List of works - Stefan G. Sarafianos

2'-deoxy-4'-C-ethynyl-2-halo-adenosines active against drug-resistant human immunodeficiency virus type 1 variants

scientific article

3-Hydroxypyrimidine-2,4-dione-5-N-benzylcarboxamides Potently Inhibit HIV-1 Integrase and RNase H.

scientific article published on 10 June 2016

3-Hydroxypyrimidine-2,4-diones as Selective Active Site Inhibitors of HIV Reverse Transcriptase-Associated RNase H: Design, Synthesis, and Biochemical Evaluations.

scientific article published on March 2016

4'-modified nucleoside analogs: potent inhibitors active against entecavir-resistant hepatitis B virus.

scientific article

6-Cyclohexylmethyl-3-hydroxypyrimidine-2,4-dione as an inhibitor scaffold of HIV reverase transcriptase: Impacts of the 3-OH on inhibiting RNase H and polymerase

scientific article published on 30 January 2017

AT32P-dependent estimation of nanomoles of fatty acids: its use in the assay of phospholipase A2 activity

scientific article published on 01 May 1990

Adaptation of HIV-1/HIV-2 Chimeras with Defects in Genome Packaging and Viral Replication

scientific article published in 2022

Amino acid mutation N348I in the connection subdomain of human immunodeficiency virus type 1 reverse transcriptase confers multiclass resistance to nucleoside and nonnucleoside reverse transcriptase inhibitors

scientific article

Analysis of mutations at positions 115 and 116 in the dNTP binding site of HIV-1 reverse transcriptase.

scientific article

Antiviral drugs specific for coronaviruses in preclinical development

scientific article

Antiviral therapies: focus on hepatitis B reverse transcriptase

scientific article

Biochemical analysis of catalytically crucial aspartate mutants of human immunodeficiency virus type 1 reverse transcriptase.

scientific article

Biochemical mechanism of HIV-1 resistance to rilpivirine

scientific article

Biochemical, inhibition and inhibitor resistance studies of xenotropic murine leukemia virus-related virus reverse transcriptase

scientific article published on 8 September 2011

Biochemistry. RT slides home...

scientific article

Broad-spectrum aptamer inhibitors of HIV reverse transcriptase closely mimic natural substrates.

scientific article

CODAS syndrome is associated with mutations of LONP1, encoding mitochondrial AAA+ Lon protease.

scientific article

Clinical relevance of substitutions in the connection subdomain and RNase H domain of HIV-1 reverse transcriptase from a cohort of antiretroviral treatment-naïve patients

scientific article

Crystal structure of HIV-1 reverse transcriptase in complex with a polypurine tract RNA:DNA

scientific article

Cutting into the Substrate Dominance: Pharmacophore and Structure-Based Approaches toward Inhibiting Human Immunodeficiency Virus Reverse Transcriptase-Associated Ribonuclease H

scientific article published on 27 December 2019

Design of peptide-based inhibitors for human immunodeficiency virus type 1 strains resistant to T-20

scientific article published on 10 December 2008

Design, Synthesis, and Biological Evaluations of Hydroxypyridonecarboxylic Acids as Inhibitors of HIV Reverse Transcriptase Associated RNase H.

scientific article published on 20 April 2016

Design, synthesis, biochemical, and antiviral evaluations of C6 benzyl and C6 biarylmethyl substituted 2-hydroxylisoquinoline-1,3-diones: dual inhibition against HIV reverse transcriptase-associated RNase H and polymerase with antiviral activities

scientific article

Determinants of Active-Site Inhibitor Interaction with HIV-1 RNase H

scientific article published on 02 October 2019

Development of a vaginal delivery film containing EFdA, a novel anti-HIV nucleoside reverse transcriptase inhibitor

scientific article published on 09 December 2013

Divergent evolution in reverse transcriptase (RT) of HIV-1 group O and M lineages: impact on structure, fitness, and sensitivity to nonnucleoside RT inhibitors.

