RT Journal Article
T1 A strategic discovery roadmap towards high-quality leads and drug development candidates for kinetoplastid diseases. Part 2: from molecule to confirmed hit
A1 Hendrickx, Sarah
A1 Ilbeigi, Kayhan
A1 Thoré, Eli S J
A1 Bertram, Michael G
A1 Calvo-Alvarez, Estefanía
A1 Cintesun, Sener
A1 Olías-Molero, Ana Isabel
A1 Corral, María Jesús
A1 Mateo Barrientos, Marta
A1 Estaquier, Jérôme
A1 Pomel, Sébastien
A1 Alunda Rodríguez, José María
A1 Gul, Sheraz
A1 Van Bocxlaer, Katrien
A1 Frézard, Frédéric
A1 Tavares, Joana
A1 Cordeiro Da Silva, Anabela
A1 Costi, Maria Paola
A1 Maes, Louis
A1 Caljon, Guy
AB Given the medical importance and challenges related to kinetoplastid diseases, a strategic roadmap is needed for the identification of high-quality leads and drug development candidates. Within the aim to deliver more compelling proof-of-concept read-outs, this part proposes a systematic flow-chart of laboratory experiments and decision criteria, focusing on African trypanosomiasis, Chagas disease and visceral and cutaneous leishmaniasis. Next to precision experimental design and reporting, an overview is provided of various complementary laboratory models reproducing kinetoplastid infection and disease. Technical aspects of conventional in vitro and in vivo approaches and, more recently, in silico methods are presented with reference to specific preclinical R&D stages from ‘hit finding’ to ‘profiling of a confirmed hit’, covering the expertise areas of medicinal chemistry, primary pharmacology, (eco)toxicology, pharmacokinetics and pharmaceutics (Figure 1)
PB Oxford University Press
SN 0305-7453
YR 2026
FD 2026
LK https://hdl.handle.net/20.500.14352/134931
UL https://hdl.handle.net/20.500.14352/134931
LA eng
NO Hendrickx, S., Ilbeigi, K., Thoré, E. S. J., Bertram, M. G., Calvo-Alvarez, E., Cintesun, S., Olías-Molero, A. I., Corral, M. J., Mateo-Barrientos, M., Estaquier, J., Pomel, S., Alunda, J. M., Gul, S., Van Bocxlaer, K., Frézard, F., Tavares, J., Cordeiro Da Silva, A., Costi, M. P., Maes, L., & Caljon, G. (2026). A strategic discovery roadmap towards high-quality leads and drug development candidates for kinetoplastid diseases. Part 2: from molecule to confirmed hit. The Journal of antimicrobial chemotherapy, 81(4), dkag110. https://doi.org/10.1093/jac/dkag110
NO European Commission
NO Fonds Wetenschappelijk Onderzoek (FWO) Vlaanderen
NO Swedish Research Council Formas
NO Kempe Foundation
DS Docta Complutense
RD 28 abr 2026