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1-Benzyl-3-aryl-2-thiohydantoin Derivatives as New Anti-Trypanosoma brucei Agents: SAR and in Vivo Efficacy

artículo científico publicado en 2017

5-Fluoroimidazo[4,5-b]pyridine Is a Privileged Fragment That Conveys Bioavailability to Potent Trypanosomal Methionyl-tRNA Synthetase Inhibitors

artículo científico publicado en 2016

A 71-year-old man with recurrent pulmonary mycobacterial avium complex infections and lymphopenia

scientific article published on 01 January 2020

A binding hotspot in Trypanosoma cruzi histidyl-tRNA synthetase revealed by fragment-based crystallographic cocktail screens

artículo científico publicado en 2015

A class of sterol 14-demethylase inhibitors as anti-Trypanosoma cruzi agents.

artículo científico publicado en 2003

A new chemotype with promise against Trypanosoma cruzi

scientific article published on 31 October 2019

Advances in Chagas disease drug development: 2009-2010

artículo científico publicado en 2010

Altered sterol profile induced in Leishmania amazonensis by a natural dihydroxymethoxylated chalcone.

scientific article published on 28 January 2009

An essential farnesylated kinesin in Trypanosoma brucei

artículo científico publicado en 2011

Bioactivity of Farnesyltransferase Inhibitors Against Entamoeba histolytica and Schistosoma mansoni

scientific article published on 29 May 2019

Bioisosteric transformations and permutations in the triazolopyrimidine scaffold to identify the minimum pharmacophore required for inhibitory activity against Plasmodium falciparum dihydroorotate dehydrogenase

artículo científico publicado en 2012

Brucella melitensis Methionyl-tRNA-Synthetase (MetRS), a Potential Drug Target for Brucellosis

artículo científico publicado en 2016

Buffer optimization of thermal melt assays of Plasmodium proteins for detection of small-molecule ligands

artículo científico publicado en 2009

C-terminal proteolysis of prenylated proteins in trypanosomatids and RNA interference of enzymes required for the post-translational processing pathway of farnesylated proteins

artículo científico publicado en 2007

Characterization of Trypanosoma brucei dihydroorotate dehydrogenase as a possible drug target; structural, kinetic and RNAi studies

artículo científico publicado en 2008

Clinical Features and Outcomes of 105 Hospitalized patients with COVID-19 in Seattle, Washington

scientific article published on 22 May 2020

Cloning and analysis of Trypanosoma cruzi lanosterol 14alpha-demethylase

artículo científico publicado en 2003

Cloning, heterologous expression, and substrate specificities of protein farnesyltransferases from Trypanosoma cruzi and Leishmania major

artículo científico publicado en 2002

Colorimetric assay for screening compounds against Leishmania amastigotes grown in macrophages.

artículo científico publicado en 2005

Confirmation of Chagas' cardiomyopathy following heart transplantation

artículo científico publicado en 2006

Correction: Brucella melitensis Methionyl-tRNA-Synthetase (MetRS), a Potential Drug Target for Brucellosis

artículo científico publicado en 2016

Crystal Structures of Trypanosomal Histidyl-tRNA Synthetase Illuminate Differences between Eukaryotic and Prokaryotic Homologs

artículo científico publicado en 2010

Crystal structure of glyceraldehyde-3-phosphate dehydrogenase from Plasmodium falciparum at 2.25 A resolution reveals intriguing extra electron density in the active site.

artículo científico publicado en 2006

Crystal structure of the aspartyl-tRNA synthetase from Entamoeba histolytica

artículo científico publicado en 2010

Crystal structures and proposed structural/functional classification of three protozoan proteins from the isochorismatase superfamily.

artículo científico publicado en 2005

Crystal structures of Plasmodium falciparum cytosolic tryptophanyl-tRNA synthetase and its potential as a target for structure-guided drug design

artículo científico publicado en 2013

Crystal structures of three protozoan homologs of tryptophanyl-tRNA synthetase

artículo científico publicado en 2011

Delusional parasitosis: six-year experience with 23 consecutive cases at an academic medical center

artículo científico publicado en 2009

Design and synthesis of peptidomimetic protein farnesyltransferase inhibitors as anti-Trypanosoma brucei agents.

