From selection hits to clinical leads: progress in aptamer discovery

Keith E. Maier1, Matthew Levy1
1Department of Biochemistry, Albert Einstein College of Medicine, Bronx, New York, USA

Tóm tắt

Từ khóa


Tài liệu tham khảo

Tuerk, 1990, Systematic evolution of ligands by exponential enrichment: RNA ligands to bacteriophage T4 DNA polymerase, Science, 249, 505, 10.1126/science.2200121

Ellington, 1990, In vitro selection of RNA molecules that bind specific ligands, Nature, 346, 818, 10.1038/346818a0

Hall, 2009, 1

Yan, 2014, Cell internalization SELEX: in vitro selection for molecules that internalize into cells, Methods Mol Biol, 1103, 241, 10.1007/978-1-62703-730-3_18

Zhou, 2014, Cell-type-specific, aptamer-functionalized agents for targeted disease therapy, Mol Ther Nucleic Acids, 3, e169, 10.1038/mtna.2014.21

Mi, 2010, In vivo selection of tumor-targeting RNA motifs, Nat Chem Biol, 6, 22, 10.1038/nchembio.277

Darmostuk, 2015, Current approaches in SELEX: an update to aptamer selection technology, Biotechnol Adv, 33, 1141, 10.1016/j.biotechadv.2015.02.008

Keefe, 2010, Aptamers as therapeutics, Nat Rev Drug Discov, 9, 537, 10.1038/nrd3141

Ni, 2011, Nucleic acid aptamers: clinical applications and promising new horizons, Curr Med Chem, 18, 4206, 10.2174/092986711797189600

Sundaram, 2013, Therapeutic RNA aptamers in clinical trials, Eur J Pharm Sci, 48, 259, 10.1016/j.ejps.2012.10.014

Kong, 2013, Nucleic Acid aptamers: new methods for selection, stabilization, and application in biomedical science, Biomol Ther (Seoul), 21, 423, 10.4062/biomolther.2013.085

Ashrafuzzaman, 2014, Aptamers as both drugs and drug-carriers, Biomed Res Int, 2014, 697923, 10.1155/2014/697923

Gouveia, 2015, Good manufacturing practices for medicinal products for human use, J Pharm Bioallied Sci, 7, 87, 10.4103/0975-7406.154424

Wincott, 2001, Strategies for oligoribonucleotide synthesis according to the phosphoramidite method, Curr Protoc Nucleic Acid Chem, Chapter 3, Unit 3.5

Beaucage, 2001, Synthetic strategies and parameters involved in the synthesis of oligodeoxyribonucleotides according to the phosphoramidite method, Curr Protoc Nucleic Acid Chem, Chapter 3, Unit 3.3

Dass, 2002, Cellular uptake, distribution, and stability of 10-23 deoxyribozymes, Antisense Nucleic Acid Drug Dev, 12, 289, 10.1089/108729002761381276

Morrissey, 2005, Activity of stabilized short interfering RNA in a mouse model of hepatitis B virus replication, Hepatology, 41, 1349, 10.1002/hep.20702

Manoharan, 2011, Unique gene-silencing and structural properties of 2'-fluoro-modified siRNAs, Angew Chem Int Ed Engl, 50, 2284, 10.1002/anie.201006519

Cekaite, 2007, Gene expression analysis in blood cells in response to unmodified and 2'-modified siRNAs reveals TLR-dependent and independent effects, J Mol Biol, 365, 90, 10.1016/j.jmb.2006.09.034

Judge, 2006, Design of noninflammatory synthetic siRNA mediating potent gene silencing in vivo, Mol Ther, 13, 494, 10.1016/j.ymthe.2005.11.002

Cho, 2009, Small interfering RNA-induced TLR3 activation inhibits blood and lymphatic vessel growth, Proc Natl Acad Sci USA, 106, 7137, 10.1073/pnas.0812317106

Heil, 2004, Species-specific recognition of single-stranded RNA via toll-like receptor 7 and 8, Science, 303, 1526, 10.1126/science.1093620

Kumagai, 2008, TLR9 as a key receptor for the recognition of DNA, Adv Drug Deliv Rev, 60, 795, 10.1016/j.addr.2007.12.004

Padilla, 1999, Efficient synthesis of nucleic acids heavily modified with non-canonical ribose 2'-groups using a mutantT7 RNA polymerase (RNAP), Nucleic Acids Res, 27, 1561, 10.1093/nar/27.6.1561

Ruckman, 1998, 2'-Fluoropyrimidine RNA-based aptamers to the 165-amino acid form of vascular endothelial growth factor (VEGF165). Inhibition of receptor binding and VEGF-induced vascular permeability through interactions requiring the exon 7-encoded domain, J Biol Chem, 273, 20556, 10.1074/jbc.273.32.20556

