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Structure-Activity Relationship of Azaindole-Based Glucokinase Activators.
Paczal A, Bálint B, Wéber C, Szabó ZB, Ondi L, Theret I, De Ceuninck F, Bernard C, Ktorza A, Perron-Sierra F, Kotschy A. Paczal A, et al. Among authors: ktorza a. J Med Chem. 2016 Jan 28;59(2):687-706. doi: 10.1021/acs.jmedchem.5b01594. Epub 2016 Jan 15. J Med Chem. 2016. PMID: 26685731
Small molecule glucokinase activators disturb lipid homeostasis and induce fatty liver in rodents: a warning for therapeutic applications in humans.
De Ceuninck F, Kargar C, Ilic C, Caliez A, Rolin JO, Umbdenstock T, Vinson C, Combettes M, de Fanti B, Harley E, Sadlo M, Lefèvre AL, Broux O, Wierzbicki M, Fourquez JM, Perron-Sierra F, Kotschy A, Ktorza A. De Ceuninck F, et al. Among authors: ktorza a. Br J Pharmacol. 2013 Jan;168(2):339-53. doi: 10.1111/j.1476-5381.2012.02184.x. Br J Pharmacol. 2013. PMID: 22925001 Free PMC article.
S 50131 and S 51434, two novel small molecule glucokinase activators, lack chronic efficacy despite potent acute antihyperglycaemic activity in diabetic mice.
De Ceuninck F, Kargar C, Charton Y, Goldstein S, Perron-Sierra F, Ilic C, Caliez A, Rolin JO, Sadlo M, Harley E, Vinson C, Ktorza A. De Ceuninck F, et al. Among authors: ktorza a. Br J Pharmacol. 2013 Jul;169(5):999-1010. doi: 10.1111/bph.12172. Br J Pharmacol. 2013. PMID: 23488540 Free PMC article.
Anti-diabetic activity of fused PPARγ-SIRT1 ligands with limited body-weight gain by mimicking calorie restriction and decreasing SGK1 expression.
Pirat C, Dacquet C, Leclerc V, Hennuyer N, Beucher-Gaudin M, Zanirato G, Géant A, Staels B, Ktorza A, Farce A, Caignard DH, Berthelot P, Lebegue N. Pirat C, et al. Among authors: ktorza a. Eur J Med Chem. 2017 Sep 8;137:310-326. doi: 10.1016/j.ejmech.2017.06.006. Epub 2017 Jun 12. Eur J Med Chem. 2017. PMID: 28609708
109 results