Structures of BCL-2 in complex with venetoclax reveal the molecular basis of resistance mutations
oleh: Richard W. Birkinshaw, Jia-nan Gong, Cindy S. Luo, Daisy Lio, Christine A. White, Mary Ann Anderson, Piers Blombery, Guillaume Lessene, Ian J. Majewski, Rachel Thijssen, Andrew W. Roberts, David C. S. Huang, Peter M. Colman, Peter E. Czabotar
| Format: | Article |
|---|---|
| Diterbitkan: | Nature Portfolio 2019-06-01 |
Deskripsi
The BCL-2 mutation G101V reduces venetoclax affinity and confers drug resistance in patients with chronic lymphocytic leukaemia. Here, the authors present crystal structures and biochemical analyses of venetoclax bound to BCL-2 and the G101V mutant, revealing the structural basis for venetoclax resistance.