artículo científico publicado en 2004

Development of methionyl-tRNA synthetase inhibitors as antibiotics for Gram-positive bacterial infections.

artículo científico publicado en 2017

Dialkylimidazole inhibitors of Trypanosoma cruzi sterol 14α-demethylase as anti-Chagas disease agents

artículo científico publicado en 2013

Differential drug binding by the highly conserved Plasmodium falciparum thymidylate synthase

artículo científico publicado en 2005

Discovery of N-(2-aminoethyl)-N-benzyloxyphenyl benzamides: New potent Trypanosoma brucei inhibitors

artículo científico publicado en 2016

Distinct States of Methionyl-tRNA Synthetase Indicate Inhibitor Binding by Conformational Selection

artículo científico publicado en 2012

Efficacy, Pharmacokinetics, and Metabolism of Tetrahydroquinoline Inhibitors of Plasmodium falciparum Protein Farnesyltransferase

artículo científico publicado en 2007

Experimental Chemotherapy and Approaches to Drug Discovery for Trypanosoma cruzi Infection

artículo científico publicado el 1 de enero de 2011

Fragment-based cocktail crystallography by the medical structural genomics of pathogenic protozoa consortium

artículo científico publicado en 2009

From Cells to Mice to Target: Characterization of NEU-1053 (SB-443342) and Its Analogues for Treatment of Human African Trypanosomiasis.

artículo científico publicado en 2017

Genomic-scale prioritization of drug targets: the TDR Targets database

artículo científico publicado en 2008

Glycogen synthase kinase 3 is a potential drug target for African trypanosomiasis therapy

artículo científico publicado en 2008

Heterologous expression of L. major proteins in S. cerevisiae: a test of solubility, purity, and gene recoding.

artículo científico publicado en 2009

Heterologous expression of proteins from Plasmodium falciparum: results from 1000 genes

artículo científico publicado en 2006

High-throughput screening of amastigotes of Leishmania donovani clinical isolates against drugs using a colorimetric beta-lactamase assay

artículo científico publicado en 2009

Hydroxychloroquine for treatment of SARS-CoV-2 infection? Improving our confidence in a model-based approach to dose selection

scientific article published on 08 April 2020

Identification of a metabolically stable triazolopyrimidine-based dihydroorotate dehydrogenase inhibitor with antimalarial activity in mice

artículo científico publicado en 2009

Identification of potent inhibitors of the Trypanosoma brucei methionyl-tRNA synthetase via high-throughput orthogonal screening.

artículo científico publicado en 2014

Identification of three classes of heteroaromatic compounds with activity against intracellular Trypanosoma cruzi by chemical library screening

artículo científico publicado en 2009

In vitro and in vivo antimalarial activity of peptidomimetic protein farnesyltransferase inhibitors with improved membrane permeability

artículo científico publicado en 2004

Induced resistance to methionyl-tRNA synthetase inhibitors in Trypanosoma brucei is due to overexpression of the target.

artículo científico publicado en 2013

Induction of resistance to azole drugs in Trypanosoma cruzi

artículo científico publicado en 1998

Inhibitors of methionyl-tRNA synthetase have potent activity against Giardia intestinalis trophozoites

artículo científico publicado en 2015

Isoquinoline-based analogs of the cancer drug clinical candidate tipifarnib as anti-Trypanosoma cruzi agents

artículo científico publicado en 2009

Isothiazole dioxides: synthesis and inhibition of Trypanosoma brucei protein farnesyltransferase.

artículo científico publicado en 2002

Lead optimization of aryl and aralkyl amine-based triazolopyrimidine inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase with antimalarial activity in mice

artículo científico publicado en 2011

Leishmania donovani tyrosyl-tRNA synthetase structure in complex with a tyrosyl adenylate analog and comparisons with human and protozoan counterparts

artículo científico publicado en 2017

Leishmania inactivation in human pheresis platelets by a psoralen (amotosalen HCl) and long-wavelength ultraviolet irradiation.

