Empirical and rational approaches for development of inhibitors of the human immunodeficiency virus — HIV-1

3'-Azido-3'-deoxythymidine (BW A509U): an antiviral agent that inhibits the infectivity and cytopathic effect of human T-lymphotropic virus type III/lymphadenopathy-associated virus in vitro.

1985 • 1,830 citations

Inhibition of Rous sarcoma virus replication and cell transformation by a specific oligodeoxynucleotide.

1978 • 1,668 citations

HIV with Reduced Sensitivity to Zidovudine (AZT) Isolated During Prolonged Therapy

1989 • 1,574 citations

Sequence-Specific Cleavage of Double Helical DNA by Triple Helix Formation

1987 • 1,275 citations

Conserved Folding in Retroviral Proteases: Crystal Structure of Synthetic HIV-1 Protease

1989 • 1,155 citations

Three-dimensional structure of aspartyl protease from human immunodeficiency virus HIV-1

1989 • 883 citations

Mitochondrial Myopathy Caused by Long-Term Zidovudine Therapy

1990 • 845 citations

ADMINISTRATION OF 3'-AZIDO-3'-DEOXYTHYMIDINE, AN INHIBITOR OF HTLV-III/LAV REPLICATION, TO PATIENTS WITH AIDS OR AIDS-RELATED COMPLEX

1986 • 806 citations

Molecular Targets for AIDS Therapy

1990 • 736 citations

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

1987 • 530 citations

The Site of Attachment in Human Rhinovirus 14 for Antiviral Agents That Inhibit Uncoating

1986 • 462 citations

THE ROLE OF ANTISENSE RNA IN GENE REGULATION

1986 • 456 citations

VIRAL PROTEINASES

1988 • 448 citations

Therapeutic Applications of Oligonucleotides

1992 • 438 citations

Oligodeoxynucleotides as inhibitors of gene expression: a review.

1988 • 419 citations

HIV protease: a novel chemotherapeutic target for AIDS

1991 • 411 citations

Uniformly modified 2'-deoxy-2'-fluoro-phosphorothioate oligonucleotides as nuclease-resistant antisense compounds with high affinity and specificity for RNA targets

1993 • 410 citations

Antisense Gene Inhibition by Oligonucleotides Containing C-5 Propyne Pyrimidines

1993 • 405 citations

Inhibition of replication and expression of human T-cell lymphotropic virus type III in cultured cells by exogenous synthetic oligonucleotides complementary to viral RNA.

1986 • 403 citations

The Atomic Structure of Mengo Virus at 3.0 Å Resolution

1987 • 353 citations

The HIV-1 Protease as a Therapeutic Target for AIDS

1992 • 343 citations

Both 2′,3′-dideoxythymidine and its 2′,3′-unsaturated derivative (2′,3′-dideoxythymidinene) are potent and selective inhibitors of human immunodeficiency virus replication in vitro

1987 • 340 citations

Differential Patterns of Intracellular Metabolism of 2′,3′-Didehydro-2′,3′-dideoxythymidine and 3′-Azido-2′,3′-dideoxythymidine, Two Potent Anti-human Immunodeficiency Virus Compounds

1989 • 340 citations

Nucleosides. V. The Monomesylates of 1-(2'-Deoxy-β-D-lyxofuranosyl)thymine^1,2

1964 • 337 citations

Synthesis and biological activities of iododeoxyuridine, an analog of thymidine

1959 • 332 citations

Specific antiviral activity of a poly(L-lysine)-conjugated oligodeoxyribonucleotide sequence complementary to vesicular stomatitis virus N protein mRNA initiation site.

1987 • 329 citations

Inhibition of the serine proteases leukocyte elastase, pancreatic elastase, cathepsin G, and chymotrypsin by peptide boronic acids.

1984 • 296 citations

Antiviral effect of an oligo(nucleoside methylphosphonate) complementary to the splice junction of herpes simplex virus type 1 immediate early pre-mRNAs 4 and 5.

1986 • 295 citations

Human immunodeficiency virus protease expressed in Escherichia coli exhibits autoprocessing and specific maturation of the gag precursor.