scientific article

Drug resistance in non-B subtype HIV-1: impact of HIV-1 reverse transcriptase inhibitors

scientific article

Effect of mutations at position E138 in HIV-1 reverse transcriptase and their interactions with the M184I mutation on defining patterns of resistance to nonnucleoside reverse transcriptase inhibitors rilpivirine and etravirine

scientific article published on 22 April 2013

Effects of substitutions at the 4' and 2 positions on the bioactivity of 4'-ethynyl-2-fluoro-2'-deoxyadenosine

scientific article published on 07 October 2013

Evaluation of Combinations of 4'-Ethynyl-2-Fluoro-2'-Deoxyadenosine with Clinically Used Antiretroviral Drugs

scientific article published on 24 June 2013

Evaluation of SSYA10-001 as a replication inhibitor of severe acute respiratory syndrome, mouse hepatitis, and Middle East respiratory syndrome coronaviruses

scientific article published on 19 May 2014

Expression and purification of SARS coronavirus proteins using SUMO-fusions.

scientific article published on 23 February 2005

Expression, purification, and characterization of SARS coronavirus RNA polymerase.

scientific article

Factors influencing the efficacy of rilpivirine in HIV-1 subtype C in low- and middle-income countries

scientific article

Fast hepatitis C virus RNA elimination and NS5A redistribution by NS5A inhibitors studied by a multiplex assay approach

scientific article published on 6 April 2015

Future treatment strategies for novel Middle East respiratory syndrome coronavirus infection

scientific article published on December 2013

Glutamine 151 participates in the substrate dNTP binding function of HIV-1 reverse transcriptase

scientific article published on 01 May 1995

HIV-1 resistance mechanism to an electrostatically constrained peptide fusion inhibitor that is active against T-20-resistant strains

scientific article published on 20 May 2013

Hypersusceptibility mechanism of Tenofovir-resistant HIV to EFdA.

scientific article published on 24 June 2013

Identification and characterization of coumestans as novel HCV NS5B polymerase inhibitors.

scientific article published on 18 January 2008

In vitro transport characteristics of EFdA, a novel nucleoside reverse transcriptase inhibitor using Caco-2 and MDCKII cell monolayers

scientific article

Increased replication capacity following evolution of PYxE insertion in Gag-p6 is associated with enhanced virulence in HIV-1 subtype C from East Africa.

scientific article

Inhibition of bacterial RNA polymerase by streptolydigin: stabilization of a straight-bridge-helix active-center conformation

scientific article

Inhibitors of HIV-1 Reverse Transcriptase-Associated Ribonuclease H Activity

scientific article published on October 2012

Inhibitors of foot and mouth disease virus targeting a novel pocket of the RNA-dependent RNA polymerase

scientific article

Interactions of conformationally biased north and south 2'-fluoro-2', 3'-dideoxynucleoside 5'-triphosphates with the active site of HIV-1 reverse transcriptase.

scientific article published in September 2000

K70Q adds high-level tenofovir resistance to "Q151M complex" HIV reverse transcriptase through the enhanced discrimination mechanism

scientific article

Lamivudine (3TC) resistance in HIV-1 reverse transcriptase involves steric hindrance with beta-branched amino acids

scientific article

Marine Natural Products as Leads against SARS-CoV-2 Infection

publication published on 15 March 2022

Mechanism of inhibition of HIV-1 reverse transcriptase by 4'-Ethynyl-2-fluoro-2'-deoxyadenosine triphosphate, a translocation-defective reverse transcriptase inhibitor.

scientific article published on December 2009

Mechanism of interaction of human mitochondrial DNA polymerase γ with the novel nucleoside reverse transcriptase inhibitor 4'-ethynyl-2-fluoro-2'-deoxyadenosine indicates a low potential for host toxicity.

scientific article published on 12 December 2011

Mechanism of nucleic acid unwinding by SARS-CoV helicase.

scientific article

Mechanism of resistance to S138A substituted enfuvirtide and its application to peptide design

scientific article

Molecular biology: an HIV secret uncovered

scientific article published on 01 May 2008

Molecular model of SARS coronavirus polymerase: implications for biochemical functions and drug design

scientific article

Multifunctionality of a picornavirus polymerase domain: nuclear localization signal and nucleotide recognition

scientific article published on 22 April 2015

Mutation of amino acids in the connection domain of human immunodeficiency virus type 1 reverse transcriptase that contact the template-primer affects RNase H activity.

