Chemically diverse activity-based probes with unexpected inhibitory mechanisms targeting trypsin-like serine proteases

Autor: Alba Ramos-Llorca, Lisse Decraecker, Valérie M. Y. Cacheux, Irena Zeiburlina, Michelle De bruyn, Louise Battut, Carlos Moreno-Cinos, Davide Ceradini, Eric Espinosa, Gilles Dietrich, Maya Berg, Ingrid De Meester, Pieter Van Der Veken, Guy Boeckxstaens, Anne-Marie Lambeir, Alexandre Denadai-Souza, Koen Augustyns

Publikováno v: Frontiers in Chemistry, Vol 10 (2023)

Activity-based probes (ABP) are molecules that bind covalently to the active form of an enzyme family, making them an attractive tool for target and biomarker identification and drug discovery. The present study describes the synthesis and biochemica

Externí odkaz: https://doaj.org/article/084ad8fa8c424c0d8ed10c4e2a49fa74

Identification of Phenylpyrazolone Dimers as a New Class of Anti-Trypanosoma cruzi Agents

Autor: Louis Maes, Maria de Nazaré Correia Soeiro, Rob Leurs, Alba Ramos Llorca, Geert Jan Sterk, Lydia Stiny, Iwan J. P. de Esch, An Matheeussen, Maarten Sijm, Julianna Siciliano de Araújo, Kristina M. Orrling

Publikováno v: ChemMedChem, 14(18), 1662-1668. John Wiley and Sons Ltd
Sijm, M, Siciliano de Araújo, J, Ramos Llorca, A, Orrling, K, Stiny, L, Matheeussen, A, Maes, L, de Esch, I J P, de Nazaré Correia Soeiro, M, Sterk, G J & Leurs, R 2019, ' Identification of Phenylpyrazolone Dimers as a New Class of Anti-Trypanosoma cruzi Agents ', ChemMedChem, vol. 14, no. 18, pp. 1662-1668 . https://doi.org/10.1002/cmdc.201900370
ChemMedChem
Chemmedchem

Chagas disease is becoming a worldwide problem; it is currently estimated that over six million people are infected. The two drugs in current use, benznidazole and nifurtimox, require long treatment regimens, show limited efficacy in the chronic phas

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c2cbb02e74cb3733e8369cd7cbb4f3b0
https://research.vu.nl/en/publications/0fc16b36-d48a-4130-af08-17e6014afc5f