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Lee Yujin,Jang Jiyoon,Bibi Maimoona,Duggirala Krishna Babu,Ji Sang Hee,Lee Ji Hun,Ahn Sunjoo,Song Jin Sook,Chae Chong Hak,Kim Seong Hwan,Lee Kwangho 대한화학회 2021 Bulletin of the Korean Chemical Society Vol.42 No.6
Apoptosis signal-regulating kinase 1 (ASK1) is a member of mitogen-activated protein kinase kinase kinase (MAP3K) family that involves downstream phosphorylation of MAP kinases, c-Jun N-terminal kinases, and p38 MAP kinases. ASK1 inhibitors could possibly be beneficial for ameliorating the development and progression of diseases. Especially, ASK1 has been of interest as one of therapeutic targets for nonalcoholic fatty liver disease as the most common chronic liver diseases including simple steatosis and nonalcoholic steatohepatitis. In this manuscript, novel ASK1 inhibitor lead KTA-29 which has an imidazo [1,2-b]pyridazine core with novel C6-bicycloheptaneimidazole is disclosed. With the novel imidazo[1,2-b] pyridazine core, structure-activity-relationship study for ASK1 potency is described and KTA-29 affinity toward ASK1 with molecular modeling study is explained.
Identification of TRD-35 as Potent and Selective DRAK2 Inhibitor
Imran Ali,Sangjun Park,정명은,Nari Lee,Maimoona Bibi,채종학,양경민,김성진,Gildon Choi,이광호 대한화학회 2020 Bulletin of the Korean Chemical Society Vol.41 No.5
Proposed binding mode of TRD-35 (thick cyan sticks) in the DRAK2.