This shows that sex hormones have no direct activating action on insulinase but only promote the development of this enzyme system during ontogenesis. These data may lead to the conclusion that inactivation of hepatic insulinase by sulfonamides plays an important role in the mechanism of their ...
Anticonvulsant Sulfonamides/Sulfamates/Sulfamides with Carbonic Anhydrase Inhibitory Activity: Drug Design and Mechanism of Action. T.; Masereel, B., Anticonvulsant sulfonamides/sulfamates/sulfamides with carbonic anhydrase inhibitory activity: drug design and mechanism of action. Curr ... Thiry,Anne,Dog...
This refers to the mechanism of action of a small-molecule drug, whereby its function is transiently recruited to a target protein in a catalytic manner (for example, ubiquitylation by an E3 ligase recruited by a proteolysis-targeting chimera (PROTAC)), resulting in a pharmacological effect (deg...
In concert with improvements in personal hygiene and public sanitation, the discovery and development of antibiotics during the latter half of the last century has reduced substantially the morbidity and mortality associated with bacterial diseases. However, the past decade has witnessed a sharp reduction...
Fig. 1. Top: structure of the GFP and its chromophore and the 8-aminoquinoline-zinc-complex. Bottom: concept for the mechanism of our proposed sensor. 8-Aminoquinolines have been successfully used as selective ionophores for Zn2+.[48], [49], [50], [51] We envisioned that a freely rot...
This functional head is capable of participating in several noncovalent and electrostatic bonding interactions to stabilise protein-ligand interactions in the receptors [8]. In contrast to the flat and linear amide bioisosters, sulfonamides are bent and this unique feature provides a useful way to ...
Understanding the mechanism of action of these glycans requires the access to pure and chemically well-defined structures in reasonable amounts. The synthesis of these complex branched oligosaccharides is not trivial and few syntheses are reported in the literature with several synthetic and purification...
Recently, a structure of guinea pig BLT1 (gpBLT1) in complex with the inverse agonist BIIL-260 (PDB ID 5X33) has been solved23 at a resolution of 3.7 Å. To provide a structural basis for hBLT1 ligand recognition and a deeper understanding of its mechanism of action, here we de...
Figure 1. Schematic representation of the mechanism of action of heterobifunctional PROTACs and molecular glues Both PROTACs and molecular glues induce proximity between a protein of interest (POI) and an E3 ubiquitin ligase complex, leading to formation of a ternary complex and transfer of ubiquitin...
For these studies, we were more interested in exploring the probable mechanism of action of the synthesized compounds in the context of TB disease, such that edges they were connected to the tuberculosis nodes were extracted to understand influential genes and the number of instances where the ...