Barciszewski, 2009, Locked nucleic acid aptamers, 535, 165

Schmidt, 2004, Application of locked nucleic acids to improve aptamer in vivo stability and targeting function, Nucleic Acids Res, 32, 5757, 10.1093/nar/gkh862

Green, 1995, Nuclease-resistant nucleic acid ligands to vascular permeability factor/vascular endothelial growth factor, Chem Biol, 2, 683, 10.1016/1074-5521(95)90032-2

Yang, 2004, Progress in thioaptamer development, Curr Drug Targets, 5, 705, 10.2174/1389450043345074

Healy, 2004, Pharmacokinetics and biodistribution of novel aptamer compositions, Pharm Res, 21, 2234, 10.1007/s11095-004-7676-4

Watson, 2000, Anti-L-selectin aptamers: binding characteristics, pharmacokinetic parameters, and activity against an intravascular target in vivo, Antisense Nucleic Acid Drug Dev, 10, 63, 10.1089/oli.1.2000.10.63

Soutschek, 2004, Therapeutic silencing of an endogenous gene by systemic administration of modified siRNAs, Nature, 432, 173, 10.1038/nature03121

Rusconi, 2004, Antidote-mediated control of an anticoagulant aptamer in vivo, Nat Biotechnol, 22, 1423, 10.1038/nbt1023

Willis, 1998, Liposome-anchored vascular endothelial growth factor aptamers, Bioconjug Chem, 9, 573, 10.1021/bc980002x

Gilbert, 2007, First-in-human evaluation of anti von Willebrand factor therapeutic aptamer ARC1779 in healthy volunteers, Circulation, 116, 2678, 10.1161/CIRCULATIONAHA.107.724864

Vater, 2013, Hematopoietic stem and progenitor cell mobilization in mice and humans by a first-in-class mirror-image oligonucleotide inhibitor of CXCL12, Clin Pharmacol Ther, 94, 150, 10.1038/clpt.2013.58

Van Eijk, 2013, Randomized double-blind placebo-controlled PK/PD study on the effects of a single intravenous dose of the anti-hepcidin Spiegelmer NOX-H94 on serum iron during experimental human endotoxemia, Critical Care, 17, P352, 10.1186/cc12290

Ng, 2006, Pegaptanib, a targeted anti-VEGF aptamer for ocular vascular disease, Nat Rev Drug Discov, 5, 123, 10.1038/nrd1955

Tucker, 1999, Detection and plasma pharmacokinetics of an anti-vascular endothelial growth factor oligonucleotide-aptamer (NX1838) in rhesus monkeys, J Chromatogr B Biomed Sci Appl, 732, 203, 10.1016/S0378-4347(99)00285-6

Drolet, 2000, Pharmacokinetics and safety of an anti-vascular endothelial growth factor aptamer (NX1838) following injection into the vitreous humor of rhesus monkeys, Pharm Res, 17, 1503, 10.1023/A:1007657109012

Patel, 2006, Population pharmacokinetics/pharmacodynamics (PK/PD) of pegaptanib sodium (Macugen®) in patients with age–related macular degeneration (AMD), Investigative Ophthalmol Visual Sci, 47, 2623

Ferrara, 2005, Bevacizumab (Avastin), a humanized anti-VEGF monoclonal antibody for cancer therapy, Biochem Biophys Res Commun, 333, 328, 10.1016/j.bbrc.2005.05.132

Lowe, 2007, Ranibizumab inhibits multiple forms of biologically active vascular endothelial growth factor in vitro and in vivo, Exp Eye Res, 85, 425, 10.1016/j.exer.2007.05.008

Semeraro, 2013, Aflibercept in wet AMD: specific role and optimal use, Drug Des Devel Ther, 7, 711, 10.2147/DDDT.S40215

Rusconi, 2002, RNA aptamers as reversible antagonists of coagulation factor IXa, Nature, 419, 90, 10.1038/nature00963

Brooks, 2012, Method for manufacturing PEGylated oligonucleotides, Patent Application # 20120277419

Vavalle, 2012, The REG1 anticoagulation system: a novel actively controlled factor IX inhibitor using RNA aptamer technology for treatment of acute coronary syndrome, Future Cardiol, 8, 371, 10.2217/fca.12.5

Nimjee, 2006, A novel antidote-controlled anticoagulant reduces thrombin generation and inflammation and improves cardiac function in cardiopulmonary bypass surgery, Mol Ther, 14, 408, 10.1016/j.ymthe.2006.04.006

Bel, 2016, Inhibition of factor IXa by the pegnivacogin system during cardiopulmonary bypass: a potential substitute for heparin. A study in baboons, Eur J Cardiothorac Surg, 49, 682, 10.1093/ejcts/ezv159

