C. Callebaut

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Antiviral Activity of Tenofovir Alafenamide against HIV-1 with Thymidine Analog-Associated Mutations and M184V

R. Haubrich, Renee R Ram, M. Abram, 2020, Antimicrobial Agents and Chemotherapy.

Evolution of tenofovir‐resistant HIV‐1 isolates exposed to tenofovir alafenamide dose escalation

Michael D. Miller, Renee R Ram, N. Margot, 2017, Antiviral research.

Inhibition of HIV infection by the cytokine midkine.

S. Nisole, J. Briand, A. Hovanessian, 2001, Virology.

The V3 loop-mimicking pseudopeptide 5[Kpsi(CH2N)PR]-TASP inhibits HIV infection in primary macrophage cultures.

S. Nisole, S. Muller, J. Briand, 1999, AIDS research and human retroviruses.

Measurement of plasma HIV-1 RNA below the limit of quantification (<20 copies/mL) of commercial assays with the integrase HIV RNA single-copy assay.

J. Mellors, N. Margot, C. Callebaut, 2018, Journal of Clinical Virology.

Specific and irreversible cyclopeptide inhibitors of dipeptidyl peptidase IV activity of the T-cell activation antigen CD26.

J. Blanco, E. Jacotot, A. Hovanessian, 1998, Journal of medicinal chemistry.

Further characterization of DPP IV-beta, a novel cell surface expressed protein with dipeptidyl peptidase activity.

J. Blanco, E. Jacotot, A. Hovanessian, 1997, Advances in experimental medicine and biology.

Dipeptidyl-peptidase IV-beta, a novel form of cell-surface-expressed protein with dipeptidyl-peptidase IV activity.

J. Blanco, E. Jacotot, A. Hovanessian, 1996, European journal of biochemistry.

GS-8374 , a novel HIV protease inhibitor , 1 does not alter glucose homeostasis in cultured adipocytes 2 or in a healthy rodent model system 3 4 5

P. Hruz, J. Koster, Luong K. Tsai, 2011 .

Efficacy of oral tenofovir alafenamide/emtricitabine combination or single agent tenofovir alafenamide against vaginal SHIV infection in macaques.

W. Heneine, J. Rooney, Yeojin Park, 2019, The Journal of infectious diseases.

HIV Drug Therapy in the Americas 16–18 April 2015, Mexico City, Mexico

M. Lederman, D. Podzamczer, D. Kuritzkes, 2015, Journal of the International AIDS Society.

Antiviral Activity, Safety, and Pharmacokinetics/Pharmacodynamics of Tenofovir Alafenamide as 10-Day Monotherapy in HIV-1–Positive Adults

U. Bredeek, P. Ruane, D. Berger, 2013, Journal of acquired immune deficiency syndromes.

Cobicistat versus ritonavir as a pharmacoenhancer of atazanavir plus emtricitabine/tenofovir disoproxil fumarate in treatment-naive HIV type 1-infected patients: week 48 results.

F. Antunes, J. Gallant, J. Fehr, 2013, The Journal of infectious diseases.

Evaluation of Broadly Neutralizing Antibody Sensitivity by Genotyping and Phenotyping for Qualifying Participants to HIV Clinical Trials

H. Günthard, H. Kuster, R. Geleziunas, 2021, Journal of acquired immune deficiency syndromes.

Brief Report: Randomized, Double-Blind Comparison of Tenofovir Alafenamide (TAF) vs Tenofovir Disoproxil Fumarate (TDF), Each Coformulated With Elvitegravir, Cobicistat, and Emtricitabine (E/C/F) for Initial HIV-1 Treatment Week 144 Results

P. Sax, M. Das, A. Clarke, 2017, Journal of acquired immune deficiency syndromes.

Brief Report: A Randomized, Double-Blind Comparison of Tenofovir Alafenamide Versus Tenofovir Disoproxil Fumarate, Each Coformulated With Elvitegravir, Cobicistat, and Emtricitabine for Initial HIV-1 Treatment: Week 96 Results

K. Tashima, P. Sax, M. Das, 2016, Journal of acquired immune deficiency syndromes.

Identification of V3 Loop-binding Proteins as Potential Receptors Implicated in the Binding of HIV Particles to CD4+Cells*

E. Dam, J. Blanco, S. Muller, 1998, The Journal of Biological Chemistry.

CD26 as a positive regulator of HIV envelope-glycoprotein induced apoptosis in CD4+ T cells.

