MiRNA-29a as a tumor suppressor mediates PRIMA-1Met-induced anti-myeloma activity by targeting c-Myc. [PDF]
Oncotarget, 2016 The proto-oncogene c-Myc plays substantial role in multiple myeloma (MM) pathogenesis and is considered a potential drug target. Here we provide evidence of a novel mechanism for PRIMA-1Met, a small molecule with anti-tumor activity in phase I/II clinical trial, showing that PRIMA-1Met induces apoptosis in MM cells by suppressing c-Myc and upregulating
Saha MN, Abdi J, Yang Y, Chang H.
europepmc +3 more sources
APR-246/PRIMA-1MET inhibits thioredoxin reductase 1 and converts the enzyme to a dedicated NADPH oxidase. [PDF]
Cell Death Dis, 2017 The low-molecular-weight compound APR-246 (PRIMA-1(MET)) restores wild-type conformation and function to mutant p53, and triggers apoptosis in tumor cells. We show here that APR-246 also targets the selenoprotein thioredoxin reductase 1 (TrxR1), a key regulator of cellular redox balance.
Peng X +7 more
europepmc +7 more sources
EXTH-50. THIOREDOXIN REDUCTASE1 AND MGMT SYNTHETIC LETHALITY ENHANCES CYTOTOXICITY OF PRIMA-1MET(APR-246) AND AURANOFIN IN GLIOBLASTOMA [PDF]
Neuro Oncol, 2019 Abstract Glioblastoma multiforme (GBM), the most common and advanced primary brain malignancy in adults remains an incurable disease, despite aggressive treatment with surgery, radiation therapy and chemoradiation using the alkylating agent, Temozolomide (TMZ).
Raveendrakumar R +6 more
europepmc +3 more sources
Cell Death and Disease, 2021 Asparaginase depletes extracellular asparagine in the blood and is an important treatment for acute lymphoblastic leukemia (ALL) due to asparagine auxotrophy of ALL blasts.
Sophia Ceder +12 more
doaj +1 more source
Identification of Eight Histone Methylation Modification Regulators Associated With Breast Cancer Prognosis. [PDF]
IET Syst BiolThis study developed a risk scoring model based on histone methylation modification regulators (HMMRs) to assess their role in breast cancer (BRCA) prognosis and drug sensitivity. The model, constructed using LASSO regression, identified eight key HMMRs associated with survival, which showed independent predictive values. Immune and functional analyses
Cao YN +6 more
europepmc +2 more sources
Photo‐oxygenation of histidine residue inhibits α‐synuclein aggregation
The FASEB Journal, Volume 37, Issue 12, December 2023., 2023 Under pathological conditions in synucleinopathies, α‐syn aggregates can act as “seeds” and enhance the further aggregation of α‐syn. However, the photo‐oxygenation, which is the addition of oxygen atoms to α‐syn aggregates by the light‐activated photocatalyst, can attenuate the seeding ability of α‐syn aggregates and inhibit the aggregation. The photo‐
Reito Nakamura +14 more
wiley +1 more source
Clinical Cardiology, Volume 45, Issue 8, Page 821-830, August 2022., 2022 Abstract Background and Hypothesis The rehabilitation effect of circuit resistance training in coronary heart disease (CHD) patients remains unclear. We perform this review to examine the rehabilitation effect of circuit resistance training in CHD patients and to provide a basis for the formulation of reasonable individual exercise prescriptions for ...
Chunchun Wu +6 more
wiley +1 more source
TP53 mutated glioblastoma stem-like cell cultures are sensitive to dual mTORC1/2 inhibition while resistance in TP53 wild type cultures can be overcome by combined inhibition of mTORC1/2 and Bcl-2 [PDF]
, 2016 Background: Glioblastoma is the most malignant tumor of the central nervous system and still lacks effective treatment. This study explores mutational biomarkers of 11 drugs targeting either the RTK/Ras/PI3K, the p53 or the Rb pathway using 25 patient ...
Besselink, N. (Nicolle) +17 more
core +5 more sources
Cerebrospinal fluid and plasma metabolomics of acute endurance exercise
The FASEB Journal, Volume 36, Issue 7, July 2022., 2022 Abstract Metabolomics has emerged as a powerful new tool in precision medicine. No studies have yet been published on the metabolomic changes in cerebrospinal fluid (CSF) produced by acute endurance exercise. CSF and plasma were collected from 19 young active adults (13 males and 6 females) before and 60 min after a 90‐min monitored outdoor run.
Kefeng Li +12 more
wiley +1 more source
Sensitivity to PRIMA-1MET is associated with decreased MGMT in human glioblastoma cells and glioblastoma stem cells irrespective of p53 status. [PDF]
Oncotarget, 2016 Alterations of the TP53 tumor suppressor gene occur in ~30% of primary glioblastoma (GBM) with a high frequency of missense mutations associated with the acquisition of oncogenic "gain-of-function" (GOF) mutant (mut)p53 activities. PRIMA-1MET/APR-246, emerged as a promising compound to rescue wild-type (wt)p53 function in different cancer types ...
Patyka M +5 more
europepmc +4 more sources