JOSEPH, THOMAS LEONARD,VERMA, CHANDRA SHEKHAR,LANE, DAVID PHILLIP,BROWN, CHRISTOPHER JOHN
申请号:
EP13844064
公开号:
EP2904000A4
申请日:
2013.10.01
申请国别(地区):
EP
年份:
2016
代理人:
摘要:
By using a phage display derived peptide as an initial template, compounds have been developed that are highly specific against Mdm2/Mdm4. These compounds exhibit greater potency in p53 activation and protein-protein interaction assays than a compound derived from the p53 wild-type sequence. Unlike nutlin, a small molecule inhibitor of Mdm2/Mdm4, the phage derived compounds can arrest cells resistant to p53 induced apoptosis over a wide concentration range without cellular toxicity, suggesting they are highly suitable for cyclotherapy.