J. Blanco, E. Jacotot, Y. Rivière, 1997, Advances in experimental medicine and biology.

Commonly Transmitted HIV-1 Drug Resistance Mutations in Reverse Transcriptase and Protease in Antiretroviral Treatment-Naïve Patients do not Affect Response to Tenofovir Disoproxil Fumarate- or Tenofovir Alafenamide-Containing Regimens.

K. White, D. Porter, Pamela Wong, 2017, The Journal of infectious diseases.

Human Immunodeficiency Virus Fusion to Dendritic Cells Declines as Cells Mature

W. Greene, J. Kreisberg, M. Cavrois, 2006, Journal of Virology.

The anti-HIV pentameric pseudopeptide HB-19 is preferentially taken up in vivo by lymphoid organs where it forms a complex with nucleolin

E. Jacotot, J. Briand, C. Rougeot, 2001, Proceedings of the National Academy of Sciences of the United States of America.

Pre-Clinical Evaluation of Tenofovir and Tenofovir Alafenamide for HIV-1 Pre-Exposure Prophylaxis in Foreskin Tissue

S. Khoo, C. Herrera, N. Martinson, 2022, Pharmaceutics.

HIV & Hepatitis in the Americas 28–30 April 2016, Mexico City, Mexico

N. Volkow, K. Tashima, D. Podzamczer, 2016, Journal of the International AIDS Society.

T cell activation antigen, CD26, as a cofactor for entry of HIV in CD4+ cells.

E. Jacotot, A. Hovanessian, C. Callebaut, 1993, Science.

Pseudopeptide TASP Inhibitors of HIV Entry Bind Specifically to a 95-kDa Cell Surface Protein*

E. Jacotot, J. Briand, G. Guichard, 1997, The Journal of Biological Chemistry.

Regulation of epithelial and lymphocyte cell adhesion by adenosine deaminase-CD26 interaction.

J. Mallol, C. Lluis, R. Franco, 2002, The Biochemical journal.

Inhibition of entry of HIV into cells by poly(A).poly(U).

A. Hovanessian, C. Callebaut, B. Krust, 1993, AIDS research and human retroviruses.

Selective loss of the CD4+/CD26+ T-cell subset during HIV infection.

L. Montagnier, E. Jacotot, H. Lecoeur, 1996, Research in immunology.

Adenosine deaminase binding to human CD26 is inhibited by HIV-1 envelope glycoprotein gp120 and viral particles.

C. Lluis, R. Franco, J. Blanco, 1997, Journal of immunology.

Dipeptidyl‐peptidase IV‐β

J. Blanco, E. Jacotot, A. Hovanessian, 1998 .

Intracellular Metabolism of the Nucleotide Prodrug GS-9131, a Potent Anti-Human Immunodeficiency Virus Agent

R. Mackman, T. Cihlar, K. Lin, 2007, Antimicrobial Agents and Chemotherapy.

Tenofovir alafenamide (TAF) does not deplete mitochondrial DNA in human T-cell lines at intracellular concentrations exceeding clinically relevant drug exposures.

T. Cihlar, Kirsten M. Stray, A. Ray, 2017, Antiviral research.

High resistance barrier to tenofovir alafenamide is driven by higher loading of tenofovir diphosphate into target cells compared to tenofovir disoproxil fumarate.

Yang Liu, N. Margot, C. Callebaut, 2016, Antiviral research.

In Vitro Virology Profile of Tenofovir Alafenamide, a Novel Oral Prodrug of Tenofovir with Improved Antiviral Activity Compared to That of Tenofovir Disoproxil Fumarate

G. Stepan, Ya-Wen Tian, C. Callebaut, 2015, Antimicrobial Agents and Chemotherapy.

Two-dose emtricitabine/tenofovir alafenamide plus bictegravir prophylaxis protects macaques against SHIV infection

M. Das, T. Cihlar, D. Barouch, 2020, The Journal of antimicrobial chemotherapy.

Viability of primary osteoblasts after treatment with tenofovir alafenamide: Lack of cytotoxicity at clinically relevant drug concentrations

