Antisense Oligonucleotides as Therapeutic Agents—Is the Bullet Really Magical?

Sequence-Selective Recognition of DNA by Strand Displacement with a Thymine-Substituted Polyamide

1991 • 3,211 citations

Deoxynucleoside phosphoramidites—A new class of key intermediates for deoxypolynucleotide synthesis

1981 • 1,881 citations

Identification of the Envelope V3 Loop as the Primary Determinant of Cell Tropism in HIV-1

1991 • 871 citations

NUCLEOSIDE PHOSPHOROTHIOATES

1985 • 830 citations

Specific regulation of gene expression by antisense, sense and antigene nucleic acids

1990 • 769 citations

Antisense c-myb oligonucleotides inhibit intimal arterial smooth muscle cell accumulation in vivo

1992 • 749 citations

Characterization of oligonucleotide transport into living cells.

1989 • 739 citations

Site-Specific Oligonucleotide Binding Represses Transcription of the Human c- myc Gene in Vitro

1988 • 707 citations

Role for c-myc in Activation-Induced Apoptotic Cell Death in T Cell Hybridomas

1992 • 705 citations

A second post-transcriptional trans-activator gene required for HTLV-III replication

1986 • 639 citations

Cationic lipids enhance cellular uptake and activity of phosphorothioate antisense oligonucleotides.

1992 • 609 citations

Physicochemical properties of phospborothioate oligodeoxynucleotides

1988 • 567 citations

Pharmacokinetics, biodistribution, and stability of oligodeoxynucleotide phosphorothioates in mice.

1991 • 551 citations

Phosphorothioate analogs of oligodeoxynucleotides: inhibitors of replication and cytopathic effects of human immunodeficiency virus.

1987 • 530 citations

Mechanism of oligonucleotide uptake by cells: involvement of specific receptors?

1989 • 510 citations

Unique palindromic sequences in synthetic oligonucleotides are required to induce IFN [correction of INF] and augment IFN-mediated [correction of INF] natural killer activity.

1992 • 480 citations

Antisense oligonucleotides inhibit intercellular adhesion molecule 1 expression by two distinct mechanisms.

1991 • 468 citations

Role of RNase H in hybrid-arrested translation by antisense oligonucleotides.

1988 • 445 citations

Therapeutic Applications of Oligonucleotides

1992 • 438 citations

Oligodeoxynucleotides as inhibitors of gene expression: a review.

1988 • 419 citations

Synthesis of DNA via deoxynudeoside H-phosphonate Intermediates

1986 • 343 citations

Evidence that a triplex-forming oligodeoxyribonucleotide binds to the c-myc promoter in HeLa cells, thereby reducing c-myc mRNA levels.

1991 • 299 citations

3H-1,2-Benzodithiole-3-one 1,1-dioxide as an improved sulfurizing reagent in the solid-phase synthesis of oligodeoxyribonucleoside phosphorothioates

1990 • 296 citations

Cholesteryl-conjugated oligonucleotides: synthesis, properties, and activity as inhibitors of replication of human immunodeficiency virus in cell culture.

1989 • 296 citations

Down-regulation of a serine protease, myeloblastin, causes growth arrest and differentiation of promyelocytic leukemia cells

1989 • 293 citations

Oligodeoxynucleoside phosphoramidates and phosphorothioates as inhibitors of human immunodeficiency virus.

1988 • 289 citations

Substrate Specificity and Kinetics of Degradation of Antisense Oligonucleotides by a 3′ Exonuclease in Plasma

1991 • 285 citations

Automated solid-phase synthesis, separation, and stereochemistry of phosphorothioate analogs of oligodeoxyribonucleotides

1984 • 272 citations

Proliferation of human malignant melanomas is inhibited by antisense oligodeoxynucleotides targeted against basic fibroblast growth factor.

1989 • 270 citations

Regulation of viral expression of human immunodeficiency virus in vitro by an antisense phosphorothioate oligodeoxynucleotide against rev (art/trs) in chronically infected cells.

