Journal of Medicinal Chemistry p. 7371 - 7392 (2017)
Update date:2022-08-16
Topics:
Joncour, Agnès
Desroy, Nicolas
Housseman, Christopher
Bock, Xavier
Bienvenu, Natacha
Cherel, La?titia
Labeguere, Virginie
Peixoto, Christophe
Annoot, Denis
Lepissier, Luce
Heiermann, J?rg
Hengeveld, Willem Jan
Pilzak, Gregor
Monjardet, Alain
Wakselman, Emanuelle
Roncoroni, Veronique
Le Tallec, Sandrine
Galien, René
David, Christelle
Vandervoort, Nele
Christophe, Thierry
Conrath, Katja
Jans, Mia
Wohlkonig, Alexandre
Soror, Sameh
Steyaert, Jan
Touitou, Robert
Fleury, Damien
Vercheval, Lionel
Mollat, Patrick
Triballeau, Nicolas
Van Der Aar, Ellen
Brys, Reginald
Heckmann, Bertrand
Autotaxin (ATX) is a secreted enzyme playing a major role in the production of lysophosphatidic acid (LPA) in blood through hydrolysis of lysophosphatidyl choline (LPC). The ATX-LPA signaling axis arouses a high interest in the drug discovery industry as it has been implicated in several diseases including cancer, fibrotic diseases, and inflammation, among others. An imidazo[1,2-a]pyridine series of ATX inhibitors was identified out of a high-throughput screening (HTS). A cocrystal structure with one of these compounds and ATX revealed a novel binding mode with occupancy of the hydrophobic pocket and channel of ATX but no interaction with zinc ions of the catalytic site. Exploration of the structure-activity relationship led to compounds displaying high activity in biochemical and plasma assays, exemplified by compound 40. Compound 40 was also able to decrease the plasma LPA levels upon oral administration to rats.
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