K. Kitrinos, A. Ray, D. Babusis, 2017, PloS one.

A Randomized, Open-Label Trial to Evaluate Switching to Elvitegravir/Cobicistat/Emtricitabine/Tenofovir Alafenamide Plus Darunavir in Treatment-Experienced HIV-1-Infected Adults

J. Gallant, M. Das, P. Tebas, 2017, Journal of acquired immune deficiency syndromes.

Absence of Lenacapavir (GS-6207) Phenotypic Resistance in HIV Gag Cleavage Site Mutants and in Isolates with Resistance to Existing Drug Classes

M. Rhee, Renee R Ram, N. Margot, 2020, Antimicrobial Agents and Chemotherapy.

A Cell-Based Strategy To Assess Intrinsic Inhibition Efficiencies of HIV-1 Reverse Transcriptase Inhibitors

K. White, M. Tsiang, M. Abram, 2014, Antimicrobial Agents and Chemotherapy.

P100 Tenofovir alafenamide (TAF) in a single tablet regimen in initial HIV-1 therapy

D. Podzamczer, D. Wohl, J. Molina, 2015, Sexually Transmitted Infections.

The level of CD26 determines the rate of HIV entry in a CD4+ T-cell line.

J. Blanco, E. Jacotot, A. Hovanessian, 1997, Advances in experimental medicine and biology.

Recent Epidemiological Changes in Infectious Diseases

K. Bush, A. Cathcart, M. Pucci, 2017 .

Discovery of GS-8374, a potent human immunodeficiency virus type 1 protease inhibitor with a superior resistance profile

William A. Lee, M. Hatada, M. Desai, 2011 .

Cobicistat (GS-9350): A Potent and Selective Inhibitor of Human CYP3A as a Novel Pharmacoenhancer.

Yujin Wang, Manoj C Desai, M. Desai, 2010, ACS medicinal chemistry letters.

Structure-activity relationships of diamine inhibitors of cytochrome P450 (CYP) 3A as novel pharmacoenhancers, part I: core region.

M. Desai, Luong K. Tsai, Kirsten M. Stray, 2014, Bioorganic & medicinal chemistry letters.

Tenofovir alafenamide versus tenofovir disoproxil fumarate, coformulated with elvitegravir, cobicistat, and emtricitabine, for initial treatment of HIV-1 infection: two randomised, double-blind, phase 3, non-inferiority trials

D. Podzamczer, P. Sax, M. Saag, 2015, The Lancet.

Characterization of HIV-1 Resistance to Tenofovir Alafenamide In Vitro

N. Margot, C. Callebaut, Audun Johnson, 2015, Antimicrobial Agents and Chemotherapy.

Tenofovir Alafenamide Vs. Tenofovir Disoproxil Fumarate in Single Tablet Regimens for Initial HIV-1 Therapy: A Randomized Phase 2 Study

P. Sax, A. Zolopa, F. Post, 2014, Journal of acquired immune deficiency syndromes.

Commonly Transmitted HIV-1 Drug Resistance Mutations in Reverse-Transcriptase and Protease in Antiretroviral Treatment–Naive Patients and Response to Regimens Containing Tenofovir Disoproxil Fumarate or Tenofovir Alafenamide

K. White, D. Porter, Pamela Wong, 2017, The Journal of infectious diseases.

Rare emergence of drug resistance in HIV-1 treatment -naïve patients after 48 weeks of treatment with elvitegravir/cobicistat/emtricitabine/tenofovir alafenamide

K. Kitrinos, M. Fordyce, N. Margot, 2016, HIV clinical trials.

Lenacapavir: a first-in-class HIV-1 capsid inhibitor.

H. Dvory‐Sobol, N. Shaik, M. Rhee, 2022, Current opinion in HIV and AIDS.

Clinical targeting of HIV capsid protein with a long-acting small molecule

J. R. Somoza, W. Sundquist, Xiaohong Liu, 2020, Nature.

Resistance analyses in Highly Treatment-Experienced People with HIV Treated with the Novel Capsid HIV Inhibitor Lenacapavir.

H. Dvory‐Sobol, M. Rhee, N. Margot, 2022, The Journal of infectious diseases.

Frequency of capsid substitutions associated with GS-6207 in vitro resistance in HIV-1 from antiretroviral-naive and -experienced patients.

