Lista de obras - Thomas H. Keller - Dominio Público Uruguay

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

artículo científico publicado en 2009

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

artículo científico publicado en 2005

A practical view of 'druggability'.

artículo científico publicado en 2006

A small-molecule dengue virus entry inhibitor

artículo científico publicado en 2009

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

artículo científico publicado en 2011

An adenosine nucleoside inhibitor of dengue virus

artículo científico publicado en 2009

Anti-infectives: can cellular screening deliver?

artículo científico publicado en 2011

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

artículo científico publicado en 2016

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

artículo científico publicado en 2015

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

artículo científico publicado en 2015

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

Design and synthesis of a library of chemokine antagonists ⬇️

artículo científico publicado el 10 de septiembre de 2011

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

artículo científico publicado en 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)

artículo científico publicado en 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

artículo científico publicado en 2018

Drug Design For Flavivirus Proteases: What Are We Missing? ⬇️

artículo científico publicado el 1 de enero de 2014

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

artículo científico publicado en 2012

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

artículo científico publicado en 2018

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

artículo científico publicado en 2019

Fragment-based ligand design of novel potent inhibitors of tankyrases

artículo científico publicado en 2013

Global Bayesian models for the prioritization of antitubercular agents

artículo científico publicado en 2008

Imidazolopiperazines: hit to lead optimization of new antimalarial agents.

artículo científico publicado en 2011

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

scientific article published on April 2008

Indium mediated allylation in peptide and protein functionalization ⬇️

artículo científico publicado el 14 de julio de 2011

Inhibition of dengue virus RNA synthesis by an adenosine nucleoside

artículo científico publicado en 2010

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

artículo científico publicado en 2010

Inhibition of dengue virus polymerase by blocking of the RNA tunnel

artículo científico publicado en 2010

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

artículo científico publicado en 2012

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

artículo científico publicado en 2009

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

artículo científico publicado en 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.

artículo científico publicado en 2004

PA-824 kills nonreplicating Mycobacterium tuberculosis by intracellular NO release

artículo científico publicado en 2008

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

artículo científico publicado en 2005

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

artículo científico publicado en 2005

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

artículo científico publicado en 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

artículo científico publicado en 2002

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

artículo científico publicado en 2015

Potent and selective xanthine-based inhibitors of phosphodiesterase 5

artículo científico publicado en 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.

artículo científico publicado en 2017

Small Molecule Inhibitors That Selectively Block Dengue Virus Methyltransferase

artículo científico publicado en 2011

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

artículo científico publicado en 2010

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

artículo científico publicado en 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.

artículo científico publicado en 2006

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

artículo científico publicado en 2016

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

artículo científico publicado en 2009

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

artículo científico publicado en 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).

artículo científico publicado en 2011

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.

artículo científico publicado en 2008

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

artículo científico publicado en 2001

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

artículo científico publicado en 2013

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

artículo científico publicado en 2015

Wnt addiction of genetically defined cancers reversed by PORCN inhibition

artículo científico publicado en 2015

Yellow fever virus NS3 protease: peptide-inhibition studies.

artículo científico publicado en 2007

Zika Virus Protease: An Antiviral Drug Target

artículo científico

Lista de obras de 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

Design and synthesis of a library of chemokine antagonists ⬇️

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.

Indium mediated allylation in peptide and protein functionalization ⬇️

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