E-viri
Recenzirano
Odprti dostop
-
Konteatis, Zenon; Artin, Erin; Nicolay, Brandon; Straley, Kimberly; Padyana, Anil K; Jin, Lei; Chen, Yue; Narayaraswamy, Rohini; Tong, Shuilong; Wang, Feng; Zhou, Ding; Cui, Dawei; Cai, Zhenwei; Luo, Zhiyong; Fang, Cheng; Tang, Huachun; Lv, Xiaobing; Nagaraja, Raj; Yang, Hua; Su, Shin-San M; Sui, Zhihua; Dang, Lenny; Yen, Katharine; Popovici-Muller, Janeta; Codega, Paolo; Campos, Carl; Mellinghoff, Ingo K; Biller, Scott A
ACS medicinal chemistry letters, 02/2020, Letnik: 11, Številka: 2Journal Article
Inhibitors of mutant isocitrate dehydrogenase (mIDH) 1 and 2 cancer-associated enzymes prevent the accumulation of the oncometabolite d-2-hydroxyglutarate (2-HG) and are under clinical investigation for the treatment of several cancers harboring an IDH mutation. Herein, we describe the discovery of vorasidenib (AG-881), a potent, oral, brain-penetrant dual inhibitor of both mIDH1 and mIDH2. X-ray cocrystal structures allowed us to characterize the compound binding site, leading to an understanding of the dual mutant inhibition. Furthermore, vorasidenib penetrates the brain of several preclinical species and inhibits 2-HG production in glioma tissue by >97% in an orthotopic glioma mouse model. Vorasidenib represents a novel dual mIDH1/2 inhibitor and is currently in clinical development for the treatment of low-grade mIDH glioma.
Avtor
Vnos na polico
Trajna povezava
- URL:
Faktor vpliva
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.
Leto | Faktor vpliva | Izdaja | Kategorija | Razvrstitev | ||||
---|---|---|---|---|---|---|---|---|
JCR | SNIP | JCR | SNIP | JCR | SNIP | JCR | SNIP |
Baze podatkov, v katerih je revija indeksirana
Ime baze podatkov | Področje | Leto |
---|
Povezave do osebnih bibliografij avtorjev | Povezave do podatkov o raziskovalcih v sistemu SICRIS |
---|
Vir: Osebne bibliografije
in: SICRIS
To gradivo vam je dostopno v celotnem besedilu. Če kljub temu želite naročiti gradivo, kliknite gumb Nadaljuj.