The concept of intrinsic versus extrinsic apoptosis

L Lossi - Biochemical Journal, 2022 - portlandpress.com
Regulated cell death is a vital and dynamic process in multicellular organisms that maintains
tissue homeostasis and eliminates potentially dangerous cells. Apoptosis, one of the better …

Biological and pharmacological roles of m6A modifications in cancer drug resistance

Z Liu, H Zou, Q Dang, H Xu, L Liu, Y Zhang, J Lv, H Li… - Molecular Cancer, 2022 - Springer
Cancer drug resistance represents the main obstacle in cancer treatment. Drug-resistant
cancers exhibit complex molecular mechanisms to hit back therapy under pharmacological …

Surmounting cancer drug resistance: New insights from the perspective of N6-methyladenosine RNA modification

B Li, J Jiang, YG Assaraf, H Xiao, ZS Chen… - Drug resistance …, 2020 - Elsevier
Despite the development of targeted therapy, drug resistance remains a primary hindrance
to curative treatment of various cancers. Among several novel approaches to overcome drug …

[HTML][HTML] ONC201 and imipridones: Anti-cancer compounds with clinical efficacy

VV Prabhu, S Morrow, AR Kawakibi, L Zhou, M Ralff… - Neoplasia, 2020 - Elsevier
ONC201 was originally discovered as TNF-Related Apoptosis Inducing Ligand (TRAIL)-
inducing compound TIC10. ONC201 appears to act as a selective antagonist of the G …

Combined strategies in structure-based virtual screening

Z Wang, H Sun, C Shen, X Hu, J Gao, D Li… - Physical Chemistry …, 2020 - pubs.rsc.org
The identification and optimization of lead compounds are inalienable components in drug
design and discovery pipelines. As a powerful computational approach for the identification …

First-in-human clinical trial of oral ONC201 in patients with refractory solid tumors

MN Stein, JR Bertino, HL Kaufman, T Mayer… - Clinical cancer …, 2017 - AACR
Purpose: ONC201 is a small-molecule selective antagonist of the G protein–coupled
receptor DRD2 that is the founding member of the imipridone class of compounds. A first-in …

ATF4 induction through an atypical integrated stress response to ONC201 triggers p53-independent apoptosis in hematological malignancies

JO Ishizawa, K Kojima, D Chachad, P Ruvolo… - Science …, 2016 - science.org
The clinical challenge posed by p53 abnormalities in hematological malignancies requires
therapeutic strategies other than standard genotoxic chemotherapies. ONC201 is a first-in …

[HTML][HTML] Discovery and clinical introduction of first-in-class imipridone ONC201

JE Allen, CLB Kline, VV Prabhu, J Wagner, J Ishizawa… - Oncotarget, 2016 - ncbi.nlm.nih.gov
ONC201 is the founding member of a novel class of anti-cancer compounds called
imipridones that is currently in Phase II clinical trials in multiple advanced cancers. Since the …

Therapeutic targeting of TRAIL death receptors

F Di Cristofano, A George, V Tajiknia… - Biochemical Society …, 2023 - portlandpress.com
The discovery of tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) along with
its potent and selective antitumor effects initiated a decades-long search for therapeutic …

Biological activity of weekly ONC201 in adult recurrent glioblastoma patients

I Arrillaga-Romany, Y Odia, VV Prabhu… - Neuro …, 2020 - academic.oup.com
Background ONC201 is a dopamine receptor D2 (DRD2) antagonist that penetrates the
blood–brain barrier. ONC201 efficacy has been shown in glioblastoma animal models and …