Advertisement

Topics

Structure-activity and structure-property relationships of novel Nrf2 activators with a 1,2,4-oxadiazole core and their therapeutic effects on acetaminophen (APAP)-induced acute liver injury.

08:00 EDT 28th August 2018 | BioPortfolio

Summary of "Structure-activity and structure-property relationships of novel Nrf2 activators with a 1,2,4-oxadiazole core and their therapeutic effects on acetaminophen (APAP)-induced acute liver injury."

The antioxidant function induced by Nrf2 protects the liver from damage. We found a novel Nrf2 activator named compound 25 via structural modification of compound 1 we previously reported. In vitro, compound 25 induced Nrf2 transport into the nucleus and protected hepatocyte L02 cells from APAP-induced cytotoxicity via activating the Nrf2-ARE signaling pathway. In vivo, 25 exhibited therapeutic effects in a mouse model of acute liver injury induced by acetaminophen (APAP) by up-regulating Nrf2-dependent antioxidases and down-regulating liver injury markers in serum. Together, these results indicated that 25 is a potent Nrf2/ARE activator both in vitro and in vivo. The drug-like properties of compound 25 further revealed its potential for development as a therapeutic drug against acute liver injury.

Affiliation

Journal Details

This article was published in the following journal.

Name: European journal of medicinal chemistry
ISSN: 1768-3254
Pages: 1376-1394

Links

DeepDyve research library

PubMed Articles [22306 Associated PubMed Articles listed on BioPortfolio]

Local collaborations for physical activity promotion: a network analysis.

This study aims to describe a local network for physical activity promotion and identify factors associated to collaboration or partnership ties between its actors. The study was carried out in a dist...

Current Approaches for Choosing Feature Selection and Learning Algorithms in Quantitative Structure-Activity Relationships (QSAR).

Quantitative structure-activity/property relationships (QSAR/QSPR) are statistical models which quantitatively correlate quantitative chemical structure information (described as molecular descriptors...

Structure-Activity and Structure-Toxicity Relationships of Novel Peptoid-Based Histone Deacetylase Inhibitors with Dual-Stage Antiplasmodial Activity.

Novel malaria intervention strategies are of great importance due to the development of drug resistance in malaria endemic countries. In this regard, histone deacetylases (HDACs) have emerged as new a...

Conformation-independent quantitative structure-property relationships study on water solubility of pesticides.

Water solubility is a key physicochemical parameter in pesticide control and regulation, although sometimes its experimental determination is not an easy task. In this study, we present Quantitative S...

Author Correction: Attraction Pheromone of The Benthic Diatom Seminavis robusta: Studies on Structure-Activity Relationships.

The original version of this article unfortunately contained a mistake. The chemical structure of compound 6 in Fig. 1 was incorrect. The tested compound 6 in this study was (3S,8aS)-3-isobutylhexahy...

Clinical Trials [4506 Associated Clinical Trials listed on BioPortfolio]

A New Interdisciplinary Collaboration Structure to Improve Medication Safety in the Elderly

Suboptimal use of medications among geriatric patients is well-known problem and leads to medication errors, re-hospitalizations and death. By using a randomized controlled trial (RCT) des...

Open Access Database of Standing Full Body Radiographs in Asymptomatic Volunteers

A study of the skeletal structure and how the structure changes over time. The aim of the study is to evaluate the skeleton in 10 year increments to determine an understanding of the norma...

New Non-invasive Modalities for Assessing Retinal Structure and Function

This study investigates a new technology to assess the structure and function inside the eye. Retinal imaging of subjects with inner and outer retinal defects to detect areas of abnormal s...

A Study of the Neurobiology of Depression

Previous research studies have shown that depression is associated with changes in structure and activity in different parts of the brain and that antidepressant medication can affect brai...

Impact of Food Structure on Micronutrient Bioavailability in Human

The nutritional quality of foods strongly depends on the structure / texture of foods, because of the impact on food disintegration, and then on digestion process and nutrient utilization ...

Medical and Biotech [MESH] Definitions

A quantitative prediction of the biological, ecotoxicological or pharmaceutical activity of a molecule. It is based upon structure and activity information gathered from a series of similar compounds.

The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.

Theoretical representations and constructs that describe or explain the structure and hierarchy of relationships and interactions within or between formal organizational entities or informal social groups.

The property of antibodies which enables them to react with some ANTIGENIC DETERMINANTS and not with others. Specificity is dependent on chemical composition, physical forces, and molecular structure at the binding site.

The informal or formal organization of a group of people based on a network of personal relationships which is influenced by the size and composition, etc., of the group.

Advertisement
Quick Search
Advertisement
Advertisement

 


DeepDyve research library

Relevant Topics

Hepatology
Hepatology is the study of liver, gallbladder, biliary tree, and pancreas, and diseases associated with them. This includes viral hepatitis, alcohol damage, cirrhosis and cancer. As modern lifestyles change, with alcoholism and cancer becoming more promi...

Pharmacy
Pharmacy is the science and technique of preparing as well as dispensing drugs and medicines. It is a health profession that links health sciences with chemical sciences and aims to ensure the safe and effective use of pharmaceutical drugs. The scope of...

Drug Discovery
Clinical Approvals Clinical Trials Drug Approvals Drug Delivery Drug Discovery Generics Drugs Prescription Drugs In the fields of medicine, biotechnology and pharmacology, drug discovery is the process by which drugs are dis...


Searches Linking to this Article