List of works - Margaret A. Phillips

A Gateway® compatible vector for gene silencing in bloodstream form Trypanosoma brucei

scientific article

A Teach-Discover-Treat Application of ZincPharmer: An Online Interactive Pharmacophore Modeling and Virtual Screening Tool

scientific article

A dual regulatory circuit consisting of S-adenosylmethionine decarboxylase protein and its reaction product controls expression of the paralogous activator prozyme in Trypanosoma brucei

scientific article published on 26 October 2018

A long-duration dihydroorotate dehydrogenase inhibitor (DSM265) for prevention and treatment of malaria

scientific article

A multiple aminoacyl-tRNA synthetase complex that enhances tRNA-aminoacylation in African trypanosomes

scientific article published on 14 October 2013

A triazolopyrimidine-based dihydroorotate dehydrogenase inhibitor (DSM421) with improved drug-like properties for treatment and prevention of malaria

scientific article (publication date: 9 December 2016)

Advanced molecular design of biopolymers for transmucosal and intracellular delivery of chemotherapeutic agents and biological therapeutics

scientific article

Allosteric activation of trypanosomatid deoxyhypusine synthase by a catalytically dead paralog

scientific journal article

Allosteric regulation of an essential trypanosome polyamine biosynthetic enzyme by a catalytically dead homolog

scholarly article

Alternative pathways utilize or circumvent putrescine for biosynthesis of putrescine-containing rhizoferrin

scientific article published on 04 December 2020

Alternative spermidine biosynthetic route is critical for growth of Campylobacter jejuni and is the dominant polyamine pathway in human gut microbiota

scientific article

An alternative polyamine biosynthetic pathway is widespread in bacteria and essential for biofilm formation in Vibrio cholerae

scientific article

Analysis of flavin oxidation and electron-transfer inhibition in Plasmodium falciparum dihydroorotate dehydrogenase

scientific article

Anticancer properties of distinct antimalarial drug classes

scientific article (publication date: 2013)

Antimalarial activity of single-dose DSM265, a novel plasmodium dihydroorotate dehydrogenase inhibitor, in patients with uncomplicated Plasmodium falciparum or Plasmodium vivax malaria infection: a proof-of-concept, open-label, phase 2a study

article

Asexual populations of the human malaria parasite, Plasmodium falciparum, use a two-step genomic strategy to acquire accurate, beneficial DNA amplifications

scientific article

Assessing drug efficacy against Plasmodium falciparum liver stages in vivo

scientific article published on 11 January 2018

Atovaquone tolerance in Plasmodium falciparum parasites selected for high-level resistance to a dihydroorotate dehydrogenase inhibitor

scientific article published on 20 October 2014

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

scientific article

Cellular evaluation of synthesized insulin/transferrin bioconjugates for oral insulin delivery using intelligent complexation hydrogels

scientific article

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

scientific article

Chemical genetics of Plasmodium falciparum

scientific article (publication date: 20 May 2010)

Cross-species activation of trypanosome S-adenosylmethionine decarboxylase by the regulatory subunit prozyme

scientific article published on 10 June 2009

Deoxyhypusine Modification of Eukaryotic Translation Initiation Factor 5A (eIF5A) Is Essential for Trypanosoma brucei Growth and for Expression of Polyprolyl-containing Proteins

scientific article published on 16 June 2015

Detergent-dependent kinetics of truncated Plasmodium falciparum dihydroorotate dehydrogenase.

scientific article published on 28 February 2007

Discovery of new S-adenosylmethionine decarboxylase inhibitors for the treatment of Human African Trypanosomiasis (HAT).

scientific article published on 24 April 2009

Discovery of potent and selective inhibitors of Trypanosoma brucei ornithine decarboxylase

scientific article

Evaluation of Antigens for Development of a Serological Test for Human African Trypanosomiasis

scientific article

Evolution and multifarious horizontal transfer of an alternative biosynthetic pathway for the alternative polyamine sym-homospermidine

scientific article

Evolution of Substrate Specificity within a Diverse Family of / -Barrel-fold Basic Amino Acid Decarboxylases: X-RAY STRUCTURE DETERMINATION OF ENZYMES WITH SPECIFICITY FOR L-ARGININE AND CARBOXYNORSPERMIDINE

scientific article

Fluorine Modulates Species Selectivity in the Triazolopyrimidine Class of Plasmodium falciparum Dihydroorotate Dehydrogenase Inhibitors

scientific article

GMP synthase is essential for viability and infectivity of Trypanosoma brucei despite a redundant purine salvage pathway.

