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      Aptamers as Therapeutics.

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          Abstract

          Aptamers are single-stranded nucleic acid molecules that bind to and inhibit proteins and are commonly produced by systematic evolution of ligands by exponential enrichment (SELEX). Aptamers undergo extensive pharmacological revision, which alters affinity, specificity, and therapeutic half-life, tailoring each drug for a specific clinical need. The first therapeutic aptamer was described 25 years ago. Thus far, one aptamer has been approved for clinical use, and numerous others are in preclinical or clinical development. This review presents a short history of aptamers and SELEX, describes their pharmacological development and optimization, and reviews potential treatment of diseases including visual disorders, thrombosis, and cancer.

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          Author and article information

          Journal
          Annu. Rev. Pharmacol. Toxicol.
          Annual review of pharmacology and toxicology
          Annual Reviews
          1545-4304
          0362-1642
          Jan 06 2017
          : 57
          Affiliations
          [1 ] Department of Neurological Surgery, The Ohio State University Wexner Medical Center, Columbus, Ohio 43210; email: shahid.nimjee@osumc.edu.
          [2 ] Department of Surgery, Duke University Medical Center, Durham, North Carolina 27705; email: rebekah.white@duke.edu.
          [3 ] Department of Medicine, University of Cincinnati Medical Center, Cincinnati, Ohio 45267; email: beckerrc@ucmail.uc.edu.
          [4 ] Duke Translational Research Institute, Duke University Medical Center, Durham, North Carolina 27705; email: bruce.sullenger@duke.edu.
          Article
          10.1146/annurev-pharmtox-010716-104558
          28061688

          pharmacology, therapeutics, SELEX, antidote, aptamer

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