In vitro selection of mutant HDM2 resistant to nutlin inhibition

• Main Authors: Wei, Siau Jia., Joseph, Thomas., Sim, Adelene Y. L., Yurlova, Larisa., Zolghadr, Kourosh., Lane, David., Verma, Chandra., Ghadessy, Farid.
• Other Authors: School of Biological Sciences
• Format: Article
• Language: English
• Published: 2014
• Subjects: DRNTU::Science::Biological sciences
• Online Access: https://hdl.handle.net/10356/100150; http://hdl.handle.net/10220/18644; http://www.plosone.org/article/info%3Adoi%2F10.1371%2Fjournal.pone.0062564
• Institution: Nanyang Technological University

HDM2 binds to the p53 tumour suppressor and targets it for proteosomal degradation. Presently in clinical trials, the small molecule Nutlin-3A competitively binds to HDM2 and abrogates its repressive function. Using a novel in vitro selection methodology, we simulated the emergence of resistance by...