Kristin A Altwegg, Suryavathi Viswanadhapalli, Monica Mann, Dimple Chakravarty, Samaya Rajeshwari Krishnan, Zexuan Liu, Junhao Liu, Uday P Pratap, Behnam Ebrahimi, John R Sanchez, Xiaonan Li, Shihong Ma, Ben H Park, Bindu Santhamma, Yidong Chen, Zhao Lai, Ganesh V Raj, Yaxia Yuan, Daohong Zhou, Gangadhara R Sareddy, Rajeshwar R Tekmal, Stanton F McHardy, Tim Hui-Ming Huang, Manjeet K Rao, Hariprasad Vankayalapati, Ratna K Vadlamudi
Most patients with estrogen receptor alpha-positive breast cancers (ER+ BC) initially respond to treatment but eventually develop therapy resistance with disease progression. Overexpression of oncogenic ER coregulators, including proline, glutamic acid, and leucine-rich protein 1 (PELP1), are implicated in BC progression. The lack of small molecules that inhibits PELP1 represents a major knowledge gap. Here, using a yeast-two-hybrid screen, we identified novel peptide inhibitors of PELP1 (PIPs). Biochemical assays demonstrated that one of these peptides, PIP1, directly interacted with PELP1 to block PELP1 oncogenic functions...
August 11, 2022: Cancer Research