1987 • 285 citations

Delayed cytotoxicity and selective loss of mitochondrial DNA in cells treated with the anti-human immunodeficiency virus compound 2′,3′-dideoxycytidine

1989 • 270 citations

HIV Inhibitors Targeted at the Reverse Transcriptase

1992 • 262 citations

Potent and selective in vitro activity of 3' -deoxythymidin-2'-ene (3'-deoxy-2',3'-didehydrothymidine) against human immunodeficiency virus

1987 • 260 citations

A deletion mutation in the 5' part of the pol gene of Moloney murine leukemia virus blocks proteolytic processing of the gag and pol polyproteins

1985 • 249 citations

Use of 5-Iodo-2'-Deoxyuridine (IDU) in Treatment of Herpes Simplex Keratitis

1962 • 249 citations

Clinical Cure of Herpes Simplex Keratitis by 5-Iodo-2'-Deoxyuridine

1962 • 245 citations

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

1992 • 231 citations

Phosphorodithioate DNA as a Potential Therapeutic Drug

1993 • 219 citations

Retroviral protease-like sequence in the yeast transposon Ty 1

1985 • 219 citations

X-ray crystallographic study of boronic acid adducts with subtilisin BPN' (Novo). A model for the catalytic transition state.

1975 • 218 citations

1-(2,3-Dideoxy-.beta.-D-glycero-pent-2-enofuranosyl)thymine. A highly potent and selective anti-HIV agent

1989 • 216 citations

Evidence for the direct involvement of the rhinovirus canyon in receptor binding.

1988 • 211 citations

Cellular metabolism of 2',3'-dideoxycytidine, a compound active against human immunodeficiency virus in vitro.

1987 • 210 citations

Inhibitory effect of 2',3'-didehydro-2',3'-dideoxynucleosides on infectivity, cytopathic effects, and replication of human immunodeficiency virus

1987 • 208 citations

Susceptibilities of zidovudine-susceptible and -resistant human immunodeficiency virus isolates to antiviral agents determined by using a quantitative plaque reduction assay

1990 • 208 citations

Cellular pharmacology of 2',3'-dideoxy-2',3'-didehydrothymidine, a nucleoside analog active against human immunodeficiency virus

1989 • 201 citations

Nonionic nucleic acid analogs. Synthesis and characterization of dideoxyribonucleoside methylphosphonates

1979 • 186 citations

Present Status and Future Prospects for HIV Therapies

1993 • 184 citations

Inhibition of retroviral protease activity by an aspartyl proteinase inhibitor

1987 • 184 citations

Structural analysis of a series of antiviral agents complexed with human rhinovirus 14.

1988 • 183 citations

Human immunodeficiency virus 1 protease expressed in Escherichia coli behaves as a dimeric aspartic protease.

1989 • 180 citations

Physiological effects and metabolism of gossypol

1976 • 175 citations

Studies on the inhibition of mitochondrial DNA replication by 3′-azido-3′-dhoxythymidine and other dideoxynucleoside analogs which inhibit HIV-1 replication

1989 • 170 citations

2',3'-Didehydro-3'-deoxythymidine (d4T) in Patients with AIDS or AIDS-Related Complex: A Phase I Trial

1993 • 167 citations

Synthesis and antiviral activity of a series of HIV-1 protease inhibitors with functionality tethered to the P1 or P1' phenyl design

1992 • 167 citations

Activity of purified biosynthetic proteinase of human immunodeficiency virus on natural substrates and synthetic peptides.

1989 • 166 citations

Peptide substrates and inhibitors of the HIV-1 protease

1989 • 162 citations

Processing protease and reverse transcriptase from human immunodeficiency virus type I polyprotein in Escherichia coli

1988 • 151 citations

Dissociative inhibition of dimeric enzymes. Kinetic characterization of the inhibition of HIV-1 protease by its COOH-terminal tetrapeptide

1991 • 150 citations

Gossypol--a new antifertility agent for males.

1978 • 148 citations

2-Phenylethaneboronic acid, a possible transition-state analog for chymotrypsin

1971 • 144 citations

Serine protease mechanism: structure of an inhibitory complex of .alpha.-lytic protease and a tightly bound peptide boronic acid

1987 • 137 citations

Nitrogen-15 NMR spectroscopy of the catalytic-triad histidine of a serine protease in peptide boronic acid inhibitor complexes

1988 • 133 citations

Drug Discovery and Development

2006 • 133 citations

Retroviral proteases: First glimpses at the anatomy of a processing machine

1989 • 128 citations

Hydroxyethylene isostere inhibitors of human immunodeficiency virus-1 protease: structure-activity analysis using enzyme kinetics, x-ray crystallography, and infected T-cell assays

1992 • 128 citations

Non-nucleoside inhibitors of HIV-1 reverse transcriptase: molecular modeling and x-ray structure investigations

1993 • 126 citations

Induction of Endogenous Virus and of Thymidine Kinase by Bromodeoxyuridine in Cell Cultures Transformed by Friend Virus

1974 • 122 citations

Oligo(alpha-deoxynucleotide)s covalently linked to intercalating agents: differential binding to ribo- and deoxyribopolynucleotides and stability towards nuclease digestion.

