The pharmacogenetics of carboxylesterases: CES1 and CES2 genetic variants and their clinical effect

Z Merali, S Ross, G Paré - Drug metabolism and drug interactions, 2014 - degruyter.com
Abstract Human carboxylesterase 1 (CES1) and carboxylesterase 2 (CES2) are serine
esterases responsible for the hydrolysis of ester and amide bonds present in a number of …

Guaianolide sesquiterpene lactones, a source to discover agents that selectively inhibit acute myelogenous leukemia stem and progenitor cells

Q Zhang, Y Lu, Y Ding, J Zhai, Q Ji, W Ma… - Journal of medicinal …, 2012 - ACS Publications
Small molecules that can selectively target cancer stem cells (CSCs) remain rare currently
and exhibit no common structural features. Here we report a series of guaianolide …

Potential therapeutic advantages of doxorubicin when activated by formaldehyde to function as a DNA adduct-forming agent

SM Cutts, A Rephaeli, A Nudelman… - Current topics in …, 2015 - ingentaconnect.com
Doxorubicin has been in use as a key anticancer drug for forty years, either as a single
agent or in combination chemotherapy. It functions primarily by interfering with …

A highly selective near infrared fluorescent probe for carboxylesterase 2 and its biological applications

XY Zhang, TT Liu, JH Liang, XG Tian… - Journal of Materials …, 2021 - pubs.rsc.org
Carboxylesterase 2 (CES 2) is a key enzyme in the activation of the prodrug irinotecan (CPT-
11) in the treatment against colorectal cancer and also has some relationship with the side …

Measuring human carboxylesterase 2 activity in pancreatic cancer patient-derived xenografts using a ratiometric fluorescent chemosensor

K Kailass, O Sadovski, M Capello, Y Kang… - Chemical …, 2019 - pubs.rsc.org
Irinotecan-based therapy is a common treatment for pancreatic cancer. To elicit its
anticancer activity, the drug requires first the hydrolysis action of the enzyme human …

Activation of DNA damage response pathways as a consequence of anthracycline-DNA adduct formation

RA Forrest, LP Swift, A Rephaeli, A Nudelman… - Biochemical …, 2012 - Elsevier
The cytotoxicity of doxorubicin, a clinically used anti-neoplastic drug, can be enhanced by
formaldehyde (either endogenous or exogenous) to promote the formation of doxorubicin …

Colloidal drug aggregate stability in high serum conditions and pharmacokinetic consequence

AN Ganesh, A Aman, J Logie, BL Barthel… - ACS chemical …, 2019 - ACS Publications
Colloidal drug aggregates have been a nuisance in drug screening, yet, because they
inherently comprise drug-rich particles, they may be useful in vivo if issues of stability can be …

Carboxylesterase-2 is a highly sensitive target of the antiobesity agent orlistat with profound implications in the activation of anticancer prodrugs

D Xiao, D Shi, D Yang, B Barthel, TH Koch… - Biochemical …, 2013 - Elsevier
Orlistat has been the most used anti-obesity drug and the mechanism of its action is to
reduce lipid absorption by inhibiting gastrointestinal lipases. These enzymes, like …

Synthesis and biological characterization of protease-activated prodrugs of doxazolidine

BL Barthel, DL Rudnicki, TP Kirby… - Journal of medicinal …, 2012 - ACS Publications
Doxazolidine (doxaz) is a new anthracycline anticancer agent. While structurally similar to
doxorubicin (dox), doxaz acts via a distinct mechanism to selectively enhance anticancer …

A rapidly metabolizable and enzyme-activated NIR fluorescent probe based on isophorone for imaging in vivo

W Kang, M Ma, S Tang, Y Wang, J Li, L Xu, P Ma… - Sensors and Actuators B …, 2024 - Elsevier
Near-infrared (NIR) fluorescent probes have excellent properties such as fast imaging
speed, non-invasive, good stability and low background interference, and have great …