Glucocorticoids (GCs) are steroid hormones characterized by their anti-inflammatory and immunosuppressive nature. Although GCs are very commonly prescribed, in several diseases, including sepsis, their clinical treatment is hampered by side effects and by the occurrence of glucocorticoid resistance (GCR). Sepsis is defined as a life-threatening org...
Published in Current drug discovery technologies
In the presented work we successfully discovered several novel NQO1 inducers using the computational approaches. The phytochemical sulforaphane (SFN) is a potent inducer of carcinogen detoxication enzymes like NAD(P)H:quinone oxidoreductase 1 (NQO1) through the Kelch-like erythroid cell-derived protein with CNC homology[ECH]-associated protein 1 (K...
Published in Medicinal chemistry (Shariqah (United Arab Emirates))
New chemical agents that could combat increasing antibiotic resistance are urgently needed. In this mini-review, an old but highly relevant RNA sequence which is crucial for the continuation of bacterial life-cycle is covered. Some of the most significant advances of the last decade in sensing and targeting the bacterial rRNA A-site: a well-validat...
Published in Journal of pharmaceutical and biomedical analysis
The need of a continuous productivity increases in medicinal chemistry laboratories of the pharmaceutical industry motivated the development, over the years, of new software solutions to enable Open-Access in many analytical techniques such as NMR or LC, among others, to characterize and assess the purity of new molecules. These approaches have bee...
Alzheimer’s disease (AD) is the most prevalent cause of dementia that affects over 50 million people, and is associated strongly with the aggregation of the amyloid-β peptide (Aβ). Even though a variety of strategies has been developed towards inhibiting the aggregation of Aβ, no disease-modifying treatment has so far reached the clinic. This failu...
The protein-folding chaperone Hsp90 enables the maturation and stability of various oncogenic signaling proteins and is thus pursued as a cancer drug target. Folding in particular of protein kinases is assisted by the co-chaperone Cdc37. Several inhibitors against the Hsp90 ATP-binding site have been developed. However, they displayed significant t...
Published in Sexual medicine reviews
Peyronie's disease (PD) is a debilitating affliction for the male population, causing severe curvatures to the erect penis and erectile dysfunction in about 50% of men. This deviation of the penis significantly impairs sexual intercourse and causes depression and strains in the relationship. As of today, medical treatment options are few and far be...
To combat emerging infectious diseases like Zika virus (ZIKV), synthetic messenger RNAs (mRNAs) encoding viral antigens are very attractive as they allow a rapid, generic, and flexible production of vaccines. In this work, we engineered a self-replicating mRNA (sr-mRNA) vaccine encoding the pre-membrane and envelope (prM-E) glycoproteins of ZIKV. I...
Nature is considered a prolific source of diverse biologically active chemotypes. Medicinal plants have historically attracted the most attention and have led to the discovery of various drugs ranging from anticancer to anti-infectious agents. However, a vast array of bioactive metabolites have also been discovered from marine organisms, fungi and ...
© 2019 Elsevier Masson SAS Dengue is the most important arthropod-borne viral disease of humans, with more than half of the global population living in at-risk areas. Despite the negative impact on public health, there are no antiviral therapies available, and the only licensed vaccine, Dengvaxia®, has been contraindicated in children below nine ye...
