Proteases as antimalarial targets: strategies for genetic, chemical, and therapeutic validation

Host cell remodelling in malaria parasites: a new pool of potential drug targets

(2017) Paul R. Gilson et al.   INTERNATIONAL JOURNAL FOR PARASITOLOGY

Plasmodium berghei plasmepsin VIII is essential for sporozoite gliding motility

(2017) Babu S. Mastan et al.   INTERNATIONAL JOURNAL FOR PARASITOLOGY

Targeted Deletion of a Plasmodium Site-2 Protease Impairs Life Cycle Progression in the Mammalian Host

(2017) Konstantinos Koussis et al.   PLoS One

Positional proteomics in the era of the human proteome project on the doorstep of precision medicine

(2016) Ulrich Eckhard et al.   BIOCHIMIE

Potent dual inhibitors of Plasmodium falciparum M1 and M17 aminopeptidases through optimization of S1 pocket interactions

(2016) Nyssa Drinkwater et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

A Plasmodium falciparum S33 proline aminopeptidase is associated with changes in erythrocyte deformability

(2016) Fabio L. da Silva et al.   EXPERIMENTAL PARASITOLOGY

Plasmodium falciparum ookinete expression of plasmepsin VII and plasmepsin X

(2016) Fengwu Li et al.   MALARIA JOURNAL

Comparative Proteomics and Functional Analysis Reveal a Role ofPlasmodium falciparumOsmiophilic Bodies in Malaria Parasite Transmission

(2016) Pablo Suárez-Cortés et al.   MOLECULAR & CELLULAR PROTEOMICS

Advances in identification and validation of protein targets of natural products without chemical modification

(2016) J. Chang et al.   NATURAL PRODUCT REPORTS

Chemical proteomics approaches for identifying the cellular targets of natural products

(2016) M. H. Wright et al.   NATURAL PRODUCT REPORTS

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

(2016) Hao Li et al.   NATURE

Immune activation and induction of memory: lessons learned from controlled human malaria infection with Plasmodium falciparum

(2016) ANJA SCHOLZEN et al.   PARASITOLOGY

Normocyte-binding protein required for human erythrocyte invasion by the zoonotic malaria parasitePlasmodium knowlesi

(2016) Robert W. Moon et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

PARL: The mitochondrial rhomboid protease

(2016) Marco Spinazzi et al.   SEMINARS IN CELL & DEVELOPMENTAL BIOLOGY

Phenotypic Screens in Antimalarial Drug Discovery

(2016) Marisa L. Hovlid et al.   TRENDS IN PARASITOLOGY

Insecticide Resistance in African Anopheles Mosquitoes: A Worsening Situation that Needs Urgent Action to Maintain Malaria Control

(2016) Hilary Ranson et al.   TRENDS IN PARASITOLOGY

A broad analysis of resistance development in the malaria parasite

(2016) Victoria C. Corey et al.   Nature Communications

A versatile strategy for rapid conditional genome engineering using loxP sites in a small synthetic intron in Plasmodium falciparum

(2016) Matthew L. Jones et al.   Scientific Reports

Development and Application of a Simple Plaque Assay for the Human Malaria Parasite Plasmodium falciparum

(2016) James A. Thomas et al.   PLoS One

Recent advances and concepts in substrate specificity determination of proteases using tailored libraries of fluorogenic substrates with unnatural amino acids

(2015) Wioletta Rut et al.   BIOLOGICAL CHEMISTRY

Processing of Plasmodium falciparum Merozoite Surface Protein MSP1 Activates a Spectrin-Binding Function Enabling Parasite Egress from RBCs

(2015) Sujaan Das et al.   Cell Host & Microbe

Replication ofPlasmodiumin reticulocytes can occur without hemozoin formation, resulting in chloroquine resistance

(2015) Jing-wen Lin et al.   JOURNAL OF EXPERIMENTAL MEDICINE

Identifying rapidly parasiticidal anti-malarial drugs using a simple and reliable in vitro parasite viability fast assay

(2015) María Linares et al.   MALARIA JOURNAL

A novel multiple-stage antimalarial agent that inhibits protein synthesis

(2015) Beatriz Baragaña et al.   NATURE

The effect of malaria control on Plasmodium falciparum in Africa between 2000 and 2015

(2015) S. Bhatt et al.   NATURE

Malaria medicines: a glass half full?