Dyke, 2006, First-in-human experience of an antidote-controlled anticoagulant using RNA aptamer technology: a phase 1a pharmacodynamic evaluation of a drug-antidote pair for the controlled regulation of factor IXa activity, Circulation, 114, 2490, 10.1161/CIRCULATIONAHA.106.668434

Chan, 2008, A randomized, repeat-dose, pharmacodynamic and safety study of an antidote-controlled factor IXa inhibitor, J Thromb Haemost, 6, 789, 10.1111/j.1538-7836.2008.02932.x

Chan, 2008, Phase 1b randomized study of antidote-controlled modulation of factor IXa activity in patients with stable coronary artery disease, Circulation, 117, 2865, 10.1161/CIRCULATIONAHA.107.745687

Vavalle, 2012, A phase 1 ascending dose study of a subcutaneously administered factor IXa inhibitor and its active control agent, J Thromb Haemost, 10, 1303, 10.1111/j.1538-7836.2012.04742.x

Lincoff, 2016, Effect of the REG1 anticoagulation system versus bivalirudin on outcomes after percutaneous coronary intervention (REGULATE-PCI): a randomised clinical trial, Lancet, 387, 349, 10.1016/S0140-6736(15)00515-2

Verheugt, 2016, An anticoagulant too good to be true for revascularisation, Lancet, 387, 314, 10.1016/S0140-6736(15)00727-8

Ganson, 2015, Pre-existing anti-polyethylene glycol antibody linked to first-exposure allergic reactions to pegnivacogin, a PEGylated RNA aptamer, J Allergy Clin Immunol

Povsic, 2013, A phase 2, randomized, partially blinded, active-controlled study assessing the efficacy and safety of variable anticoagulation reversal using the REG1 system in patients with acute coronary syndromes: results of the RADAR trial, Eur Heart J, 34, 2481, 10.1093/eurheartj/ehs232

Green, 1996, Inhibitory DNA ligands to platelet-derived growth factor B-chain, Biochemistry, 35, 14413, 10.1021/bi961544+

Floege, 1999, Novel approach to specific growth factor inhibition in vivo: antagonism of platelet-derived growth factor in glomerulonephritis by aptamers, Am J Pathol, 154, 169, 10.1016/S0002-9440(10)65263-7

Diener, 2009, Inhibition of von Willebrand factor-mediated platelet activation and thrombosis by the anti-von Willebrand factor A1-domain aptamer ARC1779, J Thromb Haemost, 7, 1155, 10.1111/j.1538-7836.2009.03459.x

Jilma-Stohlawetz, 2011, Inhibition of von Willebrand factor by ARC1779 in patients with acute thrombotic thrombocytopenic purpura, Thromb Haemost, 105, 545, 10.1160/TH10-08-0520

Markus, 2011, The von Willebrand inhibitor ARC1779 reduces cerebral embolization after carotid endarterectomy: a randomized trial, Stroke, 42, 2149, 10.1161/STROKEAHA.111.616649

Siller-Matula, 2012, ARC15105 is a potent antagonist of von Willebrand factor mediated platelet activation and adhesion, Arterioscler Thromb Vasc Biol, 32, 902, 10.1161/ATVBAHA.111.237529

Bates, 1999, Antiproliferative activity of G-rich oligonucleotides correlates with protein binding, J Biol Chem, 274, 26369, 10.1074/jbc.274.37.26369

Reyes-Reyes, 2010, A new paradigm for aptamer therapeutic AS1411 action: uptake by macropinocytosis and its stimulation by a nucleolin-dependent mechanism, Cancer Res, 70, 8617, 10.1158/0008-5472.CAN-10-0920

Soundararajan, 2008, The nucleolin targeting aptamer AS1411 destabilizes Bcl-2 messenger RNA in human breast cancer cells, Cancer Res, 68, 2358, 10.1158/0008-5472.CAN-07-5723

Laber, 2006, Extended phase I study of AS1411 in renal and non-small cell lung cancers, ASCO Annual Meeting Proceedings, 24, 13098

Rosenberg, 2014, A phase II trial of AS1411 (a novel nucleolin-targeted DNA aptamer) in metastatic renal cell carcinoma, Invest New Drugs, 32, 178, 10.1007/s10637-013-0045-6

Stuart, 2009, Randomized phase II trial of the nucleolin targeting aptamer AS1411 combined with high-dose cytarabine in relapsed/refractory acute myeloid leukemia (AML), ASCO Annual Meeting Proceedings, 27, 7019

Waters, 2011, Aptamer ARC19499 mediates a procoagulant hemostatic effect by inhibiting tissue factor pathway inhibitor, Blood, 117, 5514, 10.1182/blood-2010-10-311936

