Identification of Plasmodium dipeptidyl aminopeptidase allosteric inhibitors by high throughput screening.

Autor: Mateo I Sanchez, Laura E de Vries, Christine Lehmann, Jeong T Lee, Kenny K Ang, Christopher Wilson, Steven Chen, Michelle R Arkin, Matthew Bogyo, Edgar Deu

Publikováno v: PLoS ONE, Vol 14, Iss 12, p e0226270 (2019)

Dipeptidyl aminopeptidases (DPAPs) are cysteine proteases that cleave dipeptides from the N-terminus of protein substrates and have been shown to play important roles in many pathologies including parasitic diseases such as malaria, toxoplasmosis and

Externí odkaz: https://doaj.org/article/bf56062846c6498e9b0850535a2beef1

Preclinical characterization and target validation of the antimalarial pantothenamide MMV693183

Autor: Laura E. de Vries, Patrick A. M. Jansen, Catalina Barcelo, Justin Munro, Julie M. J. Verhoef, Charisse Flerida A. Pasaje, Kelly Rubiano, Josefine Striepen, Nada Abla, Luuk Berning, Judith M. Bolscher, Claudia Demarta-Gatsi, Rob W. M. Henderson, Tonnie Huijs, Karin M. J. Koolen, Patrick K. Tumwebaze, Tomas Yeo, Anna C. C. Aguiar, Iñigo Angulo-Barturen, Alisje Churchyard, Jake Baum, Benigno Crespo Fernández, Aline Fuchs, Francisco-Javier Gamo, Rafael V. C. Guido, María Belén Jiménez-Diaz, Dhelio B. Pereira, Rosemary Rochford, Camille Roesch, Laura M. Sanz, Graham Trevitt, Benoit Witkowski, Sergio Wittlin, Roland A. Cooper, Philip J. Rosenthal, Robert W. Sauerwein, Joost Schalkwijk, Pedro H. H. Hermkens, Roger V. Bonnert, Brice Campo, David A. Fidock, Manuel Llinás, Jacquin C. Niles, Taco W. A. Kooij, Koen J. Dechering

Publikováno v: Nature Communications, 13, 1, pp. 1-16
Repositório Institucional da USP (Biblioteca Digital da Produção Intelectual)
Universidade de São Paulo (USP)
instacron:USP
Nature Communications, 13, 1-16
Nature Communications
Nature Communications, 2022, 13 (1), pp.2158. ⟨10.1038/s41467-022-29688-5⟩

Drug resistance and a dire lack of transmission-blocking antimalarials hamper malaria elimination. Here, we present the pantothenamide MMV693183 as a first-in-class acetyl-CoA synthetase (AcAS) inhibitor to enter preclinical development. Our studies

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a296a6f9baaf68a6d3f6fcb59ee269b9
https://repository.ubn.ru.nl/handle/2066/249501

Identification of Plasmodium dipeptidyl aminopeptidase allosteric inhibitors by high throughput screening

Autor: Kenny K. H. Ang, Michelle R. Arkin, Matthew Bogyo, Edgar Deu, Steven Chen, Laura E. de Vries, Mateo I. Sánchez, Christine Lehmann, Jeong T. Lee, Christopher W. Wilson

Publikováno v: PLoS ONE
PLoS ONE, Vol 14, Iss 12, p e0226270 (2019)
PloS one, vol 14, iss 12
PLoS One, 14
PLoS One, 14, 12

Dipeptidyl aminopeptidases (DPAPs) are cysteine proteases that cleave dipeptides from the N-terminus of protein substrates and have been shown to play important roles in many pathologies including parasitic diseases such as malaria, toxoplasmosis and

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::45daf4ad479991a5fd22b48251f2bf39
http://europepmc.org/articles/PMC6919601

Characterization of P. falciparum dipeptidyl aminopeptidase 3 specificity identifies differences in amino acid preferences between peptide-based substrates and covalent inhibitors

Autor: Marcin Drag, Fang Yuan, Katarzyna Groborz, Martin Horn, Edgar Deu, Chrislaine Withers-Martinez, Laurie Kuppens, Neysa Nevins, Shirin Arastu-Kapur, Matthew Bogyo, Michael Mareš, Mateo I. Sánchez, Christine Lehmann, David Jonathan Hirst, Marcin Poreba, Laura E. de Vries

Publikováno v: FEBS Journal, 286, 20, pp. 3998-4023
The Febs Journal
FEBS Journal, 286, 3998-4023

Malarial dipeptidyl aminopeptidases (DPAPs) are cysteine proteases important for parasite development thus making them attractive drug targets. In order to develop inhibitors specific to the parasite enzymes, it is necessary to map the determinants o

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::119003c3d9face13e10fdaba3ed3a2db
https://hdl.handle.net/2066/209409

Antimalarial pantothenamide metabolites target acetyl-coenzyme A biosynthesis in

Autor: Joost, Schalkwijk, Erik L, Allman, Patrick A M, Jansen, Laura E, de Vries, Julie M J, Verhoef, Suzanne, Jackowski, Peter N M, Botman, Christien A, Beuckens-Schortinghuis, Karin M J, Koolen, Judith M, Bolscher, Martijn W, Vos, Karen, Miller, Stacy A, Reeves, Helmi, Pett, Graham, Trevitt, Sergio, Wittlin, Christian, Scheurer, Sibylle, Sax, Christoph, Fischli, Iñigo, Angulo-Barturen, Mariá Belén, Jiménez-Diaz, Gabrielle, Josling, Taco W A, Kooij, Roger, Bonnert, Brice, Campo, Richard H, Blaauw, Floris P J T, Rutjes, Robert W, Sauerwein, Manuel, Llinás, Pedro H H, Hermkens, Koen J, Dechering

Publikováno v: Science translational medicine. 11(510)

Malaria eradication is critically dependent on new therapeutics that target resistant

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::841dc2b1d75efe5c50f2f7949ba194d8
https://pubmed.ncbi.nlm.nih.gov/33568524