(2015) Timothy N. C. Wells et al.   NATURE REVIEWS DRUG DISCOVERY

Advances in molecular genetic systems in malaria

(2015) Tania F. de Koning-Ward et al.   NATURE REVIEWS MICROBIOLOGY

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

(2015) Margaret A. Phillips et al.   Science Translational Medicine

Characterization of the 26S proteasome network in Plasmodium falciparum

(2015) Lihui Wang et al.   Scientific Reports

High-throughput matrix screening identifies synergistic and antagonistic antimalarial drug combinations

(2015) Bryan T. Mott et al.   Scientific Reports

Revealing the Sequence and Resulting Cellular Morphology of Receptor-Ligand Interactions during Plasmodium falciparum Invasion of Erythrocytes

(2015) Greta E. Weiss et al.   PLoS Pathogens

Picomolar Inhibition of Plasmepsin V, an Essential Malaria Protease, Achieved Exploiting the Prime Region

(2015) Luca Gambini et al.   PLoS One

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

(2014) Hao Li et al.   ACS Chemical Biology

Unnatural amino acids increase activity and specificity of synthetic substrates for human and malarial cathepsin C

(2014) Marcin Poreba et al.   AMINO ACIDS

Activity-Based Profiling of Proteases

(2014) Laura E. Sanman et al.   Annual Review of Biochemistry

Of men in mice: the success and promise of humanized mouse models for human malaria parasite infections

(2014) Alexis Kaushansky et al.   CELLULAR MICROBIOLOGY

Conditional expression of apical membrane antigen 1 inPlasmodium falciparumshows it is required for erythrocyte invasion by merozoites

(2014) Alan Yap et al.   CELLULAR MICROBIOLOGY

Two-Pronged Attack: Dual Inhibition of Plasmodium falciparum M1 and M17 Metalloaminopeptidases by a Novel Series of Hydroxamic Acid-Based Inhibitors

(2014) Shailesh N. Mistry et al.   JOURNAL OF MEDICINAL CHEMISTRY

Gene disruption reveals a dispensable role for Plasmepsin VII in the Plasmodium berghei life cycle

(2014) Babu S. Mastan et al.   MOLECULAR AND BIOCHEMICAL PARASITOLOGY

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

(2014) Mehdi Ghorbal et al.   NATURE BIOTECHNOLOGY

Efficient CRISPR-Cas9–mediated genome editing in Plasmodium falciparum

(2014) Jeffrey C Wagner et al.   NATURE METHODS

Spread of Artemisinin Resistance in Plasmodium falciparum Malaria

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

Inhibition of Plasmepsin V Activity Demonstrates Its Essential Role in Protein Export, PfEMP1 Display, and Survival of Malaria Parasites

(2014) Brad E. Sleebs et al.   PLOS BIOLOGY

Plasmodium Dipeptidyl Aminopeptidases as Malaria Transmission-Blocking Drug Targets

(2013) Takeshi Q Tanaka et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

A Key Role forPlasmodiumSubtilisin-like SUB1 Protease in Egress of Malaria Parasites from Host Hepatocytes

(2013) Lina Tawk et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Using Genetic Methods To Define the Targets of Compounds with Antimalarial Activity

(2013) Erika L. Flannery et al.   JOURNAL OF MEDICINAL CHEMISTRY

Loss-of-function analyses defines vital and redundant functions of thePlasmodiumrhomboid protease family

(2013) Jing-wen Lin et al.   MOLECULAR MICROBIOLOGY

Robust inducible Cre recombinase activity in the human malaria parasitePlasmodium falciparumenables efficient gene deletion within a single asexual erythrocytic growth cycle

(2013) Christine R. Collins et al.   MOLECULAR MICROBIOLOGY

An FtsH Protease Is Recruited to the Mitochondrion of Plasmodium falciparum

(2013) Aiman Tanveer et al.   PLoS One

Plasmodium rhoptry proteins: why order is important

(2013) Natalie A. Counihan et al.   TRENDS IN PARASITOLOGY

Genome-wide screen identifies new candidate genes associated with artemisinin susceptibility in Plasmodium falciparum in Kenya

