List of works - Frederick S Buckner

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

scientific article published on 10 July 2017

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

scientific article

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

scientific article published on 31 July 2015

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

scientific article

A new chemotype with promise against Trypanosoma cruzi

scientific article published on 31 October 2019

Advances in Chagas disease drug development: 2009-2010

scientific article published on December 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

scientific article

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

scientific article

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

scientific article

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

scientific article

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

scientific article published on March 2007

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

scientific article

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

scientific article published on December 2003

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

scientific article

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

scientific article published in May 2005

Confirmation of Chagas' cardiomyopathy following heart transplantation

scientific article published on 29 September 2006

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

scientific article

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

scientific article

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

scientific article

Crystal structure of the aspartyl-tRNA synthetase from Entamoeba histolytica

scientific article

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

scientific article

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

scientific article

Crystal structures of three protozoan homologs of tryptophanyl-tRNA synthetase

scientific article

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

scientific article

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

scientific article

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

scientific article

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

scientific article

Differential drug binding by the highly conserved Plasmodium falciparum thymidylate synthase

scientific article published on 01 September 2005

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

scientific article

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

scientific article

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

scientific article

Experimental Chemotherapy and Approaches to Drug Discovery for Trypanosoma cruzi Infection ⬇️

scientific article published on January 1, 2011

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

scientific article

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

scientific article

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

scientific article

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

scientific article published on 21 July 2008

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

scientific article

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

scientific article published on 18 April 2006

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

scientific article

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

scientific article published on April 2009

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

scientific article

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

scientific article

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

scientific article published on December 2004

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

scientific article published on 15 April 2013

Induction of resistance to azole drugs in Trypanosoma cruzi

scientific article

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

scientific article

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

scientific article published on 13 October 2009

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

scientific article

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

scientific article

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

scientific article published on 18 April 2017

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

scientific article published in September 2005

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

scientific article published on July 2002

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

scientific article published on 03 February 2020

New Class of Antitrypanosomal Agents Based on Imidazopyridines

scientific article published on 27 June 2017

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

scientific article published on 27 March 2019

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

scientific article

Oxidosqualene cyclase inhibitors as antimicrobial agents.

scientific article

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

scientific article

Phenotypic Drug Discovery for Human African Trypanosomiasis: A Powerful Approach

scientific article published on 05 February 2020

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

scientific article

Prediction of protein crystallization outcome using a hybrid method

scientific article published on 27 March 2010

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

scientific article

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

scientific article

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

scientific article

Protein farnesyltransferase inhibitors exhibit potent antimalarial activity

scientific article

Protein geranylgeranyltransferase-I of Trypanosoma cruzi

scientific article

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

scientific article published on March 2009

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

scientific article published on December 2012

Recent developments in drug discovery for leishmaniasis and human African trypanosomiasis

scientific article

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

scientific article

Screening a fragment cocktail library using ultrafiltration

scientific article

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

scientific article

Second generation tetrahydroquinoline-based protein farnesyltransferase inhibitors as antimalarials

scientific article published on 28 August 2007

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

scientific article

Setting Our Sights on Infectious Diseases

scientific article published on 06 December 2019

Sterol 14-demethylase inhibitors for Trypanosoma cruzi infections.

scientific article published on January 2008

Structural genomics of pathogenic protozoa: an overview

scientific article

Structurally simple farnesyltransferase inhibitors arrest the growth of malaria parasites

scientific article published in August 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

scientific article

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

scientific article

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

scientific article

Structure of ribose 5-phosphate isomerase from Plasmodium falciparum

scientific article

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

scientific article

Structure of the prolyl-tRNA synthetase from the eukaryotic pathogen Giardia lamblia

scientific article

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

scientific article

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

scientific article

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

scientific article

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

scientific article

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

scientific article (publication date: July 2014)

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

scientific article published on 19 October 2020

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

scientific article

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

scientific article

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

scientific article published on 28 March 2018

The effects of protein farnesyltransferase inhibitors on trypanosomatids: inhibition of protein farnesylation and cell growth ⬇️

scientific article published on July 1, 1998

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

scientific article published on August 2005

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

scientific article

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

scientific article

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

scientific article

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

scientific article

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

scientific article published in November 2002

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

scientific article published on October 1, 1997

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

scientific article published on July 1, 1997

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

scientific article published in November 2005

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

scientific article published on 19 December 2016

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

scientific article

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

scientific article published in October 2006

List of works by Frederick S Buckner

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

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

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

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

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

A new chemotype with promise against Trypanosoma cruzi

Advances in Chagas disease drug development: 2009-2010

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

An essential farnesylated kinesin in Trypanosoma brucei

Bioactivity of Farnesyltransferase Inhibitors Against Entamoeba histolytica and Schistosoma mansoni

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

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

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

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

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

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

Cloning and analysis of Trypanosoma cruzi lanosterol 14alpha-demethylase

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

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

Confirmation of Chagas' cardiomyopathy following heart transplantation

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

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

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

Crystal structure of the aspartyl-tRNA synthetase from Entamoeba histolytica

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

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

Crystal structures of three protozoan homologs of tryptophanyl-tRNA synthetase

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

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

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

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

Differential drug binding by the highly conserved Plasmodium falciparum thymidylate synthase

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

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

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

Experimental Chemotherapy and Approaches to Drug Discovery for Trypanosoma cruzi Infection ⬇️

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

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

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

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

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

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

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

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

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

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

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

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

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

Induction of resistance to azole drugs in Trypanosoma cruzi

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

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

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

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

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

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

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

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

New Class of Antitrypanosomal Agents Based on Imidazopyridines

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

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

Oxidosqualene cyclase inhibitors as antimicrobial agents.

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

Phenotypic Drug Discovery for Human African Trypanosomiasis: A Powerful Approach

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

Prediction of protein crystallization outcome using a hybrid method

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

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

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

Protein farnesyltransferase inhibitors exhibit potent antimalarial activity

Protein geranylgeranyltransferase-I of Trypanosoma cruzi

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

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

Recent developments in drug discovery for leishmaniasis and human African trypanosomiasis

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

Screening a fragment cocktail library using ultrafiltration

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

Second generation tetrahydroquinoline-based protein farnesyltransferase inhibitors as antimalarials

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