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Hypoxia-activated prodrugs: paths forward in the era of personalised medicine
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 …
using bioreductive (hypoxia-activated) prodrugs that target antineoplastic agents to low …
Enzyme-catalyzed activation of anticancer prodrugs
M Rooseboom, JNM Commandeur… - Pharmacological …, 2004 - Elsevier
The rationale for the development of prodrugs relies upon delivery of higher concentrations
of a drug to target cells compared to administration of the drug itself. In the last decades …
of a drug to target cells compared to administration of the drug itself. In the last decades …
The chemical and biological activities of quinones: overview and implications in analytical detection
Quinones are a class of natural and synthetic compounds that have several beneficial
effects. Quinones are electron carriers playing a role in photosynthesis. As vitamins, they …
effects. Quinones are electron carriers playing a role in photosynthesis. As vitamins, they …
[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 …
tumors, which are an important cause of treatment resistance to conventional therapies …
Prodrug strategies in cancer therapy
WA Denny - European journal of medicinal chemistry, 2001 - Elsevier
Systemic cytotoxic (anti-proliferative) anticancer drugs rely primarily for their therapeutic
effect on cytokinetic differences between cancer and normal cells. One approach aimed at …
effect on cytokinetic differences between cancer and normal cells. One approach aimed at …
Bioreductive prodrugs as cancer therapeutics: targeting tumor hypoxia
Hypoxia, a state of low oxygen, is a common feature of solid tumors and is associated with
disease progression as well as resistance to radiotherapy and certain chemotherapeutic …
disease progression as well as resistance to radiotherapy and certain chemotherapeutic …
Molecular and cellular pharmacology of the hypoxia-activated prodrug TH-302
F Meng, JW Evans, D Bhupathi, M Banica… - Molecular cancer …, 2012 - aacrjournals.org
Abstract TH-302 is a 2-nitroimidazole triggered hypoxia-activated prodrug (HAP) of bromo-
isophosphoramide mustard currently undergoing clinical evaluation. Here, we describe …
isophosphoramide mustard currently undergoing clinical evaluation. Here, we describe …
Quinoxaline 1,4-di-N-Oxides: Biological Activities and Mechanisms of Actions
G Cheng, W Sa, C Cao, L Guo, H Hao, Z Liu… - Frontiers in …, 2016 - frontiersin.org
Quinoxaline 1, 4-di-N-oxides (QdNOs) have manifold biological properties, including
antimicrobial, antitumoral, antitrypanosomal and antiinflammatory/antioxidant activities …
antimicrobial, antitumoral, antitrypanosomal and antiinflammatory/antioxidant activities …
Taking advantage of tumor cell adaptations to hypoxia for develo** new tumor markers and treatment strategies
P Ebbesen, EO Pettersen, TA Gorr, G Jobst… - Journal of enzyme …, 2009 - Taylor & Francis
Cancer cells in hypoxic areas of solid tumors are to a large extent protected against the
action of radiation as well as many chemotherapeutic drugs. There are, however, two …
action of radiation as well as many chemotherapeutic drugs. There are, however, two …
Bioreductive drugs: from concept to clinic
SR McKeown, RL Cowen, KJ Williams - Clinical oncology, 2007 - Elsevier
One of the key issues for radiobiologists is the importance of hypoxia to the radiotherapy
response. This review addresses the reasons for this and primarily focuses on one aspect …
response. This review addresses the reasons for this and primarily focuses on one aspect …