1989 • 264 citations

Epithelial-mesenchymal transformation of embryonic cardiac endothelial cells is inhibited by a modified antisense oligodeoxynucleotide to transforming growth factor beta 3.

1991 • 263 citations

Ablation of transplanted HTLV-I tax-transformed tumors in mice by antisense inhibition of NF-kappa B

1993 • 249 citations

Specificity of antisense oligonucleotides in vivo.

1992 • 248 citations

Release of early human hematopoietic progenitors from quiescence by antisense transforming growth factor beta 1 or Rb oligonucleotides.

1991 • 243 citations

DNA binding to human leukocytes. Evidence for a receptor-mediated association, internalization, and degradation of DNA.

1985 • 240 citations

Comparative inhibition of rabbit globin mRNA translation by modified antisense oligodeoxynucleotides

1989 • 238 citations

Oligodeoxynucleotides as Antisense Inhibitors of Gene Expression

1992 • 234 citations

Phosphorothioate oligonucleotides are inhibitors of human DNA polymerases and RNase H: implications for antisense technology.

1992 • 231 citations

Selective elimination of mRNAs in vivo: complementary oligodeoxynucleotides promote RNA degradation by an RNase H-like activity.

1987 • 225 citations

In vivo treatment of human leukemia in a scid mouse model with c-myb antisense oligodeoxynucleotides.

1992 • 223 citations

Implication of RNA structure on antisense oligonucleotide hybridization kinetics

1992 • 223 citations

cdc2 Gene Expression at the G ₁ to S Transition in Human T Lymphocytes

1990 • 220 citations

Inhibition of human immunodeficiency virus in early infected and chronically infected cells by antisense oligodeoxynucleotides and their phosphorothioate analogues.

1989 • 207 citations

Ablation of Transplanted HTLV-I Tax-Transformed Tumors in Mice by Antisense Inhibition of NF-κB

1992 • 207 citations

Short modified antisense oligonucleotides directed against Ha-ras point mutation induce selective cleavage of the mRNA and inhibit T24 cells proliferation.

1991 • 206 citations

Modification of antisense phosphodiester oligodeoxynucleotides by a 5' cholesteryl moiety increases cellular association and improves efficacy.

1993 • 203 citations

Pentosan polysulfate, a sulfated oligosaccharide, is a potent and selective anti-HIV agent in vitro

1988 • 194 citations

Stepwise mechanism of HIV reverse transcriptase: primer function of phosphorothioate oligodeoxynucleotide

1989 • 190 citations

The effect of tau antisense oligonucleotides on neurite formation of cultured cerebellar macroneurons

1991 • 189 citations

Dependence of Kidney Morphogenesis on the Expression of Nerve Growth Factor Receptor

1991 • 184 citations

Mechansism of cellular uptake of modified oligodeoxynucleotides containing methylphosphonate linkages

1991 • 174 citations

Dynamics of the internalization of phosphodiester oligodeoxynucleotides in HL60 cells

1993 • 172 citations

A triple helix-forming oligonucleotide-intercalator conjugate acts as a transcriptional repressor via inhibition of NF kappa B binding to interleukin-2 receptor alpha-regulatory sequence.

1992 • 169 citations

Use of DNA sequence and mutant analyses and antisense oligodeoxynucleotides to examine the molecular basis of nonmuscle myosin light chain kinase autoinhibition, calmodulin recognition, and activity.

1990 • 167 citations

Functional Contribution of Neuronal AChR Subunits Revealed by Antisense Oligonucleotides

1991 • 164 citations

Suppression of basic fibroblast growth factor expression by antisense oligodeoxynucleotides inhibits the growth of transformed human astrocytes.