Dockal, 2013, Aptamers to tissue factor pathway inhibitor and their use as bleeding disorder therapeutics, Patent Application #WO2012109675A1

Schaub, 2011, Aptamers to tissue factor pathway inhibitor and their use as bleeding disorder therapeutics, Patent Application # 20110098345

Waters, 2013, Aptamer BAX 499 mediates inhibition of tissue factor pathway inhibitor via interaction with multiple domains of the protein, J Thromb Haemost, 11, 1137, 10.1111/jth.12201

Gissel, 2012, Effect of BAX499 aptamer on tissue factor pathway inhibitor function and thrombin generation in models of hemophilia, Thromb Res, 130, 948, 10.1016/j.thromres.2012.08.299

Gorczyca, 2012, Inhibition of tissue factor pathway inhibitor by the aptamer BAX499 improves clotting of hemophilic blood and plasma, J Thromb Haemost, 10, 1581, 10.1111/j.1538-7836.2012.04790.x

Dockal, 2012, Biological explanation of clinically observed elevation of TFPI plasma levels after treatment with TFPI-antagonistic aptamer BAX 499, Blood, 120, 1104, 10.1182/blood.V120.21.1104.1104

Dockal, 2012, Effect of increased tissue factor pathway inhibitor (TFPI) levels on factor Xa inhibition and global hemostasis in the presence of TFPI-antagonistic aptamer BAX 499, Blood, 120, 2207, 10.1182/blood.V120.21.2207.2207

Klussmann, 1996, Mirror-image RNA that binds D-adenosine, Nat Biotechnol, 14, 1112, 10.1038/nbt0996-1112

Vater, 2015, Turning mirror-image oligonucleotides into drugs: the evolution of Spiegelmer(®) therapeutics, Drug Discov Today, 20, 147, 10.1016/j.drudis.2014.09.004

Burmeister, 2005, Direct in vitro selection of a 2'-O-methyl aptamer to VEGF, Chem Biol, 12, 25, 10.1016/j.chembiol.2004.10.017

Diener, 2012, Materials and methods for the generation of fully 2′-modified nucleic acid transcripts, Patent Application # 8105813

Chelliserrykattil, 2004, Evolution of a T7 RNA polymerase variant that transcribes 2'-O-methyl RNA, Nat Biotechnol, 22, 1155, 10.1038/nbt1001

Padilla, 2002, A Y639F/H784A T7 RNA polymerase double mutant displays superior properties for synthesizing RNAs with non-canonical NTPs, Nucleic Acids Res, 30, e138, 10.1093/nar/gnf138

Meyer, 2015, Transcription yield of fully 2'-modified RNA can be increased by the addition of thermostabilizing mutations to T7 RNA polymerase mutants, Nucleic Acids Res, 43, 7480, 10.1093/nar/gkv734

Friedman, 2015, Highly stable aptamers selected from a 2'-fully modified fGmH RNA library for targeting biomaterials, Biomaterials, 36, 110, 10.1016/j.biomaterials.2014.08.046

Pinheiro, 2012, Synthetic genetic polymers capable of heredity and evolution, Science, 336, 341, 10.1126/science.1217622

Vaught, 2010, Expanding the chemistry of DNA for in vitro selection, J Am Chem Soc, 132, 4141, 10.1021/ja908035g

Gold, 2010, Aptamer-based multiplexed proteomic technology for biomarker discovery, PLoS One, 5, e15004, 10.1371/journal.pone.0015004

Davies, 2012, Unique motifs and hydrophobic interactions shape the binding of modified DNA ligands to protein targets, Proc Natl Acad Sci USA, 109, 19971, 10.1073/pnas.1213933109

Gupta, 2014, Chemically modified DNA aptamers bind interleukin-6 with high affinity and inhibit signaling by blocking its interaction with interleukin-6 receptor, J Biol Chem, 289, 8706, 10.1074/jbc.M113.532580

Rohloff, 2014, Nucleic acid ligands with protein-like side chains: modified aptamers and their use as diagnostic and therapeutic agents, Mol Ther Nucleic Acids, 3, e201, 10.1038/mtna.2014.49

Gelinas, 2014, Crystal structure of interleukin-6 in complex with a modified nucleic acid ligand, J Biol Chem, 289, 8720, 10.1074/jbc.M113.532697

Hirota, 2016, Chemically modified interleukin-6 aptamer inhibits development of collagen-induced arthritis in cynomolgus monkeys, Nucleic Acid Ther, 26, 10, 10.1089/nat.2015.0567

Diener, 2006, Stabilized aptamers to PSMA and their use as prostate cancer therapeutics, Patent Application # Wo2006096754

Lupold, 2002, Identification and characterization of nuclease-stabilized RNA molecules that bind human prostate cancer cells via the prostate-specific membrane antigen, Cancer Res, 62, 4029