scientific article

Genetic validation of Trypanosoma brucei glutathione synthetase as an essential enzyme

scientific article

Genetic validation of aminoacyl-tRNA synthetases as drug targets in Trypanosoma brucei

scientific article published on 21 February 2014

High-throughput screening for potent and selective inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase

scientific article

Identification and Assay of Allosteric Regulators of S-Adenosylmethionine Decarboxylase ⬇️

scientific article published on 01 January 2011

Identification and mechanistic understanding of dihydroorotate dehydrogenase point mutations in Plasmodium falciparum that confer in vitro resistance to the clinical candidate DSM265

scientific article published on 13 November 2018

Identification of New Human Malaria Parasite Plasmodium falciparum Dihydroorotate Dehydrogenase Inhibitors by Pharmacophore and Structure-Based Virtual Screening

scientific article published on 25 February 2016

Identification of Trypanosoma brucei AdoMetDC Inhibitors Using a High-Throughput Mass Spectrometry-Based Assay.

scientific article published on 28 March 2017

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

scientific article published on April 2009

Improved Synthesis of MDL 73811 - a Potent AdoMetDC Inhibitor and Anti-Trypanosomal Compound

scientific article published on July 2016

Inhibition of pyrimidine synthesis reverses viral virulence factor-mediated block of mRNA nuclear export

scientific article published on February 2012

Isoxazolopyrimidine-Based Inhibitors of Dihydroorotate Dehydrogenase with Antimalarial Activity

Lead Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series for the Treatment of Malaria

scientific article published on 06 April 2020

Lead optimization of 3-carboxyl-4(1H)-quinolones to deliver orally bioavailable antimalarials

scientific article

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

scientific article

Malaria

scholarly article by Margaret A. Phillips et al published 3 August 2017 in Nature Reviews Disease Primers

Malarial dihydroorotate dehydrogenase. Substrate and inhibitor specificity.

scientific article published on 19 August 2002

Mechanisms of allosteric regulation of Trypanosoma cruzi S-adenosylmethionine decarboxylase

scientific article

Modeling of the spatial structure of eukaryotic ornithine decarboxylases ⬇️

scientific article published on July 1, 1995

Multiple active site conformations revealed by distant site mutation in ornithine decarboxylase

scientific article published in October 2004

Novel Antimalarial Tetrazoles and Amides Active against the Hemoglobin Degradation Pathway in <i>Plasmodium falciparum</i>

scientific article published on 23 February 2021

Novel Inhibitors of Plasmodium falciparum Dihydroorotate Dehydrogenase with Anti-malarial Activity in the Mouse Model

scientific article

Novel S-adenosylmethionine decarboxylase inhibitors for the treatment of human African trypanosomiasis

scientific article published on 16 March 2009

Optimization of a non-radioactive high-throughput assay for decarboxylase enzymes.

scientific article

Original 2-(3-Alkoxy-1H-pyrazol-1-yl)azines Inhibitors of Human Dihydroorotate Dehydrogenase (DHODH)

scientific article published on 30 June 2015

Ornithine decarboxylase promotes catalysis by binding the carboxylate in a buried pocket containing phenylalanine 397.

scientific article published in March 2003

Paramecium bursaria chlorella virus-1 encodes an unusual arginine decarboxylase that is a close homolog of eukaryotic ornithine decarboxylases

scientific article

Phylogenetic diversity and the structural basis of substrate specificity in the beta/alpha-barrel fold basic amino acid decarboxylases

scientific article

Plasmodium dihydroorotate dehydrogenase: a promising target for novel anti-malarial chemotherapy

scientific article

Potent Antimalarials with Development Potential Identified by Structure-Guided Computational Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series

scientific article published on 20 April 2021

Prized malaria drug target nailed ⬇️

scientific article published on May 1, 2003

Product feedback regulation implicated in translational control of the Trypanosoma brucei S‐adenosylmethionine decarboxylase regulatory subunit prozyme ⬇️