scientific article

Mutations in the 5′ End of the Human Immunodeficiency Virus Type 1 Polypurine Tract Affect RNase H Cleavage Specificity and Virus Titer ⬇️

scientific article published on October 1, 2003

Mutations in the RNase H domain of HIV-1 reverse transcriptase affect the initiation of DNA synthesis and the specificity of RNase H cleavage in vivo.

scientific article

Novel Hepatitis B Virus Capsid-Targeting Antiviral That Aggregates Core Particles and Inhibits Nuclear Entry of Viral Cores

scientific article published on 14 January 2019

Nucleoside analog resistance caused by insertions in the fingers of human immunodeficiency virus type 1 reverse transcriptase involves ATP-mediated excision.

scientific article

Oral administration of the nucleoside EFdA (4'-ethynyl-2-fluoro-2'-deoxyadenosine) provides rapid suppression of HIV viremia in humanized mice and favorable pharmacokinetic properties in mice and the rhesus macaque

scientific article

Potent anti-HIV-1 activity of N-HR-derived peptides including a deep pocket-forming region without antagonistic effects on T-20

scientific article

Preformulation studies of EFdA, a novel nucleoside reverse transcriptase inhibitor for HIV prevention

scientific article

Probing the molecular mechanism of action of the HIV-1 reverse transcriptase inhibitor 4'-ethynyl-2-fluoro-2'-deoxyadenosine (EFdA) using pre-steady-state kinetics

scientific article

Remembering Professor Walter A. Scott

scientific article

Repeated exposure to 5D9, an inhibitor of 3D polymerase, effectively limits the replication of foot-and-mouth disease virus in host cells

scientific article

Resistance profiles of novel electrostatically constrained HIV-1 fusion inhibitors

scientific article

Response of simian immunodeficiency virus to the novel nucleoside reverse transcriptase inhibitor 4'-ethynyl-2-fluoro-2'-deoxyadenosine in vitro and in vivo

scientific article

Restriction fragment mass polymorphism (RFMP) analysis based on MALDI-TOF mass spectrometry for detecting antiretroviral resistance in HIV-1 infected patients

scientific article

Rev-derived peptides inhibit HIV-1 replication by antagonism of Rev and a co-receptor, CXCR4.

scientific article published on 16 May 2010

Reverse transcriptase in motion: conformational dynamics of enzyme-substrate interactions

scientific article

Role of methionine 184 of human immunodeficiency virus type-1 reverse transcriptase in the polymerase function and fidelity of DNA synthesis.

scientific article published in February 1996

SAMHD1 has differential impact on the efficacies of HIV nucleoside reverse transcriptase inhibitors.

scientific article

SC29EK, a peptide fusion inhibitor with enhanced alpha-helicity, inhibits replication of human immunodeficiency virus type 1 mutants resistant to enfuvirtide

scientific article published on 29 December 2008

STRUCTURAL VIROLOGY. X-ray crystal structures of native HIV-1 capsid protein reveal conformational variability.

scientific article

Selective excision of AZTMP by drug-resistant human immunodeficiency virus reverse transcriptase

scientific article

Severe acute respiratory syndrome coronavirus replication inhibitor that interferes with the nucleic acid unwinding of the viral helicase

scientific article

Similarities and differences in the RNase H activities of human immunodeficiency virus type 1 reverse transcriptase and Moloney murine leukemia virus reverse transcriptase.

scientific article published on December 1999

Site-directed mutagenesis of arginine 72 of HIV-1 reverse transcriptase. Catalytic role and inhibitor sensitivity

scientific article published on 01 August 1995

Structural basis of HIV-1 resistance to AZT by excision

scientific article

Structural basis of clade-specific HIV-1 neutralization by humanized anti-V3 monoclonal antibody KD-247.

