Enzyme-Activated Fluorogenic Probes for Live-Cell and in Vivo Imaging
Fluorogenic probes, small-molecule sensors that unmask brilliant fluorescence upon
exposure to specific stimuli, are powerful tools for chemical biology. Those probes that …
exposure to specific stimuli, are powerful tools for chemical biology. Those probes that …
Quinolone: a versatile therapeutic compound class
The discovery of nalidixic acid is one pinnacle in medicinal chemistry, which opened a new
area of research that has led to the discovery of several life-saving antimicrobial agents …
area of research that has led to the discovery of several life-saving antimicrobial agents …
Nitro-group-containing drugs
K Nepali, HY Lee, JP Liou - Journal of medicinal chemistry, 2018 - ACS Publications
The nitro group is considered to be a versatile and unique functional group in medicinal
chemistry. Despite a long history of use in therapeutics, the nitro group has toxicity issues …
chemistry. Despite a long history of use in therapeutics, the nitro group has toxicity issues …
[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 …
Bioreductive fluorescent imaging agents: applications to tumour hypoxia
RBP Elmes - Chemical Communications, 2016 - pubs.rsc.org
Large tumours contain regions with very low intracellular O2 concentrations. Known as
hypoxia, this feature of tumours yields a highly reducing environment owing to the presence …
hypoxia, this feature of tumours yields a highly reducing environment owing to the presence …
Engineering a multifunctional nitroreductase for improved activation of prodrugs and PET probes for cancer gene therapy
Gene-directed enzyme-prodrug therapy (GDEPT) is a promising anti-cancer strategy.
However, inadequate prodrugs, inefficient prodrug activation, and a lack of non-invasive …
However, inadequate prodrugs, inefficient prodrug activation, and a lack of non-invasive …
Identification of P450 oxidoreductase as a major determinant of sensitivity to hypoxia-activated prodrugs
Hypoxia is a prevalent feature of many tumors contributing to disease progression and
treatment resistance, and therefore constitutes an attractive therapeutic target. Several …
treatment resistance, and therefore constitutes an attractive therapeutic target. Several …
The role of bystander effects in the antitumor activity of the hypoxia-activated prodrug PR-104
A Foehrenbacher, K Patel, MR Abbattista… - Frontiers in …, 2013 - frontiersin.org
Activation of prodrugs in tumors (eg, by bioreduction in hypoxic zones) has the potential to
generate active metabolites that can diffuse within the tumor microenvironment. Such …
generate active metabolites that can diffuse within the tumor microenvironment. Such …
Multifunctional probe based on cationic conjugated polymers for nitroreductase-related analysis: sensing, hypoxia diagnosis, and imaging
X Zhang, Q Zhao, Y Li, X Duan, Y Tang - Analytical chemistry, 2017 - ACS Publications
Nitroreductase (NTR) is overexpressed in hypoxic tumors. Moreover, hypoxia is usually
considered as the most important feature of various diseases. Thus, it is important to build a …
considered as the most important feature of various diseases. Thus, it is important to build a …
Dual targeting of hypoxia and homologous recombination repair dysfunction in triple-negative breast cancer
Triple-negative breast cancer (TNBC) is an aggressive malignancy with poor clinical
outcome and few validated drug targets. Two prevalent features of TNBC, tumor hypoxia and …
outcome and few validated drug targets. Two prevalent features of TNBC, tumor hypoxia and …