1991 • 162 citations

Biological activity of oligonucleotide-poly(L-lysine) conjugates: mechanism of cell uptake

1990 • 160 citations

Synthesis of alkylating oligonucleotide derivatives containing cholesterol or phenazinium residues at their 3′‐terminus and their interaction with DNA within mammalian cells

1989 • 147 citations

Association of antisense oligonucleotides with lipoproteins prolongs the plasma half-life and modifies the tissue distribution

1991 • 146 citations

Internucleotide phosphite sulfurization with tetraethylthiuram disulfide. Phosphorothioate oligonucleotide synthesis via phosphoramidite chemistry

1991 • 145 citations

Inhibition of leukemia cell proliferation by receptor-mediated uptake of c-myb antisense oligodeoxynucleotides.

1992 • 145 citations

Novel route to oligo(deoxyribonucleoside phosphorothioates). Stereocontrolled synthesis of P-chiral oligo(deoxyribonucleoside phosphorothioates)

1991 • 142 citations

Stereochemical course of the reaction catalyzed by 5'-nucleotide phosphodiesterase from snake venom

1979 • 141 citations

Effects of Sequence of Thioated Oligonucleotides on Cultured Human Mammary Epithelial Cells

1993 • 137 citations

Cellular Uptake and Subcellular Distribution of Phosphorothioate Oligonucleotides into Cultured Cells

1992 • 137 citations

Inhibition of HIV-LTR gene expression by oligonucleotides targeted to the TAR element

1991 • 133 citations

Human immunodeficiency virus induces phosphorylation of its cell surface receptor

1988 • 133 citations

Dextran sulfate and heparin interact with CD4 molecules to inhibit the binding of coat protein (gp120) of HIV.

1989 • 128 citations

Antimessenger oligodeoxyribonucleotides: an alternative to antisense RNA for artificial regulation of gene expression — a review

1988 • 123 citations

Phosphorothioate and normal oligodeoxyribonucleotides with 5′-linked acridine: characterization and preliminary kinetics of cellular uptake

1988 • 123 citations

In vitro toxicology and pharmacokinetics of antisense oligonucleotides.

1991 • 120 citations

Specific interaction of aurintricarboxylic acid with the human immunodeficiency virus/CD4 cell receptor.

1989 • 118 citations

Oligonucleoside Methylphosphonates as Antisense Reagents

1991 • 111 citations

Phosphorothioate oligodeoxynucleotides—anti-sense inhibitors of gene expression?

1991 • 108 citations

Prospects for antisense nucleic acid therapy of cancer and AIDS

1991 • 108 citations

Cloning of a phospholipase A2-activating protein.

1991 • 107 citations

Long-term treatment of human immunodeficiency virus-infected cells with antisense oligonucleotide phosphorothioates.

1993 • 104 citations

Antisense inhibition of ras p21 expression that is sensitive to a point mutation

1991 • 104 citations

The growth-stimulatory effect of simian virus 40 T antigen requires the interaction of insulinlike growth factor 1 with its receptor.

1992 • 99 citations

B-myb antisense oligonucleotides inhibit proliferation of human hematopoietic cell lines

1992 • 97 citations

EGF antisense oligodeoxynucleotides block murine odontogenesis in vitro

1991 • 96 citations

In vivo studies with phosphorothioate oligonucleotides: pharmacokinetics prologue.

1991 • 96 citations

Uptake of Oligodeoxyribonucleotides by Lymphoid Cells Is Heterogeneous and Inducible

1991 • 95 citations

Highly specific inhibition of IGF-I-stimulated differentiation by an antisense oligodeoxyribonucleotide to myogenin mRNA. No effects on other actions of IGF-T.

1990 • 92 citations

Cellular pharmacology of phosphorothioate homooligodeoxynucleotides in human cells.

1993 • 90 citations

B-myb antisense oligonucleotides inhibit proliferation of human hematopoietic cell lines

1992 • 89 citations

Differential effects of c-myb and c-fes antisense oligodeoxynucleotides on granulocytic differentiation of human myeloid leukemia HL60 cells.

