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“Addition” and “Subtraction”: Selectivity Design for Type-II Maternal Embryonic Leucine Zipper Kinase Inhibitors

Chen, Xin and Giraldes, John and Sprague, Elizabeth and Shakya, Subarna and Chen, Zhuoliang and Wang, Kate and Joud-Caldwell, Carol and Mathieu, Simon and Chen, Christine and Straub, Christopher and Duca, Jose and Hurov, Kristen and Yuan, Yanqiu and Shao, Wenlin and Toure, Bakary-Barry (2017) “Addition” and “Subtraction”: Selectivity Design for Type-II Maternal Embryonic Leucine Zipper Kinase Inhibitors. Journal of Medicinal Chemistry, 60. pp. 2155-2161.

Abstract

While adding the structural features that are more favored by on-target activity is the more common strategy in selectivity optimization, the opposite strategy of subtracting the structural features that contribute more to off-target activity can also be very effective. Reported here is our successful effort of improving the kinase selectivity of type II maternal embryonic leucine zipper kinase inhibitors by applying these two complementary approaches together, which clearly demonstrates the powerful synergy between them.

Item Type: Article
Keywords: selectivity design, kinase inhibitor, MELK
Date Deposited: 12 Mar 2017 00:45
Last Modified: 12 Mar 2017 00:45
URI: https://oak.novartis.com/id/eprint/28818

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