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List of works by Tomáš Cihlář

539. GS-CA2: A Novel, Potent, and Selective First-In-class Inhibitor of HIV-1 Capsid Function Displays Nonclinical Pharmacokinetics Supporting Long-Acting Potential in Humans

article

6-(Het)aryl-7-deazapurine ribonucleosides as novel potent cytostatic agents

scientific article

A highly potent long-acting small-molecule HIV-1 capsid inhibitor with efficacy in a humanized mouse model

scientific article published on 09 September 2019

A nanoluciferase SARS-CoV-2 for rapid neutralization testing and screening of anti-infective drugs for COVID-19

scientific article published on 23 June 2020

A novel and efficient one-pot synthesis of symmetrical diamide (bis-amidate) prodrugs of acyclic nucleoside phosphonates and evaluation of their biological activities

scientific article published on 23 May 2011

A pharmacogenetic candidate gene study of tenofovir-associated Fanconi syndrome.

scientific article

Abyssomicin 2 reactivates latent HIV-1 by a PKC- and HDAC-independent mechanism ⬇️

scientific article published on 5 January 2015

Accelerating Drug Development: Antiviral Therapies for Emerging Viruses as a Model.

scientific article published on 22 July 2016

Activation of 9-[(R)-2-[[(S)-[[(S)-1-(Isopropoxycarbonyl)ethyl]amino] phenoxyphosphinyl]-methoxy]propyl]adenine (GS-7340) and other tenofovir phosphonoamidate prodrugs by human proteases

scientific article published on 22 April 2008

Antiviral Activity of Bictegravir (GS-9883), a Novel Potent HIV-1 Integrase Strand Transfer Inhibitor with an Improved Resistance Profile

scientific article

Antiviral Efficacy of a Respiratory Syncytial Virus (RSV) Fusion Inhibitor in a Bovine Model of RSV Infection

scientific article published on 8 June 2015

Assessment of mitochondrial toxicity in human cells treated with tenofovir: comparison with other nucleoside reverse transcriptase inhibitors

scientific article

Blood biomarkers of expressed and inducible HIV-1.

scientific article published on 13 January 2018

Broad spectrum antiviral remdesivir inhibits human endemic and zoonotic deltacoronaviruses with a highly divergent RNA dependent RNA polymerase

scientific article published in September 2019

Broad-spectrum Investigational Agent GS-5734 for the Treatment of Ebola, MERS Coronavirus and Other Pathogenic Viral Infections with High Outbreak Potential.

scientific article published on 4 October 2017

Broad-spectrum antiviral GS-5734 inhibits both epidemic and zoonotic coronaviruses.

scientific article

Cathepsin A is the major hydrolase catalyzing the intracellular hydrolysis of the antiretroviral nucleotide phosphonoamidate prodrugs GS-7340 and GS-9131.

scientific article published on 4 December 2006

Characterization of Ebola Virus Disease (EVD) in Rhesus Monkeys for Development of EVD Therapeutics

scientific article published on 13 January 2020

Chronic administration of tenofovir to rhesus macaques from infancy through adulthood and pregnancy: summary of pharmacokinetics and biological and virological effects.

scientific article published on 23 June 2008

Clinical benefit of remdesivir in rhesus macaques infected with SARS-CoV-2

scientific article published on 16 April 2020

Clinical benefit of remdesivir in rhesus macaques infected with SARS-CoV-2

scientific article published on 09 June 2020

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

scientific article published on 01 July 2020

Comparative therapeutic efficacy of remdesivir and combination lopinavir, ritonavir, and interferon beta against MERS-CoV

scientific article published on 10 January 2020

Contribution of the organic anion transporter OAT2 to the renal active tubular secretion of creatinine and mechanism for serum creatinine elevations caused by cobicistat

scientific article

Coronavirus Susceptibility to the Antiviral Remdesivir (GS-5734) Is Mediated by the Viral Polymerase and the Proofreading Exoribonuclease

scientific article

Current status and challenges of antiretroviral research and therapy

scientific article published on 16 December 2009

Current status and prospects of HIV treatment

scientific article

Design and profiling of GS-9148, a novel nucleotide analog active against nucleoside-resistant variants of human immunodeficiency virus type 1, and its orally bioavailable phosphonoamidate prodrug, GS-9131.

scientific article

Design, synthesis, and anti-HIV activity of 4'-modified carbocyclic nucleoside phosphonate reverse transcriptase inhibitors.