scientific article published on 02 May 2013

Putrescine activation of Trypanosoma cruzi S-adenosylmethionine decarboxylase

scientific article published in November 2002

Pyrimidine Salvage Enzymes Are Essential for De Novo Biosynthesis of Deoxypyrimidine Nucleotides in Trypanosoma brucei

scientific article

RNA interference-mediated silencing of ornithine decarboxylase and spermidine synthase genes in Trypanosoma brucei provides insight into regulation of polyamine biosynthesis

scientific article published on 20 March 2009

Regulated expression of an essential allosteric activator of polyamine biosynthesis in African trypanosomes

scientific article

Relief of autoinhibition by conformational switch explains enzyme activation by a catalytically dead paralog

scientific article published on 15 December 2016

SAR-Based Optimization of a 4-Quinoline Carboxylic Acid Analogue with Potent Antiviral Activity ⬇️

scientific article published on June 13, 2013

Safety, tolerability, pharmacokinetics, and activity of the novel long-acting antimalarial DSM265: a two-part first-in-human phase 1a/1b randomised study

scientific article

Selective delivery of 2-hydroxy APA to Trypanosoma brucei using the melamine motif

scientific article

Species-Selective Pyrimidineamine Inhibitors of Trypanosoma brucei S-Adenosylmethionine Decarboxylase.

scientific article published on 22 December 2017

Structural Plasticity of Malaria Dihydroorotate Dehydrogenase Allows Selective Binding of Diverse Chemical Scaffolds

scientific article

Structure-Guided Lead Optimization of Triazolopyrimidine-Ring Substituents Identifies Potent Plasmodium falciparum Dihydroorotate Dehydrogenase Inhibitors with Clinical Candidate Potential

scientific article

Synthesis and evaluation of analogs of 5'-(((Z)-4-amino-2-butenyl)methylamino)-5'-deoxyadenosine (MDL 73811, or AbeAdo) - An inhibitor of S-adenosylmethionine decarboxylase with antitrypanosomal activity

scientific article published on 3 August 2017

Targeted Nanodelivery of Drugs and Diagnostics

scientific article

Tetrahydro-2-naphthyl and 2-Indanyl Triazolopyrimidines Targeting Plasmodium falciparum Dihydroorotate Dehydrogenase Display Potent and Selective Antimalarial Activity

scientific article published on 29 April 2016

The X-ray structure of Plasmodium falciparum dihydroorotate dehydrogenase bound to a potent and selective N-phenylbenzamide inhibitor reveals novel binding-site interactions

scientific article published on 21 April 2015

Triazolopyrimidine-based dihydroorotate dehydrogenase inhibitors with potent and selective activity against the malaria parasite Plasmodium falciparum.

scientific article published on 04 June 2008

Trypanosomatid Deoxyhypusine Synthase Activity Is Dependent on Shared Active-Site Complementation between Pseudoenzyme Paralogs

X-ray Structure of Paramecium bursaria Chlorella Virus Arginine Decarboxylase: Insight into the Structural Basis for Substrate Specificity †

scientific article

X-ray structure determination of Trypanosoma brucei ornithine decarboxylase bound to D-ornithine and to G418: insights into substrate binding and ODC conformational flexibility

scientific article (publication date: 13 June 2003)

Yeast dihydroorotate dehydrogenase as a new selectable marker for Plasmodium falciparum transfection.

scientific article

List of works by Margaret A. Phillips

A Gateway® compatible vector for gene silencing in bloodstream form Trypanosoma brucei

A Teach-Discover-Treat Application of ZincPharmer: An Online Interactive Pharmacophore Modeling and Virtual Screening Tool

A dual regulatory circuit consisting of S-adenosylmethionine decarboxylase protein and its reaction product controls expression of the paralogous activator prozyme in Trypanosoma brucei

A long-duration dihydroorotate dehydrogenase inhibitor (DSM265) for prevention and treatment of malaria

A multiple aminoacyl-tRNA synthetase complex that enhances tRNA-aminoacylation in African trypanosomes

A triazolopyrimidine-based dihydroorotate dehydrogenase inhibitor (DSM421) with improved drug-like properties for treatment and prevention of malaria

