Track topics on Twitter Track topics that are important to you
Inhibition of the sodium-glucose co-transporters (SGLT1 and SGLT2) is a validated strategy to address the increasing prevalence of type II diabetes mellitus. However, achieving selective inhibition of human SGLT1 or SGLT2 remains challenging. Orally available small molecule drugs based on the D-glucose core of the natural product Gliflozin have proven to be clinically effective in this regard, effectively impeding glucose reabsorption. Herein, we disclose the influence of molecular editing with fluorine at the C2 position of the pyranose ring of Phlorizin analogues Remogliflozin Etabonate and Dapagliflozin (Farxiga®) to concurrently direct β-selective glycosylation, as is required for biological efficacy, and enhance aspects of the physicochemical profile. Given the abundance of glycosylated pharmaceuticals in diabetes therapy that contain a β-configured D-glucose nucleus, it is envisaged that this strategy may prove to be expansive.
This article was published in the following journal.
Name: Chemistry (Weinheim an der Bergstrasse, Germany)
Efficient stereocontrolled synthesis of ladyginoside A isolated from Ladyginia bucharica is described. The presented methodology bases on the β-selective glycosylation to construct oleanate-3-O-β-gl...
The stereocontrolled synthesis of 2-deoxy-d- arabino-hexopyranosides ("galactopyranosides") using 3,4- O-isopropylidene-6- O- tert-butyldiphenylsilyl-protected glycosyl donors is reported. 2-Deoxy-thi...
Electrochemical carbon dioxide reduction (ECDRR), as a key reaction in artificial photosynthesis to implement renewable energy conversion/storage, has been inhibited by the low efficiency and high cos...
Deoxy-sugars often play a critical role in modulating the potency of many bioactive natural products. Accordingly, there has been sustained interest in methods for their synthesis over the past severa...
Fluorine-doped VOsub>2</sub>(M) nanoparticles have been successfully synthesized using the hydrothermal method at a supercritical temperature of 490°C. The pristine VO<sub>2</sub>...
The goal of this study is to better characterize the metabolic alterations and sugar structure alterations (glycosylation abnormalities) in patients diagnosed with Congenital Disorders of ...
The first purpose of this study is to determine if dopamine synthesis capacity is significantly lower in treatment non-responders from illness onset relative to treatment responders. And t...
The purpose of this study is to investigate the coagulation balance in a cohort of congenital disorder of glycosylation (CDG) patients using conventional tests combined with an integrated ...
1. Objectives 1. Which organ and how does SGLT2 inhibitor alter insulin sensitivity? 2. How does SGLT2 inhibitor increase glucagon levels and hepatic glucose production?
The objective of this study was to compare the effectiveness of sodium glucose co-transporter 2 (SGLT2) inhibitors relative to metformin for reducing subsequent cardiovascular events in pa...
Unstable isotopes of fluorine that decay or disintegrate emitting radiation. F atoms with atomic weights 17, 18, and 20-22 are radioactive fluorine isotopes.
Inorganic compounds that contain fluorine as an integral part of the molecule.
A genetically heterogeneous group of heritable disorders resulting from defects in protein N-glycosylation.
Magnetic resonance imaging diagnostic technique which uses fluorine-19 perfluorocarbon probes and contrast agents for high resolution image detection and quantitation.
A single-pass transmembrane CELL SURFACE RECEPTOR that binds ADVANCED GLYCOSYLATION END PRODUCTS to mediate cellular responses to both acute and chronic vascular inflammation in conditions such as ATHEROSCLEROSIS and DIABETES MELLITUS, TYPE 2 . It also binds AMYLOID BETA PEPTIDES and the alarmins S100A12 and S100 CALCIUM BINDING PROTEIN BETA SUBUNIT.
Within medicine, nutrition (the study of food and the effect of its components on the body) has many different roles. Appropriate nutrition can help prevent certain diseases, or treat others. In critically ill patients, artificial feeding by tubes need t...
Diabetes is a lifelong condition that causes a person's blood sugar level to become too high. The two main types of diabetes are: type 1 diabetes type 2 diabetes In the UK, diabetes affects approximately 2.9 million people. There are a...