Article
Evaluating p97 inhibitor analogues for their domain selectivity and potency against the p97-p47 complex.
ChemMedChem - 1 Jan 2015
Fang Chen-Jie, Gui Lin, Zhang Xiaoyi, Moen Derek R, Li Kelin, Frankowski Kevin J, Lin Henry J, Schoenen Frank J, Chou Tsui-Fen
Abstract excerpt
We previously found that p97 ATPase inhibitors 2-(2-amino-1H-benzo[d]imidazol-1-yl)-N-benzyl-8-methoxyquinazolin-4-amine (ML240) and 2-(2H-benzo[b][1,4]oxazin-4(3H)-yl)-N-benzyl-5,6,7,8-tetrahydroquinazolin-4-amine (ML241) specifically target the D2 domain of wild-type p97. In addition, one of the major p97 cofactors, p47, decreases their potencies by ∼50-fold. In contrast, N(2) ,N(4)...
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