scientific article

Structural determinants of slippage-mediated mutations by human immunodeficiency virus type 1 reverse transcriptase

scientific article

Structural requirements for RNA degradation by HIV-1 reverse transcriptase.

scientific article published in December 2013

Structure and function of HIV-1 reverse transcriptase: molecular mechanisms of polymerization and inhibition

scientific article

Structure and functional implications of the polymerase active site region in a complex of HIV-1 RT with a double-stranded DNA template-primer and an antibody Fab fragment at 2.8 A resolution

scientific article

Subunit-specific analysis of the human immunodeficiency virus type 1 reverse transcriptase in vivo.

scientific article

Synthesis of AZTpSpCX2ppSA and AZTpSpCX2ppSAZT: hydrolysis-resistant potential inhibitors of the AZT excision reaction of HIV-1 RT

scientific article published on 08 November 2007

Synthesis of Boranoate, Selenoate, and Thioate Analogs of AZTp(4)A and Ap(4)A.

scientific article published on September 2009

The N348I mutation at the connection subdomain of HIV-1 reverse transcriptase decreases binding to nevirapine.

scientific article

The RNA polymerase "switch region" is a target for inhibitors

scientific article

The hepatitis B virus ribonuclease H is sensitive to inhibitors of the human immunodeficiency virus ribonuclease H and integrase enzymes

scientific article

The mutation T477A in HIV-1 reverse transcriptase (RT) restores normal proteolytic processing of RT in virus with Gag-Pol mutated in the p51-RNH cleavage site

scientific article

The role of steric hindrance in 3TC resistance of human immunodeficiency virus type-1 reverse transcriptase.

scientific article published in July 2000

Trapping HIV-1 reverse transcriptase before and after translocation on DNA.

scientific article published on 28 January 2003

Vaginal Microbicide Film Combinations of Two Reverse Transcriptase Inhibitors, EFdA and CSIC, for the Prevention of HIV-1 Sexual Transmission

scientific article published on 21 March 2015

YADD mutants of human immunodeficiency virus type 1 and Moloney murine leukemia virus reverse transcriptase are resistant to lamivudine triphosphate (3TCTP) in vitro.

scientific article published in July 2001

List of works by Stefan G. Sarafianos

2'-deoxy-4'-C-ethynyl-2-halo-adenosines active against drug-resistant human immunodeficiency virus type 1 variants

3-Hydroxypyrimidine-2,4-dione-5-N-benzylcarboxamides Potently Inhibit HIV-1 Integrase and RNase H.

3-Hydroxypyrimidine-2,4-diones as Selective Active Site Inhibitors of HIV Reverse Transcriptase-Associated RNase H: Design, Synthesis, and Biochemical Evaluations.

4'-modified nucleoside analogs: potent inhibitors active against entecavir-resistant hepatitis B virus.

6-Cyclohexylmethyl-3-hydroxypyrimidine-2,4-dione as an inhibitor scaffold of HIV reverase transcriptase: Impacts of the 3-OH on inhibiting RNase H and polymerase

AT32P-dependent estimation of nanomoles of fatty acids: its use in the assay of phospholipase A2 activity

Adaptation of HIV-1/HIV-2 Chimeras with Defects in Genome Packaging and Viral Replication

Amino acid mutation N348I in the connection subdomain of human immunodeficiency virus type 1 reverse transcriptase confers multiclass resistance to nucleoside and nonnucleoside reverse transcriptase inhibitors

Analysis of mutations at positions 115 and 116 in the dNTP binding site of HIV-1 reverse transcriptase.

Antiviral drugs specific for coronaviruses in preclinical development

Antiviral therapies: focus on hepatitis B reverse transcriptase

Biochemical analysis of catalytically crucial aspartate mutants of human immunodeficiency virus type 1 reverse transcriptase.

Biochemical mechanism of HIV-1 resistance to rilpivirine

Biochemical, inhibition and inhibitor resistance studies of xenotropic murine leukemia virus-related virus reverse transcriptase

Biochemistry. RT slides home...

Broad-spectrum aptamer inhibitors of HIV reverse transcriptase closely mimic natural substrates.

