Discovery of novel enasidenib analogues targeting inhibition of mutant isocitrate dehydrogenase 2 as antileukaemic agents
Sign Up to like & getrecommendations! Published in 2023 at "Journal of Enzyme Inhibition and Medicinal Chemistry"
DOI: 10.1080/14756366.2022.2157411
Abstract: Abstract Mutant isocitrate dehydrogenase (IDH) 2 “IDH2m” acquires a neo-enzymatic activity reducing α-ketoglutarate to an oncometabolite, D-2-hydroxyglutarate (2-HG). Three s-triazine series were designed and synthesised using enasidenib as a lead compound. In vitro anticancer screening… read more here.
Keywords: mutant isocitrate; isocitrate dehydrogenase; inhibition; discovery novel ... See more keywords
Mutant Isocitrate Dehydrogenase Inhibitors as Targeted Cancer Therapeutics
Sign Up to like & getrecommendations! Published in 2019 at "Frontiers in Oncology"
DOI: 10.3389/fonc.2019.00417
Abstract: The identification of heterozygous neomorphic isocitrate dehydrogenase (IDH) mutations across multiple cancer types including both solid and hematologic malignancies has revolutionized our understanding of oncogenesis in these malignancies and the potential for targeted therapeutics using… read more here.
Keywords: dehydrogenase; dehydrogenase inhibitors; mutant isocitrate; isocitrate dehydrogenase ... See more keywords