Advanced molecular design of biopolymers for transmucosal and intracellular delivery of chemotherapeutic agents and biological therapeutics

Allosteric activation of trypanosomatid deoxyhypusine synthase by a catalytically dead paralog

Allosteric regulation of an essential trypanosome polyamine biosynthetic enzyme by a catalytically dead homolog

Alternative pathways utilize or circumvent putrescine for biosynthesis of putrescine-containing rhizoferrin

Alternative spermidine biosynthetic route is critical for growth of Campylobacter jejuni and is the dominant polyamine pathway in human gut microbiota

An alternative polyamine biosynthetic pathway is widespread in bacteria and essential for biofilm formation in Vibrio cholerae

Analysis of flavin oxidation and electron-transfer inhibition in Plasmodium falciparum dihydroorotate dehydrogenase

Anticancer properties of distinct antimalarial drug classes

Antimalarial activity of single-dose DSM265, a novel plasmodium dihydroorotate dehydrogenase inhibitor, in patients with uncomplicated Plasmodium falciparum or Plasmodium vivax malaria infection: a proof-of-concept, open-label, phase 2a study

Asexual populations of the human malaria parasite, Plasmodium falciparum, use a two-step genomic strategy to acquire accurate, beneficial DNA amplifications

Assessing drug efficacy against Plasmodium falciparum liver stages in vivo

Atovaquone tolerance in Plasmodium falciparum parasites selected for high-level resistance to a dihydroorotate dehydrogenase inhibitor

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

Cellular evaluation of synthesized insulin/transferrin bioconjugates for oral insulin delivery using intelligent complexation hydrogels

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

Chemical genetics of Plasmodium falciparum

Cross-species activation of trypanosome S-adenosylmethionine decarboxylase by the regulatory subunit prozyme

Deoxyhypusine Modification of Eukaryotic Translation Initiation Factor 5A (eIF5A) Is Essential for Trypanosoma brucei Growth and for Expression of Polyprolyl-containing Proteins

Detergent-dependent kinetics of truncated Plasmodium falciparum dihydroorotate dehydrogenase.

Discovery of new S-adenosylmethionine decarboxylase inhibitors for the treatment of Human African Trypanosomiasis (HAT).

Discovery of potent and selective inhibitors of Trypanosoma brucei ornithine decarboxylase

Evaluation of Antigens for Development of a Serological Test for Human African Trypanosomiasis

Evolution and multifarious horizontal transfer of an alternative biosynthetic pathway for the alternative polyamine sym-homospermidine

Evolution of Substrate Specificity within a Diverse Family of / -Barrel-fold Basic Amino Acid Decarboxylases: X-RAY STRUCTURE DETERMINATION OF ENZYMES WITH SPECIFICITY FOR L-ARGININE AND CARBOXYNORSPERMIDINE

Fluorine Modulates Species Selectivity in the Triazolopyrimidine Class of Plasmodium falciparum Dihydroorotate Dehydrogenase Inhibitors

GMP synthase is essential for viability and infectivity of Trypanosoma brucei despite a redundant purine salvage pathway.

Genetic validation of Trypanosoma brucei glutathione synthetase as an essential enzyme

Genetic validation of aminoacyl-tRNA synthetases as drug targets in Trypanosoma brucei

High-throughput screening for potent and selective inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase

Identification and Assay of Allosteric Regulators of S-Adenosylmethionine Decarboxylase ⬇️

Identification and mechanistic understanding of dihydroorotate dehydrogenase point mutations in Plasmodium falciparum that confer in vitro resistance to the clinical candidate DSM265

Identification of New Human Malaria Parasite Plasmodium falciparum Dihydroorotate Dehydrogenase Inhibitors by Pharmacophore and Structure-Based Virtual Screening

Identification of Trypanosoma brucei AdoMetDC Inhibitors Using a High-Throughput Mass Spectrometry-Based Assay.

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

Improved Synthesis of MDL 73811 - a Potent AdoMetDC Inhibitor and Anti-Trypanosomal Compound

Inhibition of pyrimidine synthesis reverses viral virulence factor-mediated block of mRNA nuclear export

Isoxazolopyrimidine-Based Inhibitors of Dihydroorotate Dehydrogenase with Antimalarial Activity

Lead Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series for the Treatment of Malaria

Lead optimization of 3-carboxyl-4(1H)-quinolones to deliver orally bioavailable antimalarials

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

Malaria

Malarial dihydroorotate dehydrogenase. Substrate and inhibitor specificity.