1987 • 121 citations

Stability and activity of human immunodeficiency virus protease: comparison of the natural dimer with a homologous, single-chain tethered dimer.

1990 • 119 citations

Inhibition of Serine Proteases by Arylboronic Acids

1971 • 117 citations

Comparison of the crystal structures and intersubunit interactions of human immunodeficiency and Rous sarcoma virus proteases.

1990 • 104 citations

Selective inhibition of human immunodeficiency virus type 1 replication by the (-) but not the (+) enantiomer of gossypol

1989 • 104 citations

Pharmacokinetics of Stavudine in Patients with AIDS or AIDS-Related Complex

1992 • 103 citations

Recent advances in the design of HIV proteinase inhibitors

1992 • 97 citations

Antiviral activity of 2′,3′-dideoxycytidin-2′-ene (2′,3′-dideoxy-2′,3′-didehydrocytidine) against human immunodeficiency virus in vitro

1987 • 96 citations

Scientific and Social Issues of Human Immunodeficiency Virus Vaccine Development

1993 • 95 citations

Targeted therapy of human immunodeficiency virus‐related disease

1991 • 85 citations

Comparison of in vitro biological properties and mouse toxicities of three thymidine analogs active against human immunodeficiency virus

1990 • 84 citations

The pc12 cell as a model for studies of the mechanism of induction of peripheral neuropathy by anti-HIV-1 dideoxynucleoside analogs

1991 • 83 citations

DNA triple‐helix formation: An approach to artificial gene repressors?

1992 • 83 citations

Gossypol – a New Antifertility Agent for Males

1979 • 83 citations

Antiviral activities of gossypol and its derivatives against herpes simplex virus type II

1986 • 80 citations

Targets and strategies for the antiviral chemotherapy of AIDS

1990 • 77 citations

Kinetic properties of the binding of .alpha.-lytic protease to peptide boronic acids

1988 • 76 citations

Molecular graphics and drug design

1986 • 71 citations

Anti-HIV-1 activity and cellular pharmacology of various analogs of gossypol

1993 • 70 citations

The National Cancer Institute Phase I Study of 2′,3′-Dideoxyinosine Administration in Adults with AIDS or AIDS-Related Complex: Analysis of Activity and Toxicity Profiles

1990 • 68 citations

Crystal structure of a complex of HIV‐1 protease with a dihydroxyethylene‐containing inhibitor: Comparisons with molecular modeling

1992 • 68 citations

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

1987 • 68 citations

Inhibiting herpes simplex virus type 2 infection in human epithelial cells by gossypol, a potent spermicidal and contraceptive agent

1982 • 67 citations

Peptide aldehydes as inhibitors of HIV protease

1993 • 67 citations

Strategies for indirect computer-aided drug design.

1993 • 66 citations

HIV Drug Resistance

1993 • 65 citations

n-Alkylboronic acids as bifunctional reversible inhibitors of α-chymotrypsin

1970 • 63 citations

Pharmacokinetics of (±)-, (+)-, and (−)-gossypol in humans and dogs

1986 • 61 citations

Two-step binding mechanism for HIV protease inhibitors

1992 • 59 citations

2′,3′-Didehydro-2′,3′-dideoxythymidine (D4T), an anti-HIV Agent

1991 • 56 citations

Resolution of gossypol: Analytical and preparative HPLC

1984 • 53 citations

Antiviral Activity of Gossypol and Apogossypol

1975 • 52 citations

Retrovirus protease characterized as a dimeric aspartic proteinase

1989 • 50 citations

Anti-retroviral therapy of AIDS and related disorders: General principles and specific development of dideoxynucleosides

1989 • 50 citations

Inhibition of retroviral replication by anti-sense RNA.

1986 • 47 citations

Activity and dimerization of human immunodeficiency virus protease as a function of solvent composition and enzyme concentration.

1992 • 46 citations

Advances in Chemotherapy of AIDS

1990 • 45 citations

3'-Deoxythymidin-2'-ene permeation of human lymphocyte H9 cells by nonfacilitated diffusion.