CODAS syndrome is associated with mutations of LONP1, encoding mitochondrial AAA+ Lon protease.

Clinical relevance of substitutions in the connection subdomain and RNase H domain of HIV-1 reverse transcriptase from a cohort of antiretroviral treatment-naïve patients

Crystal structure of HIV-1 reverse transcriptase in complex with a polypurine tract RNA:DNA

Cutting into the Substrate Dominance: Pharmacophore and Structure-Based Approaches toward Inhibiting Human Immunodeficiency Virus Reverse Transcriptase-Associated Ribonuclease H

Design of peptide-based inhibitors for human immunodeficiency virus type 1 strains resistant to T-20

Design, Synthesis, and Biological Evaluations of Hydroxypyridonecarboxylic Acids as Inhibitors of HIV Reverse Transcriptase Associated RNase H.

Design, synthesis, biochemical, and antiviral evaluations of C6 benzyl and C6 biarylmethyl substituted 2-hydroxylisoquinoline-1,3-diones: dual inhibition against HIV reverse transcriptase-associated RNase H and polymerase with antiviral activities

Determinants of Active-Site Inhibitor Interaction with HIV-1 RNase H

Development of a vaginal delivery film containing EFdA, a novel anti-HIV nucleoside reverse transcriptase inhibitor

Divergent evolution in reverse transcriptase (RT) of HIV-1 group O and M lineages: impact on structure, fitness, and sensitivity to nonnucleoside RT inhibitors.

Drug resistance in non-B subtype HIV-1: impact of HIV-1 reverse transcriptase inhibitors

Effect of mutations at position E138 in HIV-1 reverse transcriptase and their interactions with the M184I mutation on defining patterns of resistance to nonnucleoside reverse transcriptase inhibitors rilpivirine and etravirine

Effects of substitutions at the 4' and 2 positions on the bioactivity of 4'-ethynyl-2-fluoro-2'-deoxyadenosine

Evaluation of Combinations of 4'-Ethynyl-2-Fluoro-2'-Deoxyadenosine with Clinically Used Antiretroviral Drugs

Evaluation of SSYA10-001 as a replication inhibitor of severe acute respiratory syndrome, mouse hepatitis, and Middle East respiratory syndrome coronaviruses

Expression and purification of SARS coronavirus proteins using SUMO-fusions.

Expression, purification, and characterization of SARS coronavirus RNA polymerase.

Factors influencing the efficacy of rilpivirine in HIV-1 subtype C in low- and middle-income countries

Fast hepatitis C virus RNA elimination and NS5A redistribution by NS5A inhibitors studied by a multiplex assay approach

Future treatment strategies for novel Middle East respiratory syndrome coronavirus infection

Glutamine 151 participates in the substrate dNTP binding function of HIV-1 reverse transcriptase

HIV-1 resistance mechanism to an electrostatically constrained peptide fusion inhibitor that is active against T-20-resistant strains

Hypersusceptibility mechanism of Tenofovir-resistant HIV to EFdA.

Identification and characterization of coumestans as novel HCV NS5B polymerase inhibitors.

In vitro transport characteristics of EFdA, a novel nucleoside reverse transcriptase inhibitor using Caco-2 and MDCKII cell monolayers

Increased replication capacity following evolution of PYxE insertion in Gag-p6 is associated with enhanced virulence in HIV-1 subtype C from East Africa.

Inhibition of bacterial RNA polymerase by streptolydigin: stabilization of a straight-bridge-helix active-center conformation

Inhibitors of HIV-1 Reverse Transcriptase-Associated Ribonuclease H Activity

Inhibitors of foot and mouth disease virus targeting a novel pocket of the RNA-dependent RNA polymerase

Interactions of conformationally biased north and south 2'-fluoro-2', 3'-dideoxynucleoside 5'-triphosphates with the active site of HIV-1 reverse transcriptase.

