Design, synthesis and modelling of photoreactive chemical probes for investigating target engagement of plasmepsin IX and X in <i>Plasmodium falciparum</i>-Reference-Cited by-同舟云学术

Design, synthesis and modelling of photoreactive chemical probes for investigating target engagement of plasmepsin IX and X in Plasmodium falciparum

Published:2024 Issue:1 Volume:5 Page:19-29
ISSN:2633-0679
Container-title:RSC Chemical Biology
language:en
Short-container-title:RSC Chem. Biol.

Author:

Lisauskaitė Monika¹^ORCID,Nixon Gemma L.¹^ORCID,Woodley Christopher M.¹^ORCID,Berry Neil G.¹^ORCID,Coninckx Andy¹^ORCID,Qie L. Charlie¹^ORCID,Leung Suet C.¹,Taramelli Donatella²³^ORCID,Basilico Nicoletta⁴³^ORCID,Parapini Silvia⁵³^ORCID,Ward Stephen A.⁶^ORCID,Vadas Oscar⁷^ORCID,Soldati-Favre Dominique⁷^ORCID,Hong W. David¹^ORCID,O'Neill Paul M.¹^ORCID

Affiliation:

1. Department of Chemistry, University of Liverpool, Liverpool, L69 7ZD, UK

2. Dipartimento di Scienze Farmacologiche e Biomolecolari (DISFEB), Università degli Studi di Milano, 20133, Milano, Italy

3. Affiliated to Centro Interuniversitario di Ricerche sulla Malaria/Italian Malaria Network (CIRM-IMN), Università degli Studi di Camerino, Italy

4. Dipartimento di Scienze Biomediche, Chirurgiche e Odontoiatriche, Università degli Studi di Milano, 20133, Milano, Italy

5. Dipartimento di Scienze Biomediche per la Salute, Università degli Studi di Milano, 20133, Milano, Italy

6. Department of Tropical Disease Biology, Liverpool School of Tropical Medicine, Liverpool, L3 5QA, UK

7. Department of Microbiology and Molecular Medicine, Faculty of Medicine, CMU, 1 rue Michel-Servet, CH-1211 Genève 4, Switzerland

Abstract

We report the synthesis and biological profiling of photoreactive chemical probes based on an established plasmepsin X inhibitor scaffold. Maintained antimalarial and recombinant enzyme activity support their use in future chemical proteomic studies.

Funder

Medical Research Council

Engineering and Physical Sciences Research Council

Publisher

Royal Society of Chemistry (RSC)

Subject

Biochemistry, Genetics and Molecular Biology (miscellaneous),Molecular Biology,Biochemistry,Chemistry (miscellaneous)

Link

http://pubs.rsc.org/en/content/articlepdf/2024/CB/D3CB00109A

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2. Malaria in 2022: Increasing challenges, cautious optimism