Covalent Plasmodium falciparum-selective proteasome inhibitors exhibit a low propensity for generating resistance in vitro and synergize with multiple antimalarial agents

Artemisone and artemiside - potent pan-reactive antimalarial agents that also synergize redox imbalance in P. falciparum transmissible gametocyte stages

(2018) Dina Coertzen et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

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

(2018) Alejandro Llanos-Cuentas et al.   LANCET INFECTIOUS DISEASES

Drug resistance in Plasmodium

(2018) Kasturi Haldar et al.   NATURE REVIEWS MICROBIOLOGY

Antimalarial proteasome inhibitor reveals collateral sensitivity from intersubunit interactions and fitness cost of resistance

(2018) Laura A. Kirkman et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Mapping the malaria parasite druggable genome by using in vitro evolution and chemogenomics

(2018) Annie N. Cowell et al.   SCIENCE

Defining the Determinants of Specificity of Plasmodium Proteasome Inhibitors

(2018) Euna Yoo et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Artemisinin kills malaria parasites by damaging proteins and inhibiting the proteasome

(2018) Jessica L. Bridgford et al.   Nature Communications

Target Validation and Identification of Novel Boronate Inhibitors of the Plasmodium falciparum Proteasome

(2018) Stanley C. Xie et al.   JOURNAL OF MEDICINAL CHEMISTRY

Evidence of Artemisinin-Resistant Plasmodium falciparum Malaria in Eastern India

(2018) Sabyasachi Das et al.   NEW ENGLAND JOURNAL OF MEDICINE

Activity-based probes for the multicatalytic proteasome

(2017) David S. Hewings et al.   FEBS Journal

Development of a Potent Inhibitor of the Plasmodium Proteasome with Reduced Mammalian Toxicity

(2017) Gregory M. LaMonte et al.   JOURNAL OF MEDICINAL CHEMISTRY

The spread of artemisinin-resistant Plasmodium falciparum in the Greater Mekong subregion: a molecular epidemiology observational study

(2017) Mallika Imwong et al.   LANCET INFECTIOUS DISEASES

A high susceptibility to redox imbalance of the transmissible stages ofPlasmodium falciparumrevealed with a luciferase-based mature gametocyte assay

(2017) Giulia Siciliano et al.   MOLECULAR MICROBIOLOGY

Antimalarial drug resistance: linking Plasmodium falciparum parasite biology to the clinic

(2017) Benjamin Blasco et al.   NATURE MEDICINE

A Variant PfCRT Isoform Can Contribute to Plasmodium falciparum Resistance to the First-Line Partner Drug Piperaquine

(2017) Satish K. Dhingra et al.   mBio

Plasmodium falciparum K13 Mutations Differentially Impact Ozonide Susceptibility and Parasite Fitness In Vitro

(2017) Judith Straimer et al.   mBio

A potent antimalarial benzoxaborole targets a Plasmodium falciparum cleavage and polyadenylation specificity factor homologue

(2017) Ebere Sonoiki et al.   Nature Communications

Malaria

(2017) Margaret A. Phillips et al.   Nature Reviews Disease Primers

A Click Chemistry-Based Proteomic Approach Reveals that 1,2,4-Trioxolane and Artemisinin Antimalarials Share a Common Protein Alkylation Profile

(2016) Hanafy M. Ismail et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Endoperoxide Drug Cross-Resistance Patterns for Plasmodium falciparum Exhibiting an Artemisinin Delayed-Clearance Phenotype

(2016) A. Siriwardana et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

The cryo-EM structure of thePlasmodium falciparum20S proteasome and its use in the fight against malaria

(2016) Hao Li et al.   FEBS Journal

Antimalarial activity of artefenomel (OZ439), a novel synthetic antimalarial endoperoxide, in patients with Plasmodium falciparum and Plasmodium vivax malaria: an open-label phase 2 trial

(2016) Aung Pyae Phyo et al.   LANCET INFECTIOUS DISEASES

CRISPR-Cas9-modifiedpfmdr1protectsPlasmodium falciparumasexual blood stages and gametocytes against a class of piperazine-containing compounds but potentiates artemisinin-based combination therapy partner drugs

(2016) Caroline L. Ng et al.   MOLECULAR MICROBIOLOGY

Structure- and function-based design of Plasmodium-selective proteasome inhibitors

(2016) Hao Li et al.   NATURE

A Worldwide Map ofPlasmodium falciparumK13-Propeller Polymorphisms

(2016) Didier Ménard et al.   NEW ENGLAND JOURNAL OF MEDICINE

Artemisinin activity-based probes identify multiple molecular targets within the asexual stage of the malaria parasitesPlasmodium falciparum3D7

(2016) Hanafy M. Ismail et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Evidence of a Mild Mutator Phenotype in Cambodian Plasmodium falciparum Malaria Parasites

(2016) Andrew H. Lee et al.   PLoS One

Synthesis and Evaluation of Derivatives of the Proteasome Deubiquitinase Inhibitor b-AP15

(2015) Xin Wang et al.   Chemical Biology & Drug Design

Haemoglobin degradation underpins the sensitivity of early ring stagePlasmodium falciparumto artemisinins

(2015) Stanley C. Xie et al.   JOURNAL OF CELL SCIENCE

Role and Regulation of Glutathione Metabolism in Plasmodium falciparum

(2015) Sylke Müller   MOLECULES

A novel multiple-stage antimalarial agent that inhibits protein synthesis

(2015) Beatriz Baragaña et al.   NATURE

The cytoplasmic prolyl-tRNA synthetase of the malaria parasite is a dual-stage target of febrifugine and its analogs