V. Calvez, C. Charpentier, D. Descamps, 2020, The Journal of antimicrobial chemotherapy.

Tenofovir Alafenamide Versus Tenofovir Disoproxil Fumarate in the First Protease Inhibitor–Based Single-Tablet Regimen for Initial HIV-1 Therapy: A Randomized Phase 2 Study

M. Saag, M. Das, J. Flamm, 2015, Journal of Acquired Immune Deficiency Syndromes.

HIV-1 envelope glycoproteins-mediated apoptosis is regulated by CD4 dependent and independent mechanisms

J. Blanco, E. Jacotot, A. Hovanessian, 2004, Apoptosis.

Antiviral activity of HIV‐1 integrase strand‐transfer inhibitors against mutants with integrase resistance‐associated mutations and their frequency in treatment‐naïve individuals

K. White, M. Abram, N. Margot, 2019, Journal of medical virology.

CD8+-Cell Antiviral Factor Activity Is Not Restricted to Human Immunodeficiency Virus (HIV)-Specific T Cells and Can Block HIV Replication after Initiation of Reverse Transcription

Y. Rivière, Steven P Lee, S. Le Borgne, 2000, Journal of Virology.

Evaluation of HIV-1 reservoir size and broadly neutralizing antibody susceptibility in acute antiretroviral therapy-treated individuals

M. Kozal, H. Günthard, S. Little, 2021, AIDS.

Long-acting capsid inhibitor protects macaques from repeat SHIV challenges

R. Geleziunas, S. Yant, T. Cihlar, 2021, Nature.

73. Interim Resistance Analysis of Long-Acting Lenacapavir in Treatment-Naïve People with HIV at 28 Weeks

H. Dvory‐Sobol, Ross Martin, M. Rhee, 2021, Open Forum Infectious Diseases.

International Congress of Drug Therapy in HIV Infection 23-26 October 2016, Glasgow, UK

Raúl Tabarés Gutiérrez, Samit R. Joshi, H. Jessen, 2016, Journal of the International AIDS Society.

Increased rate of HIV-1 entry and its cytopathic effect in CD4+/CXCR4+ T cells expressing relatively high levels of CD26.

J. Blanco, E. Jacotot, A. Hovanessian, 1998, Experimental cell research.

GS-8374, a Novel HIV Protease Inhibitor, Does Not Alter Glucose Homeostasis in Cultured Adipocytes or in a Healthy-Rodent Model System

P. Hruz, J. Koster, Luong K. Tsai, 2011, Antimicrobial Agents and Chemotherapy.

The Anti-HIV Pseudopeptide HB-19 Forms a Complex with the Cell-surface-expressed Nucleolin Independent of Heparan Sulfate Proteoglycans*

S. Nisole, J. Briand, G. Guichard, 1999, The Journal of Biological Chemistry.

The HB-19 pseudopeptide 5[Kpsi(CH2N)PR]-TASP inhibits attachment of T lymophocyte- and macrophage-tropic HIV to permissive cells.

E. Dam, S. Nisole, S. Muller, 2000, AIDS research and human retroviruses.

HIV envelope glycoprotein-induced cell killing by apoptosis is enhanced with increased expression of CD26 in CD4+ T cells.

J. Blanco, E. Jacotot, Y. Rivière, 1996, Virology.

Emtricitabine and tenofovir alafenamide vs emtricitabine and tenofovir disoproxil fumarate for HIV pre-exposure prophylaxis (DISCOVER): primary results from a randomised, double-blind, multicentre, active-controlled, phase 3, non-inferiority trial

H. Jessen, R. Grant, K. Mounzer, 2020, The Lancet.

Differential detection of M184V/I between plasma historical HIV genotypes and HIV proviral DNA from PBMCs.

R. Haubrich, I. Mcnicholl, N. Margot, 2020, The Journal of antimicrobial chemotherapy.

Lack of impact of pre-existing T97A HIV-1 integrase mutation on integrase strand transfer inhibitor resistance and treatment outcome

K. White, M. Abram, N. Margot, 2017, PloS one.

HIV-1 envelope gp120 and viral particles block adenosine deaminase binding to human CD26.

C. Lluis, R. Franco, J. Blanco, 1997, Advances in experimental medicine and biology.

In Vitro Characterization of GS-8374, a Novel Phosphonate-Containing Inhibitor of HIV-1 Protease with a Favorable Resistance Profile

William A. Lee, M. Hatada, Xiaohong Liu, 2011, Antimicrobial Agents and Chemotherapy.

