Christopher R. Mansfield

Development of domain-specific probes of Plasmodium falciparum heat shock protein 70-1

Aaron M. Keeler, Gaini Ibrasheva, E. Boger, Yueqi Chen et autres

ABSTRACT In the malaria parasite Plasmodium falciparum , the essential chaperone Pf Hsp70-1 regulates proteostasis through protein folding, but its domain-specific functions remain poorly defined. The protein contains an N-terminal nucleotide-binding domain (NBD) and a C-terminal substrate-binding domain (SBD), where selective inhibitors …

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Characterization of 2,4-Dianilinopyrimidines Against Five P. falciparum Kinases PfARK1, PfARK3, PfNEK3, PfPK9, and PfPKB

Krisha Avalani, Reena Zutshi, Emily R. Derbyshire, Christopher R. Mansfield et autres

Plasmodium kinases are increasingly recognized as potential novel antiplasmodial targets for the treatment of malaria, but only a small subset of these kinases have had structure-activity relationship (SAR) campaigns reported. Herein we report the discovery of CZC-54252 (1) as an inhibitor of …

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Investigation of a cryptic ligand binding site on Plasmodium falciparum Hsp90

Christopher R. Mansfield, Elizabeth L. Taggart, Michael E. Chirgwin, Emily R. Derbyshire

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Meet the Authors: Christopher R. Mansfield and Emily R. Derbyshire

Christopher R. Mansfield, Emily R. Derbyshire

Selective targeting of Plasmodium falciparum Hsp90 disrupts the 26S proteasome

Christopher R. Mansfield, Baiyi Quan, Michael E. Chirgwin, Benjamin J. Eduful et autres

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Characterization of 2,4-Dianilinopyrimidines Against Five P. falciparum Kinases PfARK1, PfARK3, PfNEK3, PfPK9, and PfPKB

Han Wee Ong, Chandi de Silva, Krisha Avalani, Frank E. Kwarcinski et autres

High Resolution Image Download MS PowerPoint Slide Plasmodium kinases are increasingly recognized as potential novel antiplasmodial targets for the treatment of malaria, but only a small subset of these kinases have had structure–activity relationship (SAR) campaigns reported. Herein we report the discovery …

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Characterization of 2,4-dianilinopyrimidines Against Five P. falciparum Kinases PfARK1, PfARK3, PfNEK3, PfPK9 and PfPKB

Han Wee Ong, Chandi de Silva, Krisha Avalani, Frank E. Kwarcinski et autres

Plasmodium kinases are increasingly recognized as potential novel antiplasmodial targets for the treatment of malaria, but only a small subset of these kinases have had structure-activity-relationship (SAR) campaigns reported. Herein we report the discovery of CZC-54252 (1) as an inhibitor of five …

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Synthesis and activity of β-carboline antimalarials targeting the Plasmodium falciparum heat shock 90 protein

Michael E. Chirgwin, Julia Gibbs, Brianna N. Kalaj, Sierra D. Durham et autres

A collection of β-carbolines based on the natural product harmine, a compound known to target the heat shock 90 protein of Plasmodium falciparum, was synthesized and tested for antimalarial activity and potential toxicity. Several of these novel compounds display promising bioactivity, providing …

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Labeling strategies to track protozoan parasite proteome dynamics

Christopher R. Mansfield, Michael E. Chirgwin, Emily R. Derbyshire

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Cover Feature: Chemoproteomics for Plasmodium Parasite Drug Target Discovery (ChemBioChem 16/2021)

Kuan‐Yi Lu, Christopher R. Mansfield, Michael C. Fitzgerald, Emily R. Derbyshire

Understanding drugs’ mechanism of action is integral to successful antimalarial drug development. Recent advances in chemoproteomic methods have created an avenue to globally profile drug targets in the Plasmodium parasites that cause malaria. Some of these strategies even allow direct measurement in …

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Chemoproteomics for Plasmodium Parasite Drug Target Discovery

Kuan‐Yi Lu, Christopher R. Mansfield, Michael C. Fitzgerald, Emily R. Derbyshire

Emerging Plasmodium parasite drug resistance is threatening progress towards malaria control and elimination. While recent efforts in cell-based, high-throughput drug screening have produced first-in-class drugs with promising activities against different Plasmodium life cycle stages, most of these antimalarial agents have elusive mechanisms …

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Evaluation of a Novel High-Definition PCR Multiplex Assay for Simultaneous Detection of Tick-Borne Pathogens in Human Clinical Specimens

Salika M. Shakir, Christopher R. Mansfield, Elizabeth D. Hays, Marc Roger Couturier et autres

, which were confirmed by the LDTs. There were 16 samples with discordant results compared to the LDT results, five of which were resolved by repeat testing on the TBP panel and bidirectional sequencing. Following discrepant resolution, the final PPA and NPA …

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