artículo científico publicado en 2005

Leishmania major activates IL-1 alpha expression in macrophages through a MyD88-dependent pathway

artículo científico publicado en 2002

Methionyl-tRNA synthetase inhibitor has potent in vivo activity in a novel Giardia lamblia luciferase murine infection model

artículo científico publicado en 2020

New Class of Antitrypanosomal Agents Based on Imidazopyridines

artículo científico publicado en 2017

Optimization of Methionyl tRNA-Synthetase Inhibitors for Treatment of Cryptosporidium Infection

artículo científico publicado en 2019

Optimization of a binding fragment targeting the "enlarged methionine pocket" leads to potent Trypanosoma brucei methionyl-tRNA synthetase inhibitors.

artículo científico publicado en 2017

Oxidosqualene cyclase inhibitors as antimicrobial agents.

artículo científico publicado en 2003

Pharmacological Characterization, Structural Studies, and In Vivo Activities of Anti-Chagas Disease Lead Compounds Derived from Tipifarnib

artículo científico publicado en 2012

Phenotypic Drug Discovery for Human African Trypanosomiasis: A Powerful Approach

artículo científico publicado en 2020

Potent, Plasmodium-selective farnesyltransferase inhibitors that arrest the growth of malaria parasites: structure-activity relationships of ethylenediamine-analogue scaffolds and homology model validation.

artículo científico publicado en 2008

Prediction of protein crystallization outcome using a hybrid method

artículo científico publicado en 2010

Proteasome inhibition for treatment of leishmaniasis, Chagas disease and sleeping sickness

artículo científico publicado en 2016

Protein farnesyl and N-myristoyl transferases: piggy-back medicinal chemistry targets for the development of antitrypanosomatid and antimalarial therapeutics.

artículo científico publicado en 2003

Protein farnesyl transferase inhibitors for the treatment of malaria and African trypanosomiasis.

artículo científico publicado en 2005

Protein farnesyltransferase inhibitors exhibit potent antimalarial activity

artículo científico publicado en 2005

Protein geranylgeranyltransferase-I of Trypanosoma cruzi

artículo científico publicado en 2007

Rational modification of a candidate cancer drug for use against Chagas disease

artículo científico publicado en 2009

Recent Developments in Sterol 14-demethylase Inhibitors for Chagas Disease.

artículo científico publicado en 2012

Recent developments in drug discovery for leishmaniasis and human African trypanosomiasis

artículo científico publicado en 2014

Recent highlights in anti-protozoan drug development and resistance research.

artículo científico publicado en 2012

Screening a fragment cocktail library using ultrafiltration

artículo científico publicado en 2011

Second generation analogues of the cancer drug clinical candidate tipifarnib for anti-Chagas disease drug discovery.

artículo científico publicado en 2010

Second generation tetrahydroquinoline-based protein farnesyltransferase inhibitors as antimalarials

artículo científico publicado en 2007

Selective inhibitors of methionyl-tRNA synthetase have potent activity against Trypanosoma brucei Infection in Mice

artículo científico publicado en 2011

Setting Our Sights on Infectious Diseases

scientific article published on 06 December 2019

Sterol 14-demethylase inhibitors for Trypanosoma cruzi infections.

artículo científico publicado en 2008

Structural genomics of pathogenic protozoa: an overview

artículo científico publicado en 2008

Structurally simple farnesyltransferase inhibitors arrest the growth of malaria parasites

artículo científico publicado en 2005

Structurally simple inhibitors of lanosterol 14alpha-demethylase are efficacious in a rodent model of acute Chagas disease.

