Targeting the Malaria Parasite cGMP-Dependent Protein Kinase to Develop New Drugs

Mechanism of allosteric inhibition in the Plasmodiumfalciparum cGMP-dependent protein kinase

(2020) Jung Ah Byun et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Structures of the cGMP-dependent protein kinase in malaria parasites reveal a unique structural relay mechanism for activation

(2019) Majida El Bakkouri et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

High-throughput screening of the Plasmodium falciparum cGMP-dependent protein kinase identified a thiazole scaffold which kills erythrocytic and sexual stage parasites

(2019) Maria Penzo et al.   Scientific Reports

Development of Chemical Entities Endowed with Potent Fast- Killing Properties against Plasmodium falciparum Malaria Parasites

(2019) Alexios N Matralis et al.   JOURNAL OF MEDICINAL CHEMISTRY

Potent bicyclic inhibitors of malarial cGMP-dependent protein kinase: approaches to combining improvements in cell potency, selectivity and structural novelty

(2019) Jonathan M. Large et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

cGMP Signaling in the Cardiovascular System—The Role of Compartmentation and Its Live Cell Imaging

(2018) Nadja Bork et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Plasmodial Kinase Inhibitors: License to Cure?

(2018) Diego González Cabrera et al.   JOURNAL OF MEDICINAL CHEMISTRY

A protease cascade regulates release of the human malaria parasite Plasmodium falciparum from host red blood cells

(2018) James A. Thomas et al.   Nature Microbiology

Trisubstituted thiazoles as potent and selective inhibitors of Plasmodium falciparum protein kinase G (PfPKG)

(2018) Denise J. Tsagris et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Potent inhibitors of malarial P. Falciparum protein kinase G: Improving the cell activity of a series of imidazopyridines

(2018) Jonathan M. Large et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Epistasis studies reveal redundancy among calcium-dependent protein kinases in motility and invasion of malaria parasites

(2018) Hanwei Fang et al.   Nature Communications

Cyclic nucleotide signalling in malaria parasites

(2017) David A. Baker et al.   Open Biology

Invasion of hepatocytes byPlasmodiumsporozoites requires cGMP-dependent protein kinase and calcium dependent protein kinase 4

(2016) K. Govindasamy et al.   MOLECULAR MICROBIOLOGY

Imidazopyridazine Inhibitors of Plasmodium falciparum Calcium-Dependent Protein Kinase 1 Also Target Cyclic GMP-Dependent Protein Kinase and Heat Shock Protein 90 To Kill the Parasite at Different Stages of Intracellular Development

(2015) Judith L. Green et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Cyclic GMP Balance Is Critical for Malaria Parasite Transmission from the Mosquito to the Mammalian Host

(2015) Viswanathan Lakshmanan et al.   mBio

Phosphoproteomics reveals malaria parasite Protein Kinase G as a signalling hub regulating egress and invasion

(2015) Mahmood M. Alam et al.   Nature Communications

Biochemical and Antiparasitic Properties of Inhibitors of the Plasmodium falciparum Calcium-Dependent Protein Kinase PfCDPK1

(2014) Keith H. Ansell et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Dose Selection, Pharmacokinetics, and Pharmacodynamics of BRAF Inhibitor Dabrafenib (GSK2118436)

(2014) G. S. Falchook et al.   CLINICAL CANCER RESEARCH

Optimization of an Imidazopyridazine Series of Inhibitors of Plasmodium falciparum Calcium-Dependent Protein Kinase 1 (PfCDPK1)

(2014) Timothy M. Chapman et al.   JOURNAL OF MEDICINAL CHEMISTRY

Phosphoinositide Metabolism Links cGMP-Dependent Protein Kinase G to Essential Ca2+ Signals at Key Decision Points in the Life Cycle of Malaria Parasites

(2014) Mathieu Brochet et al.   PLOS BIOLOGY

Discovery of Dabrafenib: A Selective Inhibitor of Raf Kinases with Antitumor Activity against B-Raf-Driven Tumors

(2013) Tara R. Rheault et al.   ACS Medicinal Chemistry Letters

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

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

Thousands of chemical starting points for antimalarial lead identification

(2010) Francisco-Javier Gamo et al.   NATURE

A Plant-Like Kinase in Plasmodium falciparum Regulates Parasite Egress from Erythrocytes

(2010) J. D. Dvorin et al.   SCIENCE

Kinase selectivity potential for inhibitors targeting the ATP binding site: a network analysis

(2009) Danzhi Huang et al.   BIOINFORMATICS

The Malaria Parasite Cyclic GMP-Dependent Protein Kinase Plays a Central Role in Blood-Stage Schizogony

(2009) Helen M. Taylor et al.   EUKARYOTIC CELL

Role of Plasmodium berghei cGMP-dependent Protein Kinase in Late Liver Stage Development

(2009) Adebola Falae et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

A Cyclic GMP Signalling Module That Regulates Gliding Motility in a Malaria Parasite

(2009) Robert W. Moon et al.   PLoS Pathogens

Disruption of aPlasmodium falciparumcyclic nucleotide phosphodiesterase gene causes aberrant gametogenesis

(2008) Cathy J. Taylor et al.   MOLECULAR MICROBIOLOGY

Gametogenesis in Malaria Parasites Is Mediated by the cGMP-Dependent Protein Kinase

(2008) Louisa McRobert et al.   PLOS BIOLOGY