Virological Outcomes of EVG/COBI/FTC/TDF and EVG/COBI/FTC/TAF in Antiretroviral-Naive HIV-1-Infected Participants with Baseline HIV-1 RNA ≥1,000,000 Copies/ml: A Post Hoc Analysis of Phase III Clinical Trials

K. White, P. Sax, M. Das, 2018, Antiviral therapy.

Mutations in Multiple Domains of Gag Drive the Emergence of In Vitro Resistance to the Phosphonate-Containing HIV-1 Protease Inhibitor GS-8374

H. Kräusslich, B. Müller, B. Glass, 2012, Journal of Virology.

Activation of HIV-Specific CD8+ T-cells from HIV+ Donors by Vesatolimod

R. Geleziunas, J. Hesselgesser, M. Abram, 2020, Antiviral therapy.

Antiviral activity of tenofovir alafenamide (TAF) against HIV‐1 clinical isolates harboring K65R

N. Margot, C. Callebaut, S. Cox, 2023, Journal of medical virology.

Rare emergence of drug resistance in HIV-1 treatment-naïve patients receiving elvitegravir/cobicistat/emtricitabine/tenofovir alafenamide for 144 weeks.

M. Das, N. Margot, C. Callebaut, 2018, Journal of clinical virology : the official publication of the Pan American Society for Clinical Virology.

Dose finding study for on-demand HIV pre-exposure prophylaxis for insertive sex in sub-Saharan Africa: results from the CHAPS open label randomised controlled trial

J. Seeley, P. Kaleebu, S. Khoo, 2023, EBioMedicine.

Specific binding of adenosine deaminase but not HIV-1 transactivator protein Tat to human CD26.

J. Blanco, E. Jacotot, A. Hovanessian, 1996, Experimental cell research.

Dipeptidyl-peptidase IV-beta--further characterization and comparison to dipeptidyl-peptidase IV activity of CD26.

J. Blanco, E. Jacotot, A. Hovanessian, 1998, European journal of biochemistry.

55Biological Profiling of GS-9350, a Novel Pharmacoenhancer that Lacks Anti-HIV Activity and Exhibits Low Potential for Metabolic Adverse Effects In Vitro

M. Desai, Luong K. Tsai, T. Cihlar, 2010 .

Infrequent Development of Drug Resistance in HIV-1-Infected Treatment-Naive Subjects after 96 Weeks of Treatment with Elvitegravir/Cobicistat/Emtricitabine/Tenofovir Alafenamide or Elvitegravir/Cobicistat/ Emtricitabine/Tenofovir Disoproxil Fumarate

M. Das, N. Margot, C. Callebaut, 2017, Antiviral therapy.

Phenotypic resistance to lenacapavir and monotherapy efficacy in a proof-of-concept clinical study.

Ross Martin, M. Rhee, N. Margot, 2022, The Journal of antimicrobial chemotherapy.

Long-acting lenacapavir acts as an effective preexposure prophylaxis in a rectal SHIV challenge macaque model

S. Yant, Elena Bekerman, Derek Hansen, 2023, The Journal of clinical investigation.

Inhibition of HIV infection by pseudopeptides blocking viral envelope glycoprotein-mediated membrane fusion and cell death.

J. Blanco, S. Muller, E. Jacotot, 1996, Virology.

A Cell-Based Strategy To Assess Intrinsic Inhibition Efficiencies of HIV-1 Reverse Transcriptase Inhibitors

K. White, M. Tsiang, M. Abram, 2014, Antimicrobial Agents and Chemotherapy.

D. Podzamczer, P. Sax, M. Saag, 2015, The Lancet.

Cobicistat versus ritonavir as a pharmacoenhancer of atazanavir plus emtricitabine/tenofovir disoproxil fumarate in treatment-naive HIV type 1-infected patients: week 48 results.

F. Antunes, J. Gallant, J. Fehr, 2013, The Journal of infectious diseases.

Structure-activity relationships of diamine inhibitors of cytochrome P450 (CYP) 3A as novel pharmacoenhancers. Part II: P2/P3 region and discovery of cobicistat (GS-9350).

M. Desai, Luong K. Tsai, S. Swaminathan, 2014, Bioorganic & medicinal chemistry letters.