List of works - Thomas H. Keller

A fluorescence quenching assay to discriminate between specific and nonspecific inhibitors of dengue virus protease.

scientific article

A new orally bioavailable dual adenosine A2B/A3 receptor antagonist with therapeutic potential.

scientific article published in June 2005

A practical view of 'druggability'.

scientific article published on 30 June 2006

A small-molecule dengue virus entry inhibitor

scientific article

A translation inhibitor that suppresses dengue virus in vitro and in vivo

scientific article

An adenosine nucleoside inhibitor of dengue virus

scientific article

Anti-infectives: can cellular screening deliver?

scientific article

Artificial Neural Network Analysis of Pharmacokinetic and Toxicity Properties of Lead Molecules for Dengue Fever, Tuberculosis and Malaria.

scientific article

Biophysical Studies of Bacterial Topoisomerases Substantiate Their Binding Modes to an Inhibitor

scientific article published on November 2015

Characterization of the interaction between Escherichia coli topoisomerase IV E subunit and an ATP competitive inhibitor

scientific article

Correction to "Discovery of Irreversible Inhibitors Targeting Histone Methyltransferase, SMYD3"

scientific article published on 09 July 2019

Corrections to Structure−Activity Relationships of Antitubercular Nitroimidazoles. 2. Determinants of Aerobic Activity and Quantitative Structure−Activity Relationships

article published in 2009

Development of isoform selective PI3-kinase inhibitors as pharmacological tools for elucidating the PI3K pathway

scientific article published on 17 July 2012

Discovery and Optimization of 4-(8-(3-Fluorophenyl)-1,7-naphthyridin-6-yl)transcyclohexanecarboxylic Acid, an Improved PDE4 Inhibitor for the Treatment of Chronic Obstructive Pulmonary Disease (COPD)

scientific article published on 28 August 2015

Discovery and Optimization of a Porcupine Inhibitor

scientific article published on 16 July 2015

Discovery of Irreversible Inhibitors Targeting Histone Methyltransferase, SMYD3

scientific article published on 23 May 2019

Discovery of dual GyrB/ParE inhibitors active against Gram-negative bacteria

scientific article published on 11 August 2018

Drug design for flavivirus proteases: what are we missing?

scientific article published on January 2014

Exploring the binding of peptidic West Nile virus NS2B-NS3 protease inhibitors by NMR.

scientific article published on 2 December 2012

Fragment-Based Drug Discovery of Potent Protein Kinase C Iota Inhibitors.

scientific article published on 4 May 2018

Fragment-based Discovery of a Small-Molecule Protein Kinase C-iota Inhibitor Binding Post-kinase Domain Residues

scientific article published on 15 February 2019

Fragment-based ligand design of novel potent inhibitors of tankyrases

scientific article

Global Bayesian models for the prioritization of antitubercular agents

scientific article

Imidazolopiperazines: hit to lead optimization of new antimalarial agents.

scientific article published on 23 June 2011

Impact of non-profit organizations on drug discovery: opportunities, gaps, solutions.

scientific article published on April 2008

Inhibition of dengue virus RNA synthesis by an adenosine nucleoside

scientific article

Inhibition of dengue virus by an ester prodrug of an adenosine analog

scientific article

Inhibition of dengue virus polymerase by blocking of the RNA tunnel

scientific article

Mechanistic study of the spiroindolones: a new class of antimalarials.

scientific article published on 24 August 2012

N-sulfonylanthranilic acid derivatives as allosteric inhibitors of dengue viral RNA-dependent RNA polymerase

scientific article published on December 2009

NMR analysis of a novel enzymatically active unlinked dengue NS2B-NS3 protease complex

scientific article published on 19 March 2013

NMR structural characterization of the N-terminal active domain of the gyrase B subunit fromPseudomonas aeruginosaand its complex with an inhibitor

article

New highly potent and selective adenosine A(3) receptor antagonists.

scientific article published in January 2004

PA-824 kills nonreplicating Mycobacterium tuberculosis by intracellular NO release

scientific article

Peptide inhibitors of Dengue virus NS3 protease. Part 1: Warhead

scientific article published on 21 October 2005

Peptide inhibitors of dengue virus NS3 protease. Part 2: SAR study of tetrapeptide aldehyde inhibitors.

scientific article published on 21 October 2005

Peptidomimetic ethyl propenoate covalent inhibitors of the enterovirus 71 3C protease: a P2-P4 study.

