Nuclear protein 1 (NUPR1) inhibitor that suppresses NUPR1-dependent cancer growth in vitro and in vivo via necroptosis and ferroptosis induction.
ZZW-115 is a nuclear protein 1 (NUPR1) inhibitor that suppresses NUPR1-dependent cancer growth in vitro (IC50 from 0.84 μM/ANOR to 4.93 μM/HN14 among 11 pancreatic ductal adenocarcinoma cultures) and in mice in vivo (5 mg/kg q.d. or q.a.d. via i.p.) via necroptosis and ferroptosis induction. ZZW-115 blocks importins-mediated NUPR1 nuclear translocation by directly targeting NUPR1 nuclear location signal (NLS) region (Kd = 2.1 μM by calorimetric titration).
Cancer cells activate stress-response mechanisms to adapt themselves to a variety of stressful conditions. Among these protective mechanisms, those controlled by the stress-induced nuclear protein 1 (NUPR1 ) belong to the most conserved ones. NUPR1 is an 82-residue-long, monomeric, basic
The Journal of clinical investigation, 129(6), 2500-2513 (2019-03-29)
Intrinsically disordered proteins (IDPs) are emerging as attractive drug targets by virtue of their prevalence in various diseases including cancer. Drug development targeting IDPs is challenging because they have dynamical structure features and conventional drug design is not applicable. NUPR1
HCC is a highly lethal malignancy with Sorafenib as the only molecularly targeted drug. The multifunctional stress-associated protein, NUPR1, plays an essential role in controlling cell growth, migration, invasion and Sorafenib resistance in HCC. We report here that NUPR1 expression
Ferroptosis is a type of iron-dependent regulated cell death, representing an emerging disease-modulatory mechanism. Transcription factors play multiple roles in ferroptosis, although the key regulator for ferroptosis in iron metabolism remains elusive. Using NanoString technology, we identify NUPR1, a stress-inducible
Establishing the interactome of the cancer-associated stress protein Nuclear Protein 1 (NUPR1), we found that it binds to several hundreds of proteins, including proteins involved in nuclear translocation, DNA repair, and key factors of the SUMO pathway. We demonstrated that
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