1990 • 89 citations

Walking along human c-myc mRNA with antisense oligodeoxynucleotides: maximum efficacy at the 5' cap region.

1991 • 89 citations

Antisense RNA to the putative tumor-suppressor gene DCC transforms Rat-1 fibroblasts.

1992 • 88 citations

Inhibition of herpes simplex virus type 2 growth by phosphorothioate oligodeoxynucleotides

1990 • 87 citations

Effect of Phosphorothioate Homo-oligodeoxy nucleotides on Herpes Simplex Virus Type 2-induced DNA Polymerase

1989 • 85 citations

Cloning and antisense oligodeoxynucleotide inhibition of a human homolog of cdc2 required in hematopoiesis.

1992 • 84 citations

Phosphorothioate oligodeoxycytidine interferes with binding of HIV-1 gp120 to CD4.

1991 • 83 citations

An Antisense Oligodeoxynucleotide to Growth Hormone Messenger Ribonucleic Acid Inhibits Lymphocyte Proliferation*

1991 • 83 citations

Synthesis of d(GC) and d(CG) octamers containing alternating phosphorothioate linkages: effect of the phosphorothioate group on the B-Z transition

1985 • 83 citations

Mode of action of 5'-linked cholesteryl phosphorothioate oligodeoxynucleotides in inhibiting syncytia formation and infection by HIV-1 and HIV-2 in vitro

1991 • 82 citations

Phosphorothioate Oligodeoxynucleotides Bind to the Third Variable Loop Domain (v3) of Human Immunodeficiency Virus Type 1 gp120

1993 • 82 citations

In vitro selection of fast-hybridizing and effective antisense RNAs directed against the human immunodeficiency virus type 1

1993 • 80 citations

Phosphorothioate-modified oligodeoxyribonucleotides. III. NMR and UV spectroscoptc studies of theR_p-R_p,S_p-S_p, andR_p-S_pduplexes, [d(GG_sAATTCC)]₂, derived from diastereomericO-ethyl phosphorothioates

1986 • 80 citations

Cell growth stimulation by EGF: Inhibition through antisense-oligodeoxynucleotides demonstrates important role of casein kinase II

1991 • 80 citations

Antisense oligonucleotides from the stage-specific myeloid zinc finger gene MZF-1 inhibit granulopoiesis in vitro.

1991 • 79 citations

Inhibition of influenza virus replication by phosphorothioate oligodeoxynucleotides.

1990 • 78 citations

Phosphoroselenoate oligodeoxynucleotides: synthesis, physico-chemical characterization, anti-sense inhibitory properties and anti-HIV activity

1989 • 73 citations

A new approach to chemotherapy based on molecular biology and nucleic acid chemistry: Matagen (masking tape for gene expression).

1987 • 68 citations

Mechanisms of inhibition of herpes simplex virus type 2 growth by 28-mer phosphorothioate oligodeoxycytidine

1990 • 67 citations

The inhibition of neunte outgrowth in PC12 cells by tubulin antisense oligodeoxyribonucleotides

1988 • 63 citations

Phosphorothioate oligonucleotides: chemistry, purification, analysis, scale-up and future directions.

1991 • 62 citations

Modulation of multidrug resistance by verapamil or mdr1 anti‐sense oligodeoxynucleotide does not change the high susceptibility to lymphokine‐activated killers in mdr‐resistant human carcinoma (LoVo) line

1990 • 62 citations

Synthetic repeating sequence DNAs containing plsosphorothioates: nuclease sensitivity and triplex formation

1989 • 61 citations

Human T-cell leukemia virus type I tax transformation is associated with increased uptake of oligodeoxynucleotides in vitro and in vivo.

1992 • 59 citations

Stereochemical course of DNA hydrolysis by nuclease S1.

1983 • 57 citations

A comparison of gag, pol and rev antisense oligodeoxynucleotides as inhibitors of HIV-1

1992 • 56 citations

Oligodeoxyribonucleotide Phosphorothioate Fluxes and Localization in Hematopoietic Cells

1992 • 55 citations

Target dependence of antisense oligodeoxynucleotide inhibition of c-Ha-ras p21 expression and focus formation in T24-transformed NIH3T3 cells.