K70Q adds high-level tenofovir resistance to "Q151M complex" HIV reverse transcriptase through the enhanced discrimination mechanism

Lamivudine (3TC) resistance in HIV-1 reverse transcriptase involves steric hindrance with beta-branched amino acids

Marine Natural Products as Leads against SARS-CoV-2 Infection

Mechanism of inhibition of HIV-1 reverse transcriptase by 4'-Ethynyl-2-fluoro-2'-deoxyadenosine triphosphate, a translocation-defective reverse transcriptase inhibitor.

Mechanism of interaction of human mitochondrial DNA polymerase γ with the novel nucleoside reverse transcriptase inhibitor 4'-ethynyl-2-fluoro-2'-deoxyadenosine indicates a low potential for host toxicity.

Mechanism of nucleic acid unwinding by SARS-CoV helicase.

Mechanism of resistance to S138A substituted enfuvirtide and its application to peptide design

Molecular biology: an HIV secret uncovered

Molecular model of SARS coronavirus polymerase: implications for biochemical functions and drug design

Multifunctionality of a picornavirus polymerase domain: nuclear localization signal and nucleotide recognition

Mutation of amino acids in the connection domain of human immunodeficiency virus type 1 reverse transcriptase that contact the template-primer affects RNase H activity.

Mutations in the 5′ End of the Human Immunodeficiency Virus Type 1 Polypurine Tract Affect RNase H Cleavage Specificity and Virus Titer ⬇️

Mutations in the RNase H domain of HIV-1 reverse transcriptase affect the initiation of DNA synthesis and the specificity of RNase H cleavage in vivo.

Novel Hepatitis B Virus Capsid-Targeting Antiviral That Aggregates Core Particles and Inhibits Nuclear Entry of Viral Cores

Nucleoside analog resistance caused by insertions in the fingers of human immunodeficiency virus type 1 reverse transcriptase involves ATP-mediated excision.

Oral administration of the nucleoside EFdA (4'-ethynyl-2-fluoro-2'-deoxyadenosine) provides rapid suppression of HIV viremia in humanized mice and favorable pharmacokinetic properties in mice and the rhesus macaque

Potent anti-HIV-1 activity of N-HR-derived peptides including a deep pocket-forming region without antagonistic effects on T-20

Preformulation studies of EFdA, a novel nucleoside reverse transcriptase inhibitor for HIV prevention

Probing the molecular mechanism of action of the HIV-1 reverse transcriptase inhibitor 4'-ethynyl-2-fluoro-2'-deoxyadenosine (EFdA) using pre-steady-state kinetics

Remembering Professor Walter A. Scott

Repeated exposure to 5D9, an inhibitor of 3D polymerase, effectively limits the replication of foot-and-mouth disease virus in host cells

Resistance profiles of novel electrostatically constrained HIV-1 fusion inhibitors

Response of simian immunodeficiency virus to the novel nucleoside reverse transcriptase inhibitor 4'-ethynyl-2-fluoro-2'-deoxyadenosine in vitro and in vivo

Restriction fragment mass polymorphism (RFMP) analysis based on MALDI-TOF mass spectrometry for detecting antiretroviral resistance in HIV-1 infected patients

Rev-derived peptides inhibit HIV-1 replication by antagonism of Rev and a co-receptor, CXCR4.

Reverse transcriptase in motion: conformational dynamics of enzyme-substrate interactions

Role of methionine 184 of human immunodeficiency virus type-1 reverse transcriptase in the polymerase function and fidelity of DNA synthesis.

SAMHD1 has differential impact on the efficacies of HIV nucleoside reverse transcriptase inhibitors.

SC29EK, a peptide fusion inhibitor with enhanced alpha-helicity, inhibits replication of human immunodeficiency virus type 1 mutants resistant to enfuvirtide

STRUCTURAL VIROLOGY. X-ray crystal structures of native HIV-1 capsid protein reveal conformational variability.

Selective excision of AZTMP by drug-resistant human immunodeficiency virus reverse transcriptase

Severe acute respiratory syndrome coronavirus replication inhibitor that interferes with the nucleic acid unwinding of the viral helicase

Similarities and differences in the RNase H activities of human immunodeficiency virus type 1 reverse transcriptase and Moloney murine leukemia virus reverse transcriptase.