(2015) Jonathan D. Herman et al.   Science Translational Medicine

Characterization of the 26S proteasome network in Plasmodium falciparum

(2015) Lihui Wang et al.   Scientific Reports

Targeting the Cell Stress Response of Plasmodium falciparum to Overcome Artemisinin Resistance

(2015) Con Dogovski et al.   PLOS BIOLOGY

Monoclonal Antibodies That Recognize the Alkylation Signature of Antimalarial Ozonides OZ277 (Arterolane) and OZ439 (Artefenomel)

(2015) Joëlle Jourdan et al.   ACS Infectious Diseases

Assessing Subunit Dependency of the Plasmodium Proteasome Using Small Molecule Inhibitors and Active Site Probes

(2014) Hao Li et al.   ACS Chemical Biology

Identification of pathogen genomic variants through an integrated pipeline

(2014) Micah J Manary et al.   BMC BIOINFORMATICS

ER-associated degradation: Protein quality control and beyond

(2014) Annamaria Ruggiano et al.   JOURNAL OF CELL BIOLOGY

Efficacy and Safety of Triple Combination Therapy With Artesunate-Amodiaquine–Methylene Blue for Falciparum Malaria in Children: A Randomized Controlled Trial in Burkina Faso

(2014) Boubacar Coulibaly et al.   JOURNAL OF INFECTIOUS DISEASES

Origin of Robustness in Generating Drug-Resistant Malaria Parasites

(2014) Krittikorn Kümpornsin et al.   MOLECULAR BIOLOGY AND EVOLUTION

Genome editing in the human malaria parasite Plasmodium falciparum using the CRISPR-Cas9 system

(2014) Mehdi Ghorbal et al.   NATURE BIOTECHNOLOGY

Spread of Artemisinin Resistance in Plasmodium falciparum Malaria

(2014) Elizabeth A. Ashley et al.   NEW ENGLAND JOURNAL OF MEDICINE

K13-propeller mutations confer artemisinin resistance in Plasmodium falciparum clinical isolates

(2014) J. Straimer et al.   SCIENCE

Population transcriptomics of human malaria parasites reveals the mechanism of artemisinin resistance

(2014) S. Mok et al.   SCIENCE

The emerging family of CULLIN3-RING ubiquitin ligases (CRL3s): cellular functions and disease implications

(2013) Pascal Genschik et al.   EMBO JOURNAL

Novel phenotypic assays for the detection of artemisinin-resistant Plasmodium falciparum malaria in Cambodia: in-vitro and ex-vivo drug-response studies

(2013) Benoit Witkowski et al.   LANCET INFECTIOUS DISEASES

A molecular marker of artemisinin-resistant Plasmodium falciparum malaria

(2013) Frédéric Ariey et al.   NATURE

Altered temporal response of malaria parasites determines differential sensitivity to artemisinin

(2013) N. Klonis et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

A program for annotating and predicting the effects of single nucleotide polymorphisms, SnpEff

(2012) Pablo Cingolani et al.   FLY

Eeyarestatin causes cervical cancer cell sensitization to bortezomib treatment by augmenting ER stress and CHOP expression

(2012) German J. Brem et al.   GYNECOLOGIC ONCOLOGY

In VivoandIn VitroAntimalarial Properties of Azithromycin-Chloroquine Combinations That Include the Resistance Reversal Agent Amlodipine

(2011) Marcus R. Pereira et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Identifying apicoplast-targeting antimalarials using high-throughput compatible approaches

(2011) Eric H. Ekland et al.   FASEB JOURNAL

Structure-Guided Lead Optimization of Triazolopyrimidine-Ring Substituents Identifies PotentPlasmodium falciparumDihydroorotate Dehydrogenase Inhibitors with Clinical Candidate Potential

(2011) Jose M. Coteron et al.   JOURNAL OF MEDICINAL CHEMISTRY

Inhibition of proteasome deubiquitinating activity as a new cancer therapy

(2011) Pádraig D'Arcy et al.   NATURE MEDICINE

The discovery of artemisinin (qinghaosu) and gifts from Chinese medicine

(2011) Youyou Tu   NATURE MEDICINE

Quantitative assessment of Plasmodium falciparum sexual development reveals potent transmission-blocking activity by methylene blue

(2011) S. H. Adjalley et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Artemisinin activity against Plasmodium falciparum requires hemoglobin uptake and digestion

(2011) N. Klonis et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The ERAD Inhibitor Eeyarestatin I Is a Bifunctional Compound with a Membrane-Binding Domain and a p97/VCP Inhibitory Group

(2010) Qiuyan Wang et al.   PLoS One

Spiroindolones, a Potent Compound Class for the Treatment of Malaria

(2010) M. Rottmann et al.   SCIENCE

Role of Plasmodium falciparum Digestive Vacuole Plasmepsins in the Specificity and Antimalarial Mode of Action of Cysteine and Aspartic Protease Inhibitors

(2009) P. A. Moura et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

The Proteasome Inhibitor Epoxomicin Has Potent Plasmodium falciparum Gametocytocidal Activity

(2009) B. Czesny et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Plasmodium Food Vacuole Plasmepsins Are Activated by Falcipains

(2008) Mark E. Drew et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Qinghaosu (Artemisinin): The Price of Success

(2008) N. J. White   SCIENCE

Adaptive Copy Number Evolution in Malaria Parasites

(2008) Shalini Nair et al.   PLoS Genetics