scientific article

Discovery and Synthesis of a Phosphoramidate Prodrug of a Pyrrolo[2,1-f][triazin-4-amino] Adenine C-Nucleoside (GS-5734) for the Treatment of Ebola and Emerging Viruses

scientific article published on 26 January 2017

Discovery of GS-9131: Design, synthesis and optimization of amidate prodrugs of the novel nucleoside phosphonate HIV reverse transcriptase (RT) inhibitor GS-9148.

scientific article published on 27 March 2010

Discovery of an oral respiratory syncytial virus (RSV) fusion inhibitor (GS-5806) and clinical proof of concept in a human RSV challenge study

scientific article published on 27 January 2015

Drug resistance assessment following administration of RSV fusion inhibitor presatovir to participants experimentally infected with respiratory syncytial virus

scientific article published on 23 January 2020

Evaluation of the effect of cobicistat on the in vitro renal transport and cytotoxicity potential of tenofovir.

scientific article published on 29 July 2013

GS-5734 and its parent nucleoside analog inhibit Filo-, Pneumo-, and Paramyxoviruses

scientific article

GS-5806 Inhibits a Broad Range of Respiratory Syncytial Virus Clinical Isolates by Blocking the Virus-Cell Fusion Process

scientific article

GS-8374, a novel HIV protease inhibitor, does not alter glucose homeostasis in cultured adipocytes or in a healthy-rodent model system.

scientific article

GS-9219--a novel acyclic nucleotide analogue with potent antineoplastic activity in dogs with spontaneous non-Hodgkin's lymphoma

scientific article

Histone deacetylase inhibitor romidepsin induces HIV expression in CD4 T cells from patients on suppressive antiretroviral therapy at concentrations achieved by clinical dosing

scientific article

Human respiratory syncytial virus Memphis 37 grown in HEp-2 cells causes more severe disease in lambs than virus grown in Vero cells

scientific article

Human respiratory syncytial virus memphis 37 causes acute respiratory disease in perinatal lamb lung

scientific article published on April 2014

Identification of NK Cell Subpopulations That Differentiate HIV-Infected Subject Cohorts with Diverse Levels of Virus Control

scientific article published on 21 March 2019

In vitro characterization of GS-8374, a novel phosphonate-containing inhibitor of HIV-1 protease with a favorable resistance profile

scientific article published on 18 January 2011

In vitro cytotoxicity and mitochondrial toxicity of tenofovir alone and in combination with other antiretrovirals in human renal proximal tubule cells

scientific article

Inhibition of Respiratory Syncytial Virus Fusion by the Small Molecule VP-14637 via Specific Interactions with F Protein ⬇️

scientific article published on May 1, 2003

Inhibition of the human organic anion transporter 1 by the caffeine metabolite 1-methylxanthine

scientific article

Intracellular Activation of Tenofovir Alafenamide and the Effect of Viral and Host Protease Inhibitors

scientific article published on 26 October 2015

Intracellular metabolism of the nucleotide prodrug GS-9131, a potent anti-human immunodeficiency virus agent

scientific article published on 3 December 2007

Mechanism of active renal tubular efflux of tenofovir

scientific article

Metabolism and antiretroviral activity of tenofovir alafenamide in CD4+ T-cells and macrophages from demographically diverse donors

scientific article published on 14 March 2014

Molecular assessment of the potential for renal drug interactions between tenofovir and HIV protease inhibitors.

scientific article published in January 2007

Multiple classes of antiviral agents exhibit in vitro activity against human rhinovirus type C

scientific article

Mutations in adenosine deaminase-like (ADAL) protein confer resistance to the antiproliferative agents N6-cyclopropyl-PMEDAP and GS-9219.

scientific article published on May 2013

Mutations in multiple domains of Gag drive the emergence of in vitro resistance to the phosphonate-containing HIV-1 protease inhibitor GS-8374.

scientific article published on 24 October 2012

Non-catalytic site HIV-1 integrase inhibitors disrupt core maturation and induce a reverse transcription block in target cells

scientific article (publication date: 2013)

Novel nucleotide human immunodeficiency virus reverse transcriptase inhibitor GS-9148 with a low nephrotoxic potential: characterization of renal transport and accumulation.

scientific article

Novel targets for HIV therapy

scientific article

Nucleoside and nucleotide HIV reverse transcriptase inhibitors: 25 years after zidovudine.