scientific article published on 20 March 2015

Pharmacological profile of PKF242-484 and PKF241-466, novel dual inhibitors of TNF-alpha converting enzyme and matrix metalloproteinases, in models of airway inflammation

scientific article

Pharmacophore Model for Wnt/Porcupine Inhibitors and Its Use in Drug Design

scientific article published on 15 June 2015

Potent and selective xanthine-based inhibitors of phosphodiesterase 5

scientific article published on 10 November 2006

Probing the specificity of the S1 binding site of subtilisin Carlsberg with boronic acids

scientific article published on 01 April 1991

Probing the specificity of the S1 binding site of subtilisin Carlsberg with boronic acids

scientific article published on 01 January 1994

Scaffold Hopping and Optimization of Maleimide Based Porcupine Inhibitors.

scientific article

Small Molecule Inhibitors That Selectively Block Dengue Virus Methyltransferase

scientific article

Solubility-driven optimization of phosphodiesterase-4 inhibitors leading to a clinical candidate

scientific article published on 30 August 2012

Spiroindolones, a potent compound class for the treatment of malaria

scientific article

Spirotetrahydro beta-carbolines (spiroindolones): a new class of potent and orally efficacious compounds for the treatment of malaria.

scientific article published on July 2010

State of the art technologies in drug discovery 2011

scientific article published on 21 July 2011

Structural and Functional Analyses of an Allosteric EYA2 Phosphatase Inhibitor That Has On-Target Effects in Human Lung Cancer Cells

scientific article published on 08 July 2019

Structural basis for the activation of flaviviral NS3 proteases from dengue and West Nile virus.

scientific article

Structure-Activity Relationship Studies of Mitogen Activated Protein Kinase Interacting Kinase (MNK) 1 and 2 and BCR-ABL1 Inhibitors Targeting Chronic Myeloid Leukemic Cells.

scientific article

Structure-activity relationships of antitubercular nitroimidazoles. 1. Structural features associated with aerobic and anaerobic activities of 4- and 5-nitroimidazoles

scientific article published on March 2009

Structure-activity relationships of antitubercular nitroimidazoles. 2. Determinants of aerobic activity and quantitative structure-activity relationships

scientific article published on March 2009

Structure-activity relationships of antitubercular nitroimidazoles. 3. Exploration of the linker and lipophilic tail of ((s)-2-nitro-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazin-6-yl)-(4-trifluoromethoxybenzyl)amine (6-amino PA-824).

scientific article

Synthesis and antitubercular activity of 7-(R)- and 7-(S)-methyl-2-nitro-6-(S)-(4-(trifluoromethoxy)benzyloxy)-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazines, analogues of PA-824.

scientific article published on 7 March 2008

Synthesis and structure-activity relationship of N-arylrolipram derivatives as inhibitors of PDE4 isozymes.

scientific article published in August 2001

The importance of molecular complexity in the design of screening libraries.

scientific article

The use of porcupine inhibitors to target Wnt-driven cancers.

scientific article

Wnt addiction of genetically defined cancers reversed by PORCN inhibition

scientific article

Yellow fever virus NS3 protease: peptide-inhibition studies.

scientific article published on August 2007

Zika Virus Protease: An Antiviral Drug Target

scientific article published on 05 August 2017

List of works by Thomas H. Keller

A fluorescence quenching assay to discriminate between specific and nonspecific inhibitors of dengue virus protease.

A new orally bioavailable dual adenosine A2B/A3 receptor antagonist with therapeutic potential.

A practical view of 'druggability'.

A small-molecule dengue virus entry inhibitor

A translation inhibitor that suppresses dengue virus in vitro and in vivo

An adenosine nucleoside inhibitor of dengue virus

Anti-infectives: can cellular screening deliver?

Artificial Neural Network Analysis of Pharmacokinetic and Toxicity Properties of Lead Molecules for Dengue Fever, Tuberculosis and Malaria.

Biophysical Studies of Bacterial Topoisomerases Substantiate Their Binding Modes to an Inhibitor

Characterization of the interaction between Escherichia coli topoisomerase IV E subunit and an ATP competitive inhibitor

Correction to "Discovery of Irreversible Inhibitors Targeting Histone Methyltransferase, SMYD3"

Corrections to Structure−Activity Relationships of Antitubercular Nitroimidazoles. 2. Determinants of Aerobic Activity and Quantitative Structure−Activity Relationships

Development of isoform selective PI3-kinase inhibitors as pharmacological tools for elucidating the PI3K pathway

Discovery and Optimization of 4-(8-(3-Fluorophenyl)-1,7-naphthyridin-6-yl)transcyclohexanecarboxylic Acid, an Improved PDE4 Inhibitor for the Treatment of Chronic Obstructive Pulmonary Disease (COPD)

Discovery and Optimization of a Porcupine Inhibitor

Discovery of Irreversible Inhibitors Targeting Histone Methyltransferase, SMYD3

Discovery of dual GyrB/ParE inhibitors active against Gram-negative bacteria

Drug design for flavivirus proteases: what are we missing?

