?Addition? and ?Subtraction? [electronic resource] : Selectivity Design for Type II Maternal Embryonic Leucine Zipper Kinase Inhibitors

• Ngôn ngữ: eng
• Ký hiệu phân loại: 547 Organic chemistry
• Thông tin xuất bản: Argonne, Ill. : Oak Ridge, Tenn. : Argonne National Laboratory ; Distributed by the Office of Scientific and Technical Information, U.S. Dept. of Energy, 2017
• Mô tả vật lý: Size: p. 2155-2161 : , digital, PDF file.
• Bộ sưu tập: Metadata
• ID: 260644
• Chủ đề: 1. 37 inorganic, organic, physical, and analytical chemistry; 2. 60 applied life sciences; 3. Amides; 4. Mixtures; 5. Peptides and proteins; 6. Salts; 7. Selectivity

Tóm tắt

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. Furthermore, 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.