title: Modulation of the Coagulation Cascade Using Aptamers.
abstract: As a novel class of therapeutics, aptamers, or nucleic acid ligands, have garnered clinical interest because of the ease of isolating a highly specific aptamer against a wide range of targets, their chemical flexibility and synthesis, and their inherent ability to have their function reversed. The following review details the development and molecular mechanisms of aptamers targeting specific proteases in the coagulation cascade. The ability of these anticoagulant aptamers to bind to and inhibit exosite function rather than binding within the active site highlights the importance of exosites in blocking protein function. As both exosite inhibitors and reversible agents, the use of aptamers is a promising strategy for future therapeutics.
authors: From the Bloodworks Northwest Research Institute, Seattle, WA (R.S.W.); Department of Medicine, University of Washington, Seattle (R.S.W.); and Duke Translational Research Institute, Department of Surgery, Duke University Medical Center, Durham, NC (B.A.S.).
authors: Rebecca S
authors: RS
authors: Woodruff
authors: From the Bloodworks Northwest Research Institute, Seattle, WA (R.S.W.); Department of Medicine, University of Washington, Seattle (R.S.W.); and Duke Translational Research Institute, Department of Surgery, Duke University Medical Center, Durham, NC (B.A.S.). bruce.sullenger@duke.edu.
authors: Bruce A
authors: BA
authors: Sullenger
mesh_terms: D052157:Aptamers, Nucleotide / Q000494:pharmacology / Q000627:therapeutic use*; D001777:Blood Coagulation / Q000187:drug effects* / Q000235:genetics; D017321:Clinical Trials, Phase I as Topic; D017322:Clinical Trials, Phase II as Topic; D005260:Female; D006801:Humans; D008297:Male; D058990:Molecular Targeted Therapy / Q000379:methods*; D011516:Prothrombin / Q000187:drug effects / Q000378:metabolism; D012680:Sensitivity and Specificity; D012697:Serine Endopeptidases / Q000187:drug effects / Q000378:metabolism; D013917:Thrombin / Q000187:drug effects / Q000378:metabolism
chemical_list: D052157:Aptamers, Nucleotide; D011516:Prothrombin; D012697:Serine Endopeptidases; D013917:Thrombin
keywords: anticoagulation; aptamer; coagulation cascade; nucleic acids; serine endopeptidases