Mechanisms of allosteric regulation of Trypanosoma cruzi S-adenosylmethionine decarboxylase

Modeling of the spatial structure of eukaryotic ornithine decarboxylases ⬇️

Multiple active site conformations revealed by distant site mutation in ornithine decarboxylase

Novel Antimalarial Tetrazoles and Amides Active against the Hemoglobin Degradation Pathway in <i>Plasmodium falciparum</i>

Novel Inhibitors of Plasmodium falciparum Dihydroorotate Dehydrogenase with Anti-malarial Activity in the Mouse Model

Novel S-adenosylmethionine decarboxylase inhibitors for the treatment of human African trypanosomiasis

Optimization of a non-radioactive high-throughput assay for decarboxylase enzymes.

Original 2-(3-Alkoxy-1H-pyrazol-1-yl)azines Inhibitors of Human Dihydroorotate Dehydrogenase (DHODH)

Ornithine decarboxylase promotes catalysis by binding the carboxylate in a buried pocket containing phenylalanine 397.

Paramecium bursaria chlorella virus-1 encodes an unusual arginine decarboxylase that is a close homolog of eukaryotic ornithine decarboxylases

Phylogenetic diversity and the structural basis of substrate specificity in the beta/alpha-barrel fold basic amino acid decarboxylases

Plasmodium dihydroorotate dehydrogenase: a promising target for novel anti-malarial chemotherapy

Potent Antimalarials with Development Potential Identified by Structure-Guided Computational Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series

Prized malaria drug target nailed ⬇️

Product feedback regulation implicated in translational control of the Trypanosoma brucei S‐adenosylmethionine decarboxylase regulatory subunit prozyme ⬇️

Putrescine activation of Trypanosoma cruzi S-adenosylmethionine decarboxylase

Pyrimidine Salvage Enzymes Are Essential for De Novo Biosynthesis of Deoxypyrimidine Nucleotides in Trypanosoma brucei

RNA interference-mediated silencing of ornithine decarboxylase and spermidine synthase genes in Trypanosoma brucei provides insight into regulation of polyamine biosynthesis

Regulated expression of an essential allosteric activator of polyamine biosynthesis in African trypanosomes

Relief of autoinhibition by conformational switch explains enzyme activation by a catalytically dead paralog

SAR-Based Optimization of a 4-Quinoline Carboxylic Acid Analogue with Potent Antiviral Activity ⬇️

Safety, tolerability, pharmacokinetics, and activity of the novel long-acting antimalarial DSM265: a two-part first-in-human phase 1a/1b randomised study

Selective delivery of 2-hydroxy APA to Trypanosoma brucei using the melamine motif

Species-Selective Pyrimidineamine Inhibitors of Trypanosoma brucei S-Adenosylmethionine Decarboxylase.

Structural Plasticity of Malaria Dihydroorotate Dehydrogenase Allows Selective Binding of Diverse Chemical Scaffolds

Structure-Guided Lead Optimization of Triazolopyrimidine-Ring Substituents Identifies Potent Plasmodium falciparum Dihydroorotate Dehydrogenase Inhibitors with Clinical Candidate Potential

Synthesis and evaluation of analogs of 5'-(((Z)-4-amino-2-butenyl)methylamino)-5'-deoxyadenosine (MDL 73811, or AbeAdo) - An inhibitor of S-adenosylmethionine decarboxylase with antitrypanosomal activity

Targeted Nanodelivery of Drugs and Diagnostics

Tetrahydro-2-naphthyl and 2-Indanyl Triazolopyrimidines Targeting Plasmodium falciparum Dihydroorotate Dehydrogenase Display Potent and Selective Antimalarial Activity

The X-ray structure of Plasmodium falciparum dihydroorotate dehydrogenase bound to a potent and selective N-phenylbenzamide inhibitor reveals novel binding-site interactions

Triazolopyrimidine-based dihydroorotate dehydrogenase inhibitors with potent and selective activity against the malaria parasite Plasmodium falciparum.