Exploring the binding of peptidic West Nile virus NS2B-NS3 protease inhibitors by NMR.

Fragment-Based Drug Discovery of Potent Protein Kinase C Iota Inhibitors.

Fragment-based Discovery of a Small-Molecule Protein Kinase C-iota Inhibitor Binding Post-kinase Domain Residues

Fragment-based ligand design of novel potent inhibitors of tankyrases

Global Bayesian models for the prioritization of antitubercular agents

Imidazolopiperazines: hit to lead optimization of new antimalarial agents.

Impact of non-profit organizations on drug discovery: opportunities, gaps, solutions.

Inhibition of dengue virus RNA synthesis by an adenosine nucleoside

Inhibition of dengue virus by an ester prodrug of an adenosine analog

Inhibition of dengue virus polymerase by blocking of the RNA tunnel

Mechanistic study of the spiroindolones: a new class of antimalarials.

N-sulfonylanthranilic acid derivatives as allosteric inhibitors of dengue viral RNA-dependent RNA polymerase

NMR analysis of a novel enzymatically active unlinked dengue NS2B-NS3 protease complex

NMR structural characterization of the N-terminal active domain of the gyrase B subunit fromPseudomonas aeruginosaand its complex with an inhibitor

New highly potent and selective adenosine A(3) receptor antagonists.

PA-824 kills nonreplicating Mycobacterium tuberculosis by intracellular NO release

Peptide inhibitors of Dengue virus NS3 protease. Part 1: Warhead

Peptide inhibitors of dengue virus NS3 protease. Part 2: SAR study of tetrapeptide aldehyde inhibitors.

Peptidomimetic ethyl propenoate covalent inhibitors of the enterovirus 71 3C protease: a P2-P4 study.

Pharmacological profile of PKF242-484 and PKF241-466, novel dual inhibitors of TNF-alpha converting enzyme and matrix metalloproteinases, in models of airway inflammation

Pharmacophore Model for Wnt/Porcupine Inhibitors and Its Use in Drug Design

Potent and selective xanthine-based inhibitors of phosphodiesterase 5

Probing the specificity of the S1 binding site of subtilisin Carlsberg with boronic acids

Probing the specificity of the S1 binding site of subtilisin Carlsberg with boronic acids

Scaffold Hopping and Optimization of Maleimide Based Porcupine Inhibitors.

Small Molecule Inhibitors That Selectively Block Dengue Virus Methyltransferase

Solubility-driven optimization of phosphodiesterase-4 inhibitors leading to a clinical candidate

Spiroindolones, a potent compound class for the treatment of malaria

Spirotetrahydro beta-carbolines (spiroindolones): a new class of potent and orally efficacious compounds for the treatment of malaria.

State of the art technologies in drug discovery 2011

Structural and Functional Analyses of an Allosteric EYA2 Phosphatase Inhibitor That Has On-Target Effects in Human Lung Cancer Cells

Structural basis for the activation of flaviviral NS3 proteases from dengue and West Nile virus.

Structure-Activity Relationship Studies of Mitogen Activated Protein Kinase Interacting Kinase (MNK) 1 and 2 and BCR-ABL1 Inhibitors Targeting Chronic Myeloid Leukemic Cells.

Structure-activity relationships of antitubercular nitroimidazoles. 1. Structural features associated with aerobic and anaerobic activities of 4- and 5-nitroimidazoles

Structure-activity relationships of antitubercular nitroimidazoles. 2. Determinants of aerobic activity and quantitative structure-activity relationships

Structure-activity relationships of antitubercular nitroimidazoles. 3. Exploration of the linker and lipophilic tail of ((s)-2-nitro-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazin-6-yl)-(4-trifluoromethoxybenzyl)amine (6-amino PA-824).

Synthesis and antitubercular activity of 7-(R)- and 7-(S)-methyl-2-nitro-6-(S)-(4-(trifluoromethoxy)benzyloxy)-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazines, analogues of PA-824.

Synthesis and structure-activity relationship of N-arylrolipram derivatives as inhibitors of PDE4 isozymes.

The importance of molecular complexity in the design of screening libraries.

The use of porcupine inhibitors to target Wnt-driven cancers.

Wnt addiction of genetically defined cancers reversed by PORCN inhibition

Yellow fever virus NS3 protease: peptide-inhibition studies.

Zika Virus Protease: An Antiviral Drug Target