li, Xuegong Xu, Baoqin Liu*, Aiping Lyu*, Ge Zhang*

*Corresponding author for this work

Research output: Contribution to journalJournal articlepeer-review

50 Citations (Scopus)
23 Downloads (Pure)


Monoclonal antibodies are the dominant agents used in inhibition of biological target molecules for disease therapeutics, but there are concerns of immunogenicity, production, cost and stability. Oligonucleotide aptamers have comparable affinity and specificity to targets with monoclonal antibodies whilst they have minimal immunogenicity, high production, low cost and high stability, thus are promising inhibitors to rival antibodies for disease therapy. In this review, we will compare the detailed advantages and disadvantages of antibodies and aptamers in therapeutic applications and summarize recent progress in aptamer selection and modification approaches. We will present therapeutic oligonucleotide aptamers in preclinical studies for skeletal diseases and further discuss oligonucleotide aptamers in different stages of clinical evaluation for various disease therapies including macular degeneration, cancer, inflammation and coagulation to highlight the bright commercial future and potential challenges of therapeutic oligonucleotide aptamers.

Original languageEnglish
Article number358
Number of pages19
JournalInternational Journal of Molecular Sciences
Issue number3
Publication statusPublished - 1 Mar 2016

Scopus Subject Areas

  • Catalysis
  • Molecular Biology
  • Spectroscopy
  • Computer Science Applications
  • Physical and Theoretical Chemistry
  • Organic Chemistry
  • Inorganic Chemistry

User-Defined Keywords

  • Clinical evaluation
  • Diseases therapy
  • Monoclonal antibodies
  • Oligonucleotide aptamers
  • Preclinical study


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