Mechanisms of activation of the transcription factor Nrf2 by redox stressors, nutrient cues, and energy status and the pathways through which it attenuates …

LE Tebay, H Robertson, ST Durant, SR Vitale… - Free Radical Biology …, 2015 - Elsevier
Abstract Nuclear factor-erythroid 2 p45-related factor 2 (Nrf2) regulates the basal and stress-
inducible expression of a battery of genes encoding key components of the glutathione …

Aldo-keto reductases and cancer drug resistance

TM Penning, S Jonnalagadda, PC Trippier… - Pharmacological …, 2021 - Elsevier
Human aldo-keto reductases (AKRs) catalyze the NADPH-dependent reduction of carbonyl
groups to alcohols for conjugation reactions to proceed. They are implicated in resistance to …

Targeting hypoxia in cancer therapy

WR Wilson, MP Hay - Nature Reviews Cancer, 2011 - nature.com
Hypoxia is a feature of most tumours, albeit with variable incidence and severity within a
given patient population. It is a negative prognostic and predictive factor owing to its multiple …

Hypoxia-activated prodrugs: paths forward in the era of personalised medicine

FW Hunter, BG Wouters, WR Wilson - British journal of cancer, 2016 - nature.com
Tumour hypoxia has been pursued as a cancer drug target for over 30 years, most notably
using bioreductive (hypoxia-activated) prodrugs that target antineoplastic agents to low …

[HTML][HTML] Hypoxia-activated prodrugs and (lack of) clinical progress: The need for hypoxia-based biomarker patient selection in phase III clinical trials

L Spiegelberg, R Houben, R Niemans… - Clinical and translational …, 2019 - Elsevier
Hypoxia-activated prodrugs (HAPs) are designed to specifically target the hypoxic cells of
tumors, which are an important cause of treatment resistance to conventional therapies …

Nitroreductase gene-directed enzyme prodrug therapy: insights and advances toward clinical utility

EM Williams, RF Little, AM Mowday, MH Rich… - Biochemical …, 2015 - portlandpress.com
This review examines the vast catalytic and therapeutic potential offered by type I (ie oxygen-
insensitive) nitroreductase enzymes in partnership with nitroaromatic prodrugs, with …

The bioreductive prodrug PR-104A is activated under aerobic conditions by human aldo-keto reductase 1C3

CP Guise, MR Abbattista, RS Singleton, SD Holford… - Cancer research, 2010 - AACR
PR-104, currently in phase II clinical trials, is a phosphate ester pre-prodrug which is
converted in vivo to its cognate alcohol, PR-104A, a prodrug designed to exploit tumor …

Overview of AKR1C3: inhibitor achievements and disease insights

Y Liu, S He, Y Chen, Y Liu, F Feng, W Liu… - Journal of medicinal …, 2020 - ACS Publications
Human aldo-keto reductase family 1 member C3 (AKR1C3) is known as a hormone activity
regulator and prostaglandin F (PGF) synthase that regulates the occupancy of hormone …

Pronounced hypoxia in models of murine and human leukemia: high efficacy of hypoxia-activated prodrug PR-104

J Benito, Y Shi, B Szymanska, H Carol, I Boehm, H Lu… - PloS one, 2011 - journals.plos.org
Recent studies indicate that interactions between leukemia cells and the bone marrow (BM)
microenvironment promote leukemia cell survival and confer resistance to anti-leukemic …

Aldo-keto reductase 1C3 expression in MCF-7 cells reveals roles in steroid hormone and prostaglandin metabolism that may explain its over-expression in breast …

MC Byrns, L Duan, SH Lee, IA Blair… - The Journal of steroid …, 2010 - Elsevier
Aldo-keto reductase (AKR) 1C3 (type 5 17β-hydroxysteroid dehydrogenase and
prostaglandin F synthase), may stimulate proliferation via steroid hormone and …