1990 • 55 citations

Growth factor-dependent inhibition of normal hematopoiesis by N-ras antisense oligodeoxynucleotides.

1992 • 53 citations

Down-regulation of c-MYC antigen expression in lymphocytes of Emu-c-myc transgenic mice treated with anti-c-myc DNA methylphosphonates.

1992 • 52 citations

An autocrine role for erythropoietin in mouse hematopoietic cell differentiation [published erratum appears in Blood 1992 Jun 15;79(12):3397]

1991 • 50 citations

Inhibition of endothelin-1 induced myocardial protein synthesis by an antisense oligonucleotide against the early growth response gene-1

1991 • 45 citations

Non–Sequence-Specific Inhibition of Transferrin Receptor Expression in HL-60 Leukemia Cells by Phosphorothioate Oligodeoxynucleotides

1991 • 43 citations

An antisense oligonucleotide complementary to a sequence in I gamma 2b increases gamma 2b germline transcripts, stimulates B cell DNA synthesis, and inhibits immunoglobulin secretion.

1992 • 43 citations

Cell Membranes as Barriers for Antisense Constructions

1992 • 34 citations

Binding of oligonucleotides to cell membranes at acidic pH

1991 • 34 citations

Preparation of 35S-labeled polyphosphorothioate oligodeoxyribonucleotides by use of hydrogen phosphonate chemistry

1990 • 33 citations

The role of the c-fms oncogene in the regulation of HL-60 cell differentiation.

1990 • 30 citations

Modulation of interleukin 1 beta gene expression using antisense phosphorothioate oligonucleotides.

1990 • 27 citations

Retinoid receptor antisense DNAs inhibit alkaline phosphatase induction and clonogenicity in malignant keratinocytes.

1989 • 27 citations

Inhibition of murine monocyte proliferation by a colony-stimulating factor-1 antisense oligodeoxynucleotide. Evidence for autocrine regulation.

1990 • 26 citations

Antisense oligodeoxynucleotide to the cystic fibrosis gene inhibits anion transport in normal cultured sweat duct cells.

1991 • 25 citations

Lipofectin Enhances Cellular Uptake of Antisense DNA While Inhibiting Tumor Cell Growth

1992 • 22 citations

The Use of Antisense Oligonucleotides to Establish Autocrine Angiotensin Growth Effects in Human Neuroblastoma and Mesangial Cells

1992 • 17 citations

Inhibition of the Binding of HIV rgp120 to CD4 by Dyes

1992 • 17 citations

Phosphorothioate Oligonucleotides as Potential Antiviral Compounds Against Human Immunodeficiency Virus and Herpes Viruses

1991 • 15 citations

A novel method to modulate desensitization and truncation of luteinizing hormone receptors using antisense oligodeoxynucleotides

1991 • 13 citations

Antisense Inhibition of β-Glucuronidase Expression in Preimplantation Mouse Embryos: A Comparison of Transgenes and Oligodeoxynucleotides

1991 • 12 citations

First Antisense Drug Trials Planned In Leukemia

1992 • 11 citations

Applications of antisense oligodeoxynucleotides in immunology and autoimmunity research

1992 • 10 citations

Antisense Strategies to Characterize the Role of Genes and Oncogenes Involved in Myeloid Differentiationa

1992 • 10 citations

Alterations in the expression of muscle-specific genes mediated by troponin C antisense oligodeoxynucleotide

1991 • 8 citations

Stimulation of Calcium Influx in HL60 Cells by Cholesteryl-Modified Homopolymer Oligodeoxynucleotides

1992 • 6 citations

Influence on metastasis of the reduction of major histocompatibility complex (MHC) class I gene with an antisense oligonucleotide.

1992 • 4 citations