1324010-65-2Relevant academic research and scientific papers
Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP
González-Lpez, Marcos,Welsh, Kate,Finlay, Darren,Ardecky, Robert J.,Ganji, Santhi Reddy,Su, Ying,Yuan, Hongbin,Teriete, Peter,MacE, Peter D.,Riedl, Stefan J.,Vuori, Kristiina,Reed, John C.,Cosford, Nicholas D.P.
, p. 4332 - 4336 (2011/08/06)
We report the systematic rational design and synthesis of new monovalent Smac mimetics that bind preferentially to the BIR2 domain of the anti-apoptotic protein XIAP. Characterization of compounds in vitro (including 9i; ML101) led to the determination of key structural requirements for BIR2 binding affinity. Compounds 9h and 9j sensitized TRAIL-resistant breast cancer cells to apoptotic cell death, highlighting the value of these probe compounds as tools to investigate the biology of XIAP.