scientific article published on June 2009

Structurally simple, potent, Plasmodium selective farnesyltransferase inhibitors that arrest the growth of malaria parasites

scientific article published on September 2006

Structure of Leishmania major methionyl-tRNA synthetase in complex with intermediate products methionyladenylate and pyrophosphate

artículo científico publicado en 2011

Structure of a ribulose 5-phosphate 3-epimerase from Plasmodium falciparum

artículo científico publicado en 2006

Structure of aTrypanosoma bruceiα/β-hydrolase fold protein with unknown function

artículo científico publicado en 2008

Structure of ribose 5-phosphate isomerase from Plasmodium falciparum

artículo científico publicado en 2006

Structure of the conserved hypothetical protein MAL13P1.257 from Plasmodium falciparum

artículo científico publicado en 2006

Structure of the prolyl-tRNA synthetase from the eukaryotic pathogenGiardia lamblia

artículo científico publicado en 2012

Structure-guided design of novel Trypanosoma brucei Methionyl-tRNA synthetase inhibitors.

artículo científico publicado en 2016

Structures of Substrate- and Inhibitor-Bound Adenosine Deaminase from a Human Malaria Parasite Show a Dramatic Conformational Change and Shed Light on Drug Selectivity

artículo científico publicado en 2008

Structures of Trypanosoma brucei methionyl-tRNA synthetase with urea-based inhibitors provide guidance for drug design against sleeping sickness

artículo científico publicado en 2014

Substituted 2-phenylimidazopyridines: a new class of drug leads for human African trypanosomiasis

artículo científico publicado en 2014

Synergy testing of FDA-approved drugs identifies potent drug combinations against Trypanosoma cruzi

artículo científico publicado en 2014

Synthesis and structure-activity relationships of imidazopyridine/pyrimidine- and furopyridine-based anti-infective agents against trypanosomiases

artículo científico publicado en 2020

The Crystal Structure and Activity of a Putative Trypanosomal Nucleoside Phosphorylase Reveal It to be a Homodimeric Uridine Phosphorylase

artículo científico publicado en 2010

The Double-Length Tyrosyl-tRNA Synthetase from the Eukaryote Leishmania major Forms an Intrinsically Asymmetric Pseudo-Dimer

artículo científico publicado en 2011

The crystal structure of the drug target Mycobacterium tuberculosis methionyl-tRNA synthetase in complex with a catalytic intermediate.

artículo científico publicado en 2018

The protein farnesyltransferase inhibitor Tipifarnib as a new lead for the development of drugs against Chagas disease

artículo científico publicado en 2005

The structure of Plasmodium vivax phosphatidylethanolamine-binding protein suggests a functional motif containing a left-handed helix

artículo científico publicado en 2007

The structure of tryptophanyl-tRNA synthetase from Giardia lamblia reveals divergence from eukaryotic homologs

artículo científico publicado en 2010

Thematic review series: lipid posttranslational modifications. Fighting parasitic disease by blocking protein farnesylation

artículo científico publicado en 2006

Toxoplasma gondii calcium-dependent protein kinase 1 is a target for selective kinase inhibitors

artículo científico publicado en 2010

Triazolopyrimidines and Imidazopyridines: Structure-Activity Relationships and in Vivo Efficacy for Trypanosomiasis

scientific article published on 04 December 2018

Trypanosoma brucei prenylated-protein carboxyl methyltransferase prefers farnesylated substrates

artículo científico publicado en 2002

Trypanosoma cruzi infection does not impair major histocompatibility complex class I presentation of antigen to cytotoxic T lymphocytes

artículo científico publicado el 1 de octubre de 1997

Trypanosoma cruzi:Use of Herpes Simplex Virus–Thymidine Kinase as a Negative Selectable Marker

artículo científico publicado el 1 de julio de 1997

Upregulation of sterol C14-demethylase expression in Trypanosoma cruzi treated with sterol biosynthesis inhibitors.

artículo científico publicado en 2005

Urea Derivatives of 2-Aryl-benzothiazol-5-amines: A New Class of Potential Drugs for Human African Trypanosomiasis

artículo científico publicado en 2016

Urea-based inhibitors of Trypanosoma brucei methionyl-tRNA synthetase: selectivity and in vivo characterization.

artículo científico publicado en 2012

Using Fragment Cocktail Crystallography To Assist Inhibitor Design ofTrypanosoma bruceiNucleoside 2-Deoxyribosyltransferase†

artículo científico publicado en 2006