(2013) Steffen Borrmann et al.   Scientific Reports

The Malarial Serine Protease SUB1 Plays an Essential Role in Parasite Liver Stage Development

(2013) Catherine Suarez et al.   PLoS Pathogens

Malaria Parasite cGMP-dependent Protein Kinase Regulates Blood Stage Merozoite Secretory Organelle Discharge and Egress

(2013) Christine R. Collins et al.   PLoS Pathogens

Active cathepsins B, L, and S in murine and human pancreatitis

(2012) Victoria Lyo et al.   AMERICAN JOURNAL OF PHYSIOLOGY-GASTROINTESTINAL AND LIVER PHYSIOLOGY

Controlled Human Blood Stage Malaria Infection: Current Status and Potential Applications

(2012) Christopher J. A. Duncan et al.   AMERICAN JOURNAL OF TROPICAL MEDICINE AND HYGIENE

Processing peptidases in mitochondria and chloroplasts

(2012) Pedro Filipe Teixeira et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

Validation of the Proteasome as a Therapeutic Target in Plasmodium Using an Epoxyketone Inhibitor with Parasite-Specific Toxicity

(2012) Hao Li et al.   CHEMISTRY & BIOLOGY

Antimalarial Drug Resistance and Early Drug Discovery

(2012) Jose F. Garcia-Bustos et al.   CURRENT PHARMACEUTICAL DESIGN

Recent Advances in Plasmepsin Medicinal Chemistry and Implications for Future Antimalarial Drug Discovery Efforts

(2012) Marvin J. Meyers et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Proteolytic Activation of the Essential Parasitophorous Vacuole Cysteine Protease SERA6 Accompanies Malaria Parasite Egress from Its Host Erythrocyte

(2012) Andrea Ruecker et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

P. falciparum In Vitro Killing Rates Allow to Discriminate between Different Antimalarial Mode-of-Action

(2012) Laura M. Sanz et al.   PLoS One

Fingerprinting the Substrate Specificity of M1 and M17 Aminopeptidases of Human Malaria, Plasmodium falciparum

(2012) Marcin Poreba et al.   PLoS One

Targeting the ERAD pathway via inhibition of signal peptide peptidase for antiparasitic therapeutic design

(2012) M. B. Harbut et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Malaria Parasite Signal Peptide Peptidase is an ER-Resident Protease Required for Growth but not for Invasion

(2012) Danushka S. Marapana et al.   TRAFFIC

Shedding of TRAP by a Rhomboid Protease from the Malaria Sporozoite Surface Is Essential for Gliding Motility and Sporozoite Infectivity

(2012) Ijeoma Ejigiri et al.   PLoS Pathogens

Proteases as regulators of pathogenesis: Examples from the Apicomplexa

(2011) Hao Li et al.   BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS

Super-Resolution Dissection of Coordinated Events during Malaria Parasite Invasion of the Human Erythrocyte

(2011) David T. Riglar et al.   Cell Host & Microbe

The moving junction of apicomplexan parasites: a key structure for invasion

(2011) Sébastien Besteiro et al.   CELLULAR MICROBIOLOGY

Functional Characterization of a SUMO Deconjugating Protease of Plasmodium falciparum Using Newly Identified Small Molecule Inhibitors

(2011) Elizabeth L. Ponder et al.   CHEMISTRY & BIOLOGY

Global Identification of Multiple Substrates forPlasmodium falciparumSUB1, an Essential Malarial Processing Protease

(2011) Natalie C. Silmon de Monerri et al.   INFECTION AND IMMUNITY

A new molecular approach for cidal vs static antimalarial determination by quantifying mRNA levels

(2011) Noemí Bahamontes-Rosa et al.   MOLECULAR AND BIOCHEMICAL PARASITOLOGY

Are protozoan metacaspases potential parasite killers?