scientific article

Nucleotide HIV reverse transcriptase inhibitors: tenofovir and beyond

scientific article published on September 2006

Prophylactic and therapeutic remdesivir (GS-5734) treatment in the rhesus macaque model of MERS-CoV infection

scientific article published on 13 February 2020

Quantitative microscopy of functional HIV post-entry complexes reveals association of replication with the viral capsid

scientific article published on 17 December 2014

Rapid In Vitro Evaluation of Antiretroviral Barrier to Resistance at Therapeutic Drug Levels

scientific article published on 29 June 2016

Remdesivir (GS-5734) protects African green monkeys from Nipah virus challenge

scientific article published on 01 May 2019

Remdesivir Inhibits SARS-CoV-2 in Human Lung Cells and Chimeric SARS-CoV Expressing the SARS-CoV-2 RNA Polymerase in Mice

scientific article published on 07 July 2020

Remdesivir potently inhibits SARS-CoV-2 in human lung cells and chimeric SARS-CoV expressing the SARS-CoV-2 RNA polymerase in mice

scientific article published on 28 April 2020

Role of cathepsin A and lysosomes in the intracellular activation of novel antipapillomavirus agent GS-9191.

scientific article

Search for small molecule activators of latent HIV.

scientific article published on 25 May 2012

Selective intracellular activation of a novel prodrug of the human immunodeficiency virus reverse transcriptase inhibitor tenofovir leads to preferential distribution and accumulation in lymphatic tissue

scientific article

Small molecules VP-14637 and JNJ-2408068 inhibit respiratory syncytial virus fusion by similar mechanisms

scientific article

Study of marine natural products including resorcyclic acid lactones from Humicola fuscoatra that reactivate latent HIV-1 expression in an in vitro model of central memory CD4+ T cells ⬇️

scientific article

Suppression of HIV-1 protease inhibitor resistance by phosphonate-mediated solvent anchoring

scientific article published on 02 August 2006

Synthesis and anti-HIV activity of 2'-fluorine modified nucleoside phosphonates: analogs of GS-9148.

scientific article

Synthesis and anti-HIV activity of GS-9148 (2'-Fd4AP), a novel nucleoside phosphonate HIV reverse transcriptase inhibitor

scientific article published on 5 December 2007

Synthesis and anti-HIV activity of cyclic pyrimidine phosphonomethoxy nucleosides and their prodrugs: a comparison of phosphonates and corresponding nucleosides

scientific article published in January 2007

Synthesis and significant cytostatic activity of 7-hetaryl-7-deazaadenosines

scientific article published on 11 July 2011

Synthesis of ester prodrugs of 9-(S)-[3-hydroxy-2-(phosphonomethoxy)propyl]-2,6-diaminopurine (HPMPDAP) as anti-poxvirus agents

scientific article published on October 2010

Synthesis, anti-HIV activity, and resistance profile of thymidine phosphonomethoxy nucleosides and their bis-isopropyloxymethylcarbonyl (bisPOC) prodrugs

scientific article

Synthesis, anti-HIV activity, and resistance profiles of ribose modified nucleoside phosphonates

scientific article published on 17 October 2007

TLR7 Agonist GS-9620 Is a Potent Inhibitor of Acute HIV-1 Infection in Human Peripheral Blood Mononuclear Cells

scientific article published on 31 October 2016

TLR7 agonists induce transient viremia and reduce the viral reservoir in SIV-infected rhesus macaques on antiretroviral therapy.

scientific article

Targeting HIV Reservoir in Infected CD4 T Cells by Dual-Affinity Re-targeting Molecules (DARTs) that Bind HIV Envelope and Recruit Cytotoxic T Cells

scientific article published on 5 November 2015

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

scientific article published on 25 January 2017

Tenofovir alafenamide is not a substrate for renal organic anion transporters (OATs) and does not exhibit OAT-dependent cytotoxicity

scientific article published on 4 April 2014

Tenofovir exhibits low cytotoxicity in various human cell types: comparison with other nucleoside reverse transcriptase inhibitors.

scientific article published on April 2002

The anti-influenza drug oseltamivir exhibits low potential to induce pharmacokinetic drug interactions via renal secretion-correlation of in vivo and in vitro studies.

scientific article

Therapeutic efficacy of the small molecule GS-5734 against Ebola virus in rhesus monkeys

scientific article

Toll-Like Receptor 7 Agonist GS-9620 Induces HIV Expression and HIV-Specific Immunity in Cells from HIV-Infected Individuals on Suppressive Antiretroviral Therapy

scientific article

Topical tenofovir, a microbicide effective against HIV, inhibits herpes simplex virus-2 replication

scientific article

Unlikely association of multidrug-resistance protein 2 single-nucleotide polymorphisms with tenofovir-induced renal adverse events

scientific article published on 01 May 2007

Visualizing the molecular interactions of a nucleotide analog, GS-9148, with HIV-1 reverse transcriptase-DNA complex

scientific article

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