| Literature DB >> 28344039 |
Xiaoju Wang1, Yuanyuan Qiao2, Irfan A Asangani2, Bushra Ateeq3, Anton Poliakov2, Marcin Cieślik2, Sethuramasundaram Pitchiaya2, Balabhadrapatruni V S K Chakravarthi4, Xuhong Cao2, Xiaojun Jing2, Cynthia X Wang2, Ingrid J Apel2, Rui Wang2, Jean Ching-Yi Tien2, Kristin M Juckette2, Wei Yan2, Hui Jiang5, Shaomeng Wang6, Sooryanarayana Varambally7, Arul M Chinnaiyan8.
Abstract
Transcription factors play a key role in the development of diverse cancers, and therapeutically targeting them has remained a challenge. In prostate cancer, the gene encoding the transcription factor ERG is recurrently rearranged and plays a critical role in prostate oncogenesis. Here, we identified a series of peptides that interact specifically with the DNA binding domain of ERG. ERG inhibitory peptides (EIPs) and derived peptidomimetics bound ERG with high affinity and specificity, leading to proteolytic degradation of the ERG protein. The EIPs attenuated ERG-mediated transcription, chromatin recruitment, protein-protein interactions, cell invasion and proliferation, and tumor growth. Thus, peptidomimetic targeting of transcription factor fusion products may provide a promising therapeutic strategy for prostate cancer as well as other malignancies.Entities:
Keywords: ERG transcription factor; peptidomimetic inhibitor; prostate cancer
Mesh：
Substances：
Year: 2017 PMID： 28344039 PMCID： PMC5443258 DOI： 10.1016/j.ccell.2017.02.017
Source DB: PubMed Journal: Cancer Cell ISSN： 1535-6108 Impact factor: 31.743