Pyridinylimidazoles as GSK3β Inhibitors: The Impact of Tautomerism on Compound Activity via Water Networks.

Glycogen synthase kinase-3β (GSK3β) is involved in many pathological conditions and represents an attractive drug target. We previously reported dual GSK3β/p38α mitogen-activated protein kinase inhibitors and identified -(4-(4-(4-fluorophenyl)-2-methyl-1-imidazol-5-yl)pyridin-2-yl)cyclopropanecarboxamide () as a potent dual inhibitor of both target kinases. In this study, we aimed to design selective GSK3β inhibitors based on our pyridinylimidazole scaffold.

Neuroprotective potential of Myrciaria plinioides D. Legrand extract in an in vitro human neuroblastoma model.

Neurodegenerative diseases are multifactorial debilitating disorders of the nervous system affecting approximately 30 million individuals worldwide. Mitochondrial dysfunction and oxidative stress have also been implicated in causing neurodegeneration. As life expectancy is increasing, neurodegenerative disorders are becoming a major social issue.

Are peptides a solution for the treatment of hyperactivated JAK3 pathways?

While the inactivation mutations that eliminate JAK3 function lead to the immunological disorders such as severe combined immunodeficiency, activation mutations, causing constitutive JAK3 signaling, are known to trigger various types of cancer or are responsible for autoimmune diseases, such as rheumatoid arthritis, psoriasis, or inflammatory bowel diseases. Treatment of hyperactivated JAK3 is still an obstacle, due to different sensibility of mutation types to conventional drugs and unwanted side effects, because these drugs are not absolutely specific for JAK3, thus inhibiting other members of the JAK family, too. Lack of information, in which way sole inhibition of JAK3 is necessary for elimination of the disease, calls for the development of isoform-specific JAK3 inhibitors.

Effect of temperature and storage time on dental bleaching effectiveness.

Objective: To evaluate the effect of storage time and temperature on the effectiveness of bleaching agents.

Methods: Enamel slabs were randomly allocated according to the concentration of carbamide peroxide (CP): 10% (CP10) and 16% (CP16). Shade evaluations were conducted at baseline and then after 3 and 12 months of storage at 3 different temperatures: 10°C (±2°C), 25°C (±2°C), and 35°C (±2°C).

Development of alginate-pectin microparticles with dairy whey using vibration technology: Effects of matrix composition on the protection of Lactobacillus spp. from adverse conditions.

In this study, lactic acid bacteria with probiotic potential, including Lactobacillus plantarum ATCC8014, L. paracasei ML33 and L. pentosus ML82, were encapsulated with whey-alginate-pectin (WAP) or whey permeate-alginate-pectin (PAP) by an extrusion process using vibrational technology, with the resulting microparticles assessed for their resistance to adverse conditions.