Hypoxia-targeted drug delivery
Hypoxia is a state of low oxygen tension found in numerous solid tumours. It is typically
associated with abnormal vasculature, which results in a reduced supply of oxygen and …
associated with abnormal vasculature, which results in a reduced supply of oxygen and …
Targeting hypoxia: hypoxia-activated prodrugs in cancer therapy
Y Li, L Zhao, XF Li - Frontiers in Oncology, 2021 - frontiersin.org
Hypoxia is an important characteristic of most solid malignancies, and is closely related to
tumor prognosis and therapeutic resistance. Hypoxia is one of the most important factors …
tumor prognosis and therapeutic resistance. Hypoxia is one of the most important factors …
Targeting hypoxia in solid and haematological malignancies
B Harris, S Saleem, N Cook, E Searle - Journal of Experimental & Clinical …, 2022 - Springer
Tumour hypoxia is a known and extensively researched phenomenon that occurs in both
solid and haematological malignancies. As cancer cells proliferate, demand for oxygen can …
solid and haematological malignancies. As cancer cells proliferate, demand for oxygen can …
[HTML][HTML] Bioreductive prodrugs as cancer therapeutics: targeting tumor hypoxia
CP Guise, AM Mowday, A Ashoorzadeh… - Chinese journal of …, 2014 - ncbi.nlm.nih.gov
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, L Lan… - Molecular cancer …, 2012 - AACR
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 …
Cytochrome P450-activated prodrugs
PR Ortiz de Montellano - Future medicinal chemistry, 2013 - Taylor & Francis
A prodrug is a compound that has negligible, or lower, activity against a specified
pharmacological target than one of its major metabolites. Prodrugs can be used to improve …
pharmacological target than one of its major metabolites. Prodrugs can be used to improve …
Selective tumor hypoxia targeting by hypoxia-activated prodrug TH-302 inhibits tumor growth in preclinical models of cancer
JD Sun, Q Liu, J Wang, D Ahluwalia, D Ferraro… - Clinical cancer …, 2012 - AACR
Purpose: Tumor hypoxia underlies treatment failure and yields a more aggressive, invasive,
and metastatic cancer phenotype. TH-302 is a 2-nitroimidazole triggered hypoxia-activated …
and metastatic cancer phenotype. TH-302 is a 2-nitroimidazole triggered hypoxia-activated …
Nitroreductase gene-directed enzyme prodrug therapy: insights and advances toward clinical utility
This review examines the vast catalytic and therapeutic potential offered by type I (ie oxygen-
insensitive) nitroreductase enzymes in partnership with nitroaromatic prodrugs, with …
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 …
converted in vivo to its cognate alcohol, PR-104A, a prodrug designed to exploit tumor …
Targeting hypoxic tumour cells to overcome metastasis
KL Bennewith, S Dedhar - BMC cancer, 2011 - Springer
The microenvironment within solid tumours can influence the metastatic dissemination of
tumour cells, and recent evidence suggests that poorly oxygenated (hypoxic) cells in primary …
tumour cells, and recent evidence suggests that poorly oxygenated (hypoxic) cells in primary …