Publications by authors named "O Werz"
Inhibiting microsomal prostaglandin E synthase-1 (mPGES-1), an inducible enzyme involved in prostaglandin E (PGE) biosynthesis and tumor microenvironment (TME) homeostasis, is a valuable strategy for treating inflammation and cancer. In this work, 5-methylcarboxamidepyrrole-based molecules were designed and synthesized as new compounds targeting mPGES-1. Remarkably, compounds 1f, 2b, 2c, and 2d were able to significantly reduce the activity of the isolated enzyme, showing IC values in the low micromolar range.
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- mPGES-1 is highlighted as a key target for developing treatments for inflammation and pain, with the study introducing new benzimidazole compounds that effectively inhibit this enzyme.
- One of the compounds, AGU654, showed exceptional selectivity for mPGES-1 over other related enzymes, with a low inhibition concentration (IC = 2.9 nM) and promising bioavailability.
- AGU654 was able to reduce PGE production from activated immune cells without affecting other prostaglandins, and it also demonstrated success in alleviating fever and pain in guinea pig models, indicating its potential for managing inflammatory diseases.
Article Synopsis
- - Psoriasis is a common skin condition that currently has no cure, and more research is needed to understand its underlying processes and develop new treatments; however, there are challenges due to the lack of effective preclinical models.
- - Recent advancements include creating 3D skin models that mimic psoriasis features, allowing researchers to study treatment responses using these replicas, which exhibit characteristics like inflammation and hyperproliferation when treated with cytokines.
- - Treatments such as dexamethasone (DEX), celastrol (CEL), and biologics like adalimumab (ADM) and bimekizumab (BMM) demonstrated varying degrees of effectiveness in reducing inflammation and promoting skin differentiation, suggesting that this new in vitro
A current trend in healthcare research is to discover multifunctional compounds, able to interact with multiple biological targets, in order to simplify multi-drug therapies and improve patient compliance. The aim of this work was to outline the growing demand for innovative multifunctional compounds, achieved through the synthesis, characterisation and SAR evaluation of a series of 2-styrylbenzothiazole derivatives. The six synthesised compounds were studied for their potential as photoprotective, antioxidant, antiproliferative, and anti-inflammatory agents.
View Article and Find Full Text PDFA library of degradable poly(2-alkyl-2-oxazoline) analogues (dPOx) with different length of the alkyl substituents was characterized in detail by gradient elution liquid chromatography. The hydrophobicity increased with increased side chain length as confirmed by a hydrophobicity row, established by reversed-phase liquid chromatography. Those dPOx were cytocompatible and formed colloidally stable nanoparticle (NP) formulations with positive zeta potential.
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