Design of Non-Nucleoside Inhibitors of HIV-1 Reverse Transcriptase with Improved Drug Resistance Properties. 1.

Crystallography & NMR System: A New Software Suite for Macromolecular Structure Determination

1998 • 15,791 citations

The nature of .pi.-.pi. interactions

1990 • 4,985 citations

Rapid turnover of plasma virions and CD4 lymphocytes in HIV-1 infection

1995 • 4,310 citations

HIV-1 Dynamics in Vivo: Virion Clearance Rate, Infected Cell Life-Span, and Viral Generation Time

1996 • 3,496 citations

Van Damme A.

1986 • 3,477 citations

Viral dynamics in human immunodeficiency virus type 1 infection

1995 • 3,277 citations

A computational procedure for determining energetically favorable binding sites on biologically important macromolecules

1985 • 2,597 citations

Accurate bond and angle parameters for X-ray protein structure refinement

1991 • 2,467 citations

Restart procedures for the conjugate gradient method

1977 • 1,684 citations

Crystal structure of human immunodeficiency virus type 1 reverse transcriptase complexed with double-stranded DNA at 3.0 A resolution shows bent DNA.

1993 • 1,097 citations

Interactive computer graphics: FRODO

1985 • 848 citations

Potent and selective inhibition of HIV-1 replication in vitro by a novel series of TIBO derivatives

1990 • 749 citations

Mechanism of Inhibition of HIV-1 Reverse Transcriptase by Nonnucleoside Inhibitors

1995 • 523 citations

High resolution structures of HIV-1 RT from four RT–inhibitor complexes

1995 • 498 citations

Opposite Modulation of Cocaine-Seeking Behavior by D ₁ - and D ₂ -Like Dopamine Receptor Agonists

1996 • 493 citations

Mechanism of inhibition of HIV-1 reverse transcriptase by non-nucleoside inhibitors

1995 • 435 citations

A novel lead for specific anti-HIV-1 agents: 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine

1989 • 376 citations

The role of non-nucleoside reverse transcriptase inhibitors (NNRTIs) in the therapy of HIV-1 infection1Presented at the Eleventh International Conference on Antiviral Research, San Diego, CA, 5–10 April 1998.1

1998 • 351 citations

Complexes of HIV-1 Reverse Transcriptase with Inhibitors of the HEPT Series Reveal Conformational Changes Relevant to the Design of Potent Non-Nucleoside Inhibitors

1996 • 338 citations

Mutations in Retroviral Genes Associated with Drug Resistance

1996 • 288 citations

Highly specific inhibition of human immunodeficiency virus type 1 by a novel 6-substituted acyclouridine derivative

1989 • 288 citations

Drug resistance mutations in HIV-1.

2004 • 282 citations

Comparative computer graphics and solution studies of the DNA interaction of substituted anthraquinones based on doxorubicin and mitoxantrone

1985 • 276 citations

Human Immunodeficiency Virus Type 1 Mutations Selected in Patients Failing Efavirenz Combination Therapy

2000 • 274 citations

Paradoxes of adherence and drug resistance to HIV antiretroviral therapy

2004 • 269 citations

Pol gene quasispecies of human immunodeficiency virus: mutations associated with drug resistance in virus from patients undergoing no drug therapy

1995 • 239 citations

The Lys103Asn mutation of HIV-1 RT: a novel mechanism of drug resistance

2001 • 193 citations

Unique features in the structure of the complex between HIV-1 reverse transcriptase and the bis(heteroaryl)piperazine (BHAP) U-90152 explain resistance mutations for this nonnucleoside inhibitor

1997 • 190 citations

Crystal Structures of 8-Cl and 9-Cl TIBO Complexed with Wild-type HIV-1 RT and 8-Cl TIBO Complexed with the Tyr181Cys HIV-1 RT Drug-resistant Mutant

1996 • 187 citations

Structural mechanisms of drug resistance for mutations at codons 181 and 188 in HIV-1 reverse transcriptase and the improved resilience of second generation non-nucleoside inhibitors 1 1Edited by J. Karn

2001 • 182 citations

The structure of HIV-1 reverse transcriptase complexed with 9-chloro-TIBO: lessons for inhibitor design

1995 • 173 citations

An antiviral target on reverse transcriptase of human immunodeficiency virus type 1 revealed by tetrahydroimidazo-[4,5,1-jk] [1,4]benzodiazepin-2 (1H)-one and -thione derivatives.

1991 • 166 citations

Perspectives of non-nucleoside reverse transcriptase inhibitors (NNRTIs) in the therapy of HIV-1 infection

1999 • 157 citations

S-1153 Inhibits Replication of Known Drug-Resistant Strains of Human Immunodeficiency Virus Type 1

1998 • 124 citations

Current Status of the Non-nucleoside Reverse Transcriptase Inhibitors of Human Immunodeficiency Virus Type 1

2004 • 124 citations

Structures of Tyr188Leu mutant and wild-type HIV-1 reverse transcriptase complexed with the non-nucleoside inhibitor HBY 097: inhibitor flexibility is a useful design feature for reducing drug resistance 1 1Edited by J. Karn

1998 • 123 citations

Binding of the Second Generation Non-nucleoside Inhibitor S-1153 to HIV-1 Reverse Transcriptase Involves Extensive Main Chain Hydrogen Bonding

