M
Martha Altieri
Publications - 5
Citations - 1356
Martha Altieri is an academic researcher. The author has contributed to research in topics: Proteolysis targeting chimera & Ubiquitin ligase. The author has an hindex of 2, co-authored 5 publications receiving 974 citations.
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Journal ArticleDOI
Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4
Jing Lu,Yimin Qian,Martha Altieri,Hanqing Dong,Jing Wang,Kanak Raina,John Hines,James D. Winkler,Andrew P. Crew,Kevin Coleman,Craig M. Crews +10 more
TL;DR: ARV-825 is designed, a hetero-bifunctional PROTAC (Proteolysis Targeting Chimera) that recruits BRD4 to the E3 ubiquitin ligase cereblon, leading to fast, efficient, and prolonged degradation ofBRD4 in all BL cell lines tested.
Journal ArticleDOI
PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer.
Kanak Raina,Jing Lu,Yimin Qian,Martha Altieri,Deborah M. Gordon,Ann Marie Rossi,Jing Wang,Xin Chen,Hanqing Dong,Kam W. Siu,James D. Winkler,Andrew P. Crew,Craig M. Crews,Kevin Coleman +13 more
TL;DR: This study proves that ARV-771, a small-molecule pan-BET degrader based on proteolysis-targeting chimera (PROTAC) technology, demonstrates dramatically improved efficacy in cellular models of CRPC as compared with BET inhibition.
Journal ArticleDOI
BRD4 Degradation By Protacs Represents a More Effective Therapeutic Strategy Than BRD4 Inhibitors in DLBCL
Jing Lu,Yimin Qian,Kanak Raina,Martha Altieri,Hanqing Dong,Jing Wang,Xin Chen,Andrew P. Crew,Kevin Coleman,Craig M. Crews,James D. Winkler +10 more
TL;DR: Hijacking E3 ubiquitin ligases, through PROTAC technology, is an innovative approach to achieve targeted, specific protein degradation that results in better downstream signaling suppression, more pronounced inhibition of proliferation and induction of apoptosis compared to the effects of small molecule inhibitors.
Proceedings ArticleDOI
Abstract LB-010: Hijacking the E3 ubiquitin ligase cereblon to create efficient BRD4 degraders
Jing Lu,Yimin Qian,Martha Altieri,Hanqing Dong,Jing Wang,Kanak Raina,Jim Winkler,AP Crew,Kevin Coleman,John Hines,Craig M. Crews +10 more
Journal ArticleDOI
BRD4 degraders produce long-lasting loss of BRD4 Ppotein and robust efficacy in Burkitt’s lymphoma cells.
Kevin Coleman,Jing Lu,Yimin Qian,Martha Altieri,Kanak Raina,Hanqing Dong,Jing Wang,John Hines,Andrew P. Crew,Craig M. Crews +9 more
TL;DR: The functional effects of BRD4 PROTACs were examined in several Burkitt’s lymphoma cell lines, comparing their effects to those observed with the clinical BRD 4 inhibitor OTX015, and it was found that treatment of cells with theBRD4 inhibitor OTx015 led to a rapid loss of BRd4.