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WR1065 conjugated to thiol-PEG polymers as novel anticancer prodrugs: broad spectrum efficacy, synergism, and drug resistance reversal.
Front Oncol
July 2023
Department of Pathology and Laboratory Medicine, Redox Biology and Pathology Program, Larner College of Medicine, University of Vermont, Burlington, VT, United States.
The lack of anticancer agents that overcome innate/acquired drug resistance is the single biggest barrier to achieving a durable complete response to cancer therapy. To address this issue, a new drug family was developed for intracellular delivery of the bioactive aminothiol WR1065 by conjugating it to discrete thiol-PEG polymers: 4-star-PEG-S-S-WR1065 (4SP65) delivers four WR1065s/molecule and m-PEG-S-S-WR1065 (1LP65) delivers one. Infrequently, WR1065 has exhibited anticancer effects when delivered via the FDA-approved cytoprotectant amifostine, which provides one WR1065/molecule extracellularly.
View Article and Find Full Text PDFDetermination of plasma levels of the active thiol form of the direct-acting PrC-210 ROS-scavenger using a fluorescence-based assay.
Anal Biochem
March 2021
Wisconsin Institutes of Medical Research, University of Wisconsin-Madison, Madison, WI, USA. Electronic address:
PrC-210 is a direct-acting ROS-scavenger. It's active when administered orally, IV, or topically; it has none of the nausea/emesis nor hypotension side effects that have precluded human amifostine use. PrC-210 confers 100% survival to mice and rats that received an otherwise 100% lethal radiation dose and 36% reduction of ischemia-reperfusion-induced mouse myocardial infarct damage, and thus is a viable candidate to prevent human ROS-induced ischemia-reperfusion and ionizing radiation toxicities.
View Article and Find Full Text PDFThe efficacy and safety of amifostine for the acute radiation syndrome.
Expert Opin Drug Saf
November 2019
Tech Micro Services , Bethesda , MD , USA.
: A radiation countermeasure that can be used prior to radiation exposure to protect the population from the harmful effects of radiation exposure remains a major unmet medical need and is recognized as an important area for research. Despite substantial advances in the research and development for finding nontoxic, safe, and effective prophylactic countermeasures for the acute radiation syndrome (ARS), no such agent has been approved by the United States Food and Drug Administration (FDA). : Despite the progress made to improve the effectiveness of amifostine as a radioprotector for ARS, none of the strategies have resolved the issue of its toxicity/side effects.
View Article and Find Full Text PDFManaging myocardial infarction (MI) to reduce cardiac cell death relies primarily on timely reperfusion of the affected coronary site, but reperfusion itself induces cell death through a toxic, ROS-mediated process. In this study, we determined whether the PrC-210 aminothiol ROS-scavenger could prevent ROS-induced damage in post-MI hearts. In a series of both in vitro and in vivo experiments, we show that: (a) in vitro, PrC-210 was the most potent and effective ROS-scavenger when functionally compared to eight of the most commonly studied antioxidants in the MI literature, (b) in vitro PrC-210 ROS-scavenging efficacy was both immediate (seconds) and long-lasting (hours), which would make it effective in both (1) (), as post-MI or cardiac surgery hearts are reperfused with PrC-210-containing blood, and (2) (s) as hearts are bathed with systemic PrC-210 after MI or surgery, (c) systemic PrC-210 caused a significant 36% reduction of mouse cardiac muscle death following a 45-minute cardiac IR insult; in a striking coincidence, the PrC-210 36% reduction in cardiac muscle death equals the 36% of the MI-induced cardiac cell death estimated 6 years ago by Ovize and colleagues to result from "reperfusion injury," (d) hearts in PrC-210-treated mice performed better than controls after heart attacks when functionally analyzed using echocardiography, and (e) the PrC-210 ROS-scavenging mechanism of action was corroborated by its ability to prevent >85% of the direct, HO-induced killing of neonate cardiomyocytes in cell culture.
View Article and Find Full Text PDFRole of drugs in the prevention and amelioration of radiation induced toxic effects.
Eur J Pharmacol
January 2018
School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, India. Electronic address:
As the use of radiation technology for nuclear warfare or for the benefits of mankind (e.g. in radiotherapy or radio-diagnosis) is increasing tremendously, the risk of associated side effects is becoming a cause of concern.
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