(2011) Benoît Meslin et al.   Parasites & Vectors

Plasmodium falciparum Metacaspase PfMCA-1 Triggers a z-VAD-fmk Inhibitable Protease to Promote Cell Death

(2011) Benoît Meslin et al.   PLoS One

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

Bestatin-based chemical biology strategy reveals distinct roles for malaria M1- and M17-family aminopeptidases

(2011) M. B. Harbut et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Focus on the ringleader: the role of AMA1 in apicomplexan invasion and replication

(2011) Jessica S. Tyler et al.   TRENDS IN PARASITOLOGY

The contribution of Plasmodium chabaudi to our understanding of malaria

(2011) Robin Stephens et al.   TRENDS IN PARASITOLOGY

Plasmodium Protease ROM1 Is Important for Proper Formation of the Parasitophorous Vacuole

(2011) Iset Medina Vera et al.   PLoS Pathogens

Functional Studies of Plasmodium falciparum Dipeptidyl Aminopeptidase I Using Small Molecule Inhibitors and Active Site Probes

(2010) Edgar Deu et al.   CHEMISTRY & BIOLOGY

Mitochondrial localization of the threonine peptidase PfHslV, a ClpQ ortholog in Plasmodium falciparum

(2010) Serena Tschan et al.   INTERNATIONAL JOURNAL FOR PARASITOLOGY

Global Profiling of Proteolysis during Rupture ofPlasmodium falciparumfrom the Host Erythrocyte

(2010) Paul W. Bowyer et al.   MOLECULAR & CELLULAR PROTEOMICS

Biochemical characterization of Plasmodium falciparum dipeptidyl aminopeptidase 1

(2010) Flora Wang et al.   MOLECULAR AND BIOCHEMICAL PARASITOLOGY

An aspartyl protease directs malaria effector proteins to the host cell

(2010) Justin A. Boddey et al.   NATURE

Plasmepsin V licenses Plasmodium proteins for export into the host erythrocyte

(2010) Ilaria Russo et al.   NATURE

Thousands of chemical starting points for antimalarial lead identification

(2010) Francisco-Javier Gamo et al.   NATURE

Chemical genetics of Plasmodium falciparum

(2010) W. Armand Guiguemde et al.   NATURE

Emerging principles in protease-based drug discovery

(2010) Marcin Drag et al.   NATURE REVIEWS DRUG DISCOVERY

A programmed cell death pathway in the malaria parasite Plasmodium falciparum has general features of mammalian apoptosis but is mediated by clan CA cysteine proteases

(2010) J-H Ch'ng et al.   Cell Death & Disease

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

Antiparasitic activities of novel, orally available fumagillin analogs

(2009) Christopher Arico-Muendel et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Fumagillin and Fumarranol Interact with P. falciparum Methionine Aminopeptidase 2 and Inhibit Malaria Parasite Growth In Vitro and In Vivo

(2009) Xiaochun Chen et al.   CHEMISTRY & BIOLOGY

A calpain unique to alveolates is essential in Plasmodium falciparum and its knockdown reveals an involvement in pre-S-phase development

(2009) I. Russo et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Apicomplexan Parasites Co-Opt Host Calpains to Facilitate Their Escape from Infected Cells

(2009) R. Chandramohanadas et al.   SCIENCE

Distinct Roles of Plasmodium Rhomboid 1 in Parasite Development and Malaria Pathogenesis

(2009) Prakash Srinivasan et al.   PLoS Pathogens

Identification of Rhoptry Trafficking Determinants and Evidence for a Novel Sorting Mechanism in the Malaria Parasite Plasmodium falciparum

(2009) Dave Richard et al.   PLoS Pathogens

Plasmodium Food Vacuole Plasmepsins Are Activated by Falcipains

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

Reverse genetics screen identifies six proteins important for malaria development in the mosquito

(2008) Andrea Ecker et al.   MOLECULAR MICROBIOLOGY

Identification of proteases that regulate erythrocyte rupture by the malaria parasite Plasmodium falciparum

(2008) Shirin Arastu-Kapur et al.   Nature Chemical Biology

Formation of the Food Vacuole in Plasmodium falciparum: A Potential Role for the 19 kDa Fragment of Merozoite Surface Protein 1 (MSP119)

(2008) Anton R. Dluzewski et al.   PLoS One

Plasmodium falciparum signal peptidase is regulated by phosphorylation and required for intra-erythrocytic growth

(2007) Renu Tuteja et al.   MOLECULAR AND BIOCHEMICAL PARASITOLOGY