1991 • 43 citations

Cellular pharmacology of 2′,3′-didehydro-2′,3′-dideoxythymidine (D4T) in human peripheral blood mononuclear cells

1990 • 41 citations

Potent HIV-1 protease inhibitors: stereoselective synthesis of a dipeptide mimic

1993 • 41 citations

Initial studies on the cellular pharmacology of 3'-deoxythymidin-2'-ene (d4t): A potent and selective inhibitor of human immunodeficiency virus

1988 • 40 citations

Structural studies of the anti-HIV agent 2′,3′-didehydro-2′,3′-dideoxythymidine (D4T)

1991 • 39 citations

Crystallization of the aspartylprotease from the human immunodeficiency virus, HIV-1

1989 • 37 citations

Basic approaches to anti-retroviral treatment.

1991 • 36 citations

Novel nucleoside strategies for anti-HIV and anti-HSV therapy

1992 • 36 citations

Synthesis of hexanucleotide analogues containing diisopropylsilyl internucleotide linkages

1988 • 36 citations

Inhibitor binding to the Phe53Trp mutant of HIV-1 protease promotes conformational changes detectable by spectrofluorometry

1993 • 35 citations

Disposition in animals of a new anti-HIV agent: 2',3'-didehydro-3'-deoxythymidine.

1990 • 31 citations

Antiretroviral therapy: strategies beyond single-agent reverse transcriptase inhibition

1992 • 30 citations

Metabolism and DNA interaction of 2',3'-didehydro-2',3'-dideoxythymidine in human bone marrow cells.

1991 • 30 citations

Properties of 2′,3′‐dideoxy‐2′,3′‐dehydrothymidine 5′‐triphosphate in terminating DNA synthesis catalyzed by several different DNA polymerases

1987 • 30 citations

Nonenzymatic sequence-specific cleavage of single-stranded DNA to nucleotide resolution. DNA methyl thioether probes

1987 • 29 citations

Drug Discovery and Development

1987 • 28 citations

Enzymatic and chemical stability of 2',3'-dideoxy-2',3'-didehydropyrimidine nucleosides: Potential anti-acquired immunodeficiency syndrome agents.

1989 • 26 citations

Chapter 29. Macromolecular X-Ray Crystallography and NMR as Tools for Structure-based Drug Design

1992 • 24 citations

Anti-AIDS drug development: challenges and strategies.

1992 • 23 citations

Resolution of racemic gossypol and interaction of individual enantiomers with serum albumins and model peptides

1986 • 22 citations

Inhibition of HIV by an anti-HIV protease synthetic peptide blocks an early step of viral replication

1992 • 21 citations

Resolution of racemic gossypol

1985 • 21 citations

Computer-Assisted Structure-Activity Correlations of Halodideoxynucleoside Analogs as Potential Anti-HIV Drugs

1992 • 21 citations

Comparative Studies of 2′,3′‐Didehydro‐2′,3′‐Dideoxythymidine (D4T) with other Pyrimidine Nucleoside Analogues

1990 • 20 citations

Antisense inhibitors of HIV: Problems and perspectives

1992 • 16 citations

Common cold viruses

1987 • 14 citations

[Antiviral properties of gossypol in experimental influenza pneumonia].

1970 • 14 citations

Äntisense nucleic acids as a potential class of pharmaceutical agents

1988 • 13 citations

Pharmacokinetics of A New Anti-HIV Ageht: 2',3'-Dideoxy-2',3'-Didehydrothymidine (d4T)

1989 • 11 citations

Viral receptors and drug design

1988 • 10 citations

RESOLUTION OF RACEMIC GOSSYPOL

1983 • 10 citations

A new peptide boronic acid inhibitor of elastase-induced lung injury in hamsters.

1986 • 8 citations

Metabolism and mode of selective inhibition of human immunodeficiency virus replication by 3'-azido-2',3'-dideoxy-5-iodouridine and 3'-azido-2',3'-dideoxy-5-bromouridine

1993 • 7 citations

Pharmacologic Studies of Nucleosides Active against the Human Immunodeficiency Virus^a

1990 • 7 citations

Dose-escalating study of safety and efficacy of dideoxy-didehydrothymidine (d4T) for HIV infection

1990 • 4 citations

How Can HIV Replication Be Controlled?

1993 • 3 citations

Computer-Aided Molecular Design Has Continuing Impact

1993 • 2 citations

2′,3′-dideoxy-2′,3′-didehydrothymidine (D4T): A potent and selective agent against human immunodeficiency virus (HIV)

1988 • 2 citations

Drug Design Effort Targets Parasite Proteases

1993 • 1 citations

Effects of 2′3′-dideoxycytidine (DDC) an anti HIV-1 nucleoside analogue on mitochondrial biogenesis, structure and function

1991 • 1 citations

Deleted Work

1955 • 0 citations