2000 • 119 citations

Activity of a novel quinoxaline derivative against human immunodeficiency virus type 1 reverse transcriptase and viral replication

1993 • 117 citations

Non-Nucleoside HIV-1 Reverse Transcriptase (RT) Inhibitors: Past, Present, and Future Perspectives

2002 • 114 citations

Design of MKC-442 (Emivirine) Analogues with Improved Activity Against Drug-Resistant HIV Mutants

1999 • 112 citations

A Rapid and Simple Colorimetric Test for the Study of Anti-HIV Agents

1988 • 98 citations

Resistance to nevirapine of HIV-1 reverse transcriptase mutants: loss of stabilizing interactions and thermodynamic or steric barriers are induced by different single amino acid substitutions

1997 • 97 citations

Alterations to the Primer Grip of p66 HIV-1 Reverse Transcriptase and Their Consequences for Template-Primer Utilization

1996 • 95 citations

Preclinical evaluation of HBY 097, a new nonnucleoside reverse transcriptase inhibitor of human immunodeficiency virus type 1 replication

1995 • 85 citations

Anti-human immunodeficiency virus synergism by zidovudine (3'-azidothymidine) and didanosine (dideoxyinosine) contrasts with their additive inhibition of normal human marrow progenitor cells

1991 • 82 citations

Alanine-scanning Mutations in the ;Primer Grip; of p66 HIV-1 Reverse Transcriptase Result in Selective Loss of RNA Priming Activity

1997 • 75 citations

Mutations within the Primer Grip Region of HIV-1 Reverse Transcriptase Result in Loss of RNase H Function

1997 • 74 citations

Micromethod for assaying reverse transcriptase of human T-cell lymphotropic virus type III/lymphadenopathy-associated virus

1987 • 73 citations

Mutating the “primer grip” of p66 HIV-1 reverse transcriptase implicates tryptophan-229 in template-primer utilization

1994 • 72 citations

HIV-1 reverse transcriptase inhibition by a dipyridodiazepinone derivative: BI-RG-587

1992 • 69 citations

Kinetic Analysis of Four HIV-1 Reverse Transcriptase Enzymes Mutated in the Primer Grip Region of p66

1997 • 67 citations

HIV-1 Reverse Transcriptase Resistance to Nonnucleoside Inhibitors

1996 • 65 citations

Design of Non-nucleoside Inhibitors of HIV-1 Reverse Transcriptase with Improved Drug Resistance Properties. 2.

2004 • 62 citations

5-Chloro-2',3'-dideoxy-3'-fluorouridine (935U83), a selective anti-human immunodeficiency virus agent with an improved metabolic and toxicological profile

1994 • 61 citations

Crystals of HIV-1 Reverse Transcriptase Diffracting to 2·2 Å Resolution

1994 • 61 citations

Mutating a Conserved Motif of the HIV-1 Reverse Transcriptase Palm Subdomain Alters Primer Utilization

1997 • 52 citations

Pharmacodynamic Activity and Efficacy of Linezolid in a Rat Model of Pneumococcal Pneumonia

2002 • 50 citations

Structural and biochemical effects of human immunodeficiency virus mutants resistant to non-nucleoside reverse transcriptase inhibitors

2004 • 49 citations

Mutational analysis of trp-229 of human immunodeficiency virus type 1 reverse transcriptase (RT) identifies this amino acid residue as a prime target for the rational design of new non-nucleoside RT inhibitors.

2000 • 47 citations

Short Communication: A Novel Mutation (F227L) Arises in the Reverse Transcriptase of Human Immunodeficiency Virus Type 1 on Dose-Escalating Treatment of HIV Type 1-Infected Cell Cultures with the Nonnucleoside Reverse Transcriptase Inhibitor Thiocarboxanilide UC-781

1998 • 43 citations

A Mutation in the 3′ Region of the Human Immunodeficiency Virus Type 1 Reverse Transcriptase (Y318F) Associated with Nonnucleoside Reverse Transcriptase Inhibitor Resistance

2002 • 42 citations

The phase problem and its relation to the spin-glass problem

1991 • 39 citations

Anti-HIV compound assessment by two novel high capacity assays

1989 • 38 citations

Mutations in the Primer Grip of Human Immunodeficiency Virus Type 1 Reverse Transcriptase Impair Proviral DNA Synthesis and Virion Maturation

1998 • 34 citations

In VitroSelection for Different Mutational Patterns in the HIV-1 Reverse Transcriptase Using High and Low Selective Pressure of the Nonnucleoside Reverse Transcriptase Inhibitor HBY 097

1997 • 34 citations

Mutational Analysis of Tyr-318 within the Non-nucleoside Reverse Transcriptase Inhibitor Binding Pocket of Human Immunodeficiency Virus Type I Reverse Transcriptase

1998 • 31 citations

Characteristics of the Pro225His mutation in human immunodeficiency virus type 1 (HIV-1) reverse transcriptase that appears under selective pressure of dose-escalating quinoxaline treatment of HIV-1

1997 • 20 citations

A proline-to-histidine substitution at position 225 of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT) sensitizes HIV-1 RT to BHAP U-90152.

1998 • 14 citations

Rationalization of molecular models

1985 • 12 citations

Allosteric Inhibitors against HIV-1 Reverse Transcriptase: Design and Synthesis of MKC-442 Analogues Having an Ω-Functionalized Acyclic Structure

1998 • 8 citations