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Chianelli, Donatella; Rucker, Paul V; Roland, Jason; Tully, David C; Nelson, John; Liu, Xiaodong; Bursulaya, Badry; Hernandez, Eloy D; Wu, Jane; Prashad, Mahavir; Schlama, Thierry; Liu, Yugang; Chu, Alan; Schmeits, James; Huang, David J; Hill, Robert; Bao, Dingjiu; Zoll, Jocelyn; Kim, Young; Groessl, Todd; McNamara, Peter; Liu, Bo; Richmond, Wendy; Sancho-Martinez, Ignacio; Phimister, Andrew; Seidel, H. Martin; Badman, Michael K; Joseph, Sean B; Laffitte, Bryan; Molteni, Valentina
Journal of medicinal chemistry, 04/2020, Letnik: 63, Številka: 8Journal Article
Farnesoid X receptor (FXR) agonists are emerging as important potential therapeutics for the treatment of nonalcoholic steatohepatitis (NASH) patients, as they exert positive effects on multiple aspects of the disease. FXR agonists reduce lipid accumulation in the liver, hepatocellular inflammation, hepatic injury, and fibrosis. While there are currently no approved therapies for NASH, the bile acid-derived FXR agonist obeticholic acid (OCA; 6-ethyl chenodeoxycholic acid) has shown promise in clinical studies. Previously, we described the discovery of tropifexor (LJN452), the most potent non-bile acid FXR agonist currently in clinical investigation. Here, we report the discovery of a novel chemical series of non-bile acid FXR agonists based on a tricyclic dihydrochromenopyrazole core from which emerged nidufexor (LMB763), a compound with partial FXR agonistic activity in vitro and FXR-dependent gene modulation in vivo. Nidufexor has advanced to Phase 2 human clinical trials in patients with NASH and diabetic nephropathy.
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Dostop do baze podatkov JCR je dovoljen samo uporabnikom iz Slovenije. Vaš trenutni IP-naslov ni na seznamu dovoljenih za dostop, zato je potrebna avtentikacija z ustreznim računom AAI.
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JCR | SNIP | JCR | SNIP | JCR | SNIP | JCR | SNIP |
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Povezave do osebnih bibliografij avtorjev | Povezave do podatkov o raziskovalcih v sistemu SICRIS |
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Vir: Osebne bibliografije
in: SICRIS
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