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Technology evaluation: SELEX, Gilead Sciences Inc.

S Sun1

  • 1ChemRx, 9640 Town Center Drive, San Diego, CA 92121, USA. ssun@chemrx.com

Current Opinion in Molecular Therapeutics
|March 16, 2001
PubMed
Summary
This summary is machine-generated.

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Systematic evolution of ligands by exponential enrichment (SELEX) is a method to find oligonucleotide drug candidates. This aptamer technology has been applied to various targets, with one entering clinical trials for blindness.

Area of Science:

  • Biotechnology
  • Molecular Biology
  • Drug Discovery

Background:

  • Systematic evolution of ligands by exponential enrichment (SELEX) is a decade-old technology for identifying oligonucleotide ligands.
  • SELEX involves selecting and amplifying RNA or DNA sequences that bind to specific targets.
  • This method yields high-affinity oligonucleotide ligands, termed aptamers, for therapeutic applications.

Purpose of the Study:

  • To describe the SELEX technology and its applications.
  • To highlight the potential of aptamers as therapeutic agents.
  • To introduce NX-1838 as a leading aptamer candidate.

Main Methods:

  • SELEX utilizes a pool of randomized oligonucleotide sequences (RNA or ssDNA).
  • Iterative cycles of target binding, isolation, and amplification enrich for high-affinity sequences.

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  • Selected sequences are identified as aptamers with potential drug-like properties.

    • Main Results:

    • SELEX has been successfully applied to diverse targets, including HIV enzymes, growth factors, and inflammation-inducing enzymes.
    • Aptamers have demonstrated significant binding affinity and specificity.
    • NX-1838, an aptamer targeting angiogenesis, has advanced to Phase I clinical trials.

    Conclusions:

    • SELEX is a versatile and powerful technology for aptamer discovery and development.
    • Aptamers represent a promising class of therapeutics with broad applicability.
    • The progression of NX-1838 into clinical studies validates the therapeutic potential of aptamer technology.