Results 21 to 30 of about 854,863 (214)

Development of a novel family of antifungal agents based on a quinone methide oxime framework

Scientific Reports
Given the widespread occurrence of fungal infections, the phenomenon of fungal drug resistance, and the limited number of systemic antimycotic therapies, novel chemicals should be developed to control pathogenic fungi.
Monika Janeczko, Maciej Masłyk, Oleg M. Demchuk, Antonina Kurowska-Okoń, Mateusz Kwaśnik, Kamila Górka, Aleksandra Martyna, Béatrice Foll-Josselin, Sandrine Ruchaud, Stéphane Bach, Przemysław Woliński, Radomir Jasiński, Barbara Mirosław, Małgorzata Sadczuk, Konrad Kubiński   +14 more
doaj   +1 more source

Synthesis of 1H-Pyrrolo[3,2-g]isoquinoline Derivatives as Ligands Targeting Haspin Kinase

Molecules
A new series of 1H-pyrrolo[3,2-g]isoquinolines, diversely substituted at the 3-position either by a heteroaromatic scaffold or by propionate/acrylate side chains, were synthesized and evaluated as Haspin kinase inhibitors.
Killian Malosse, Béatrice Josselin, Sandrine Ruchaud, Fabrice Anizon, Francis Giraud, Pascale Moreau   +5 more
doaj   +1 more source

Activation of Phosphoinositide 3-Kinase, Protein Kinase C, and Extracellular Signal-Regulated Kinase Is Required for Oridonin-Enhanced Phagocytosis of Apoptotic Bodies in Human Macrophage-Like U937 Cells

Journal of Pharmacological Sciences, 2005
Our previous study showed that oridonin isolated from Rabdosia rubescens enhanced phagocytosis of apoptotic cells by macrophage-like U937 cells through tumor necrosis factor (TNF) α and interleukin (IL)-1β release.
Yan-Qiu Liu, Song You, Shin-ichi Tashiro, Satoshi Onodera, Takashi Ikejima   +4 more
doaj   +1 more source

Organoids in pediatric cancer research

FEBS Letters, EarlyView.
Organoid technology has revolutionized cancer research, yet its application in pediatric oncology remains limited. Recent advances have enabled the development of pediatric tumor organoids, offering new insights into disease biology, treatment response, and interactions with the tumor microenvironment.
Carla Ríos Arceo, Jarno Drost
wiley   +1 more source

An isoform of 14‐3‐3 protein regulates transbilayer lipid movement at the plasma membrane

FEBS Letters, EarlyView.
Loss of 14‐3‐3ζ in CHO cells confers resistance to exogenous phosphatidylserine (PS) and impairs endocytosis‐independent inward flip‐flop of fluorescent PS at the plasma membrane. RNAi‐mediated knockdown reproduces this defect, while no additive effect is seen in ATP11C‐deficient cells.
Akiko Yamaji‐Hasegawa, Akira Hattori, Masafumi Tsujimoto, Toshihide Kobayashi   +3 more
wiley   +1 more source

An Experimentally Validated Structure-Based Virtual Screening Approach to Identify Nucleotide-Binding Protein Inhibitors as a New Source of Kinase Inhibitors

Pharmaceuticals
Background/Objectives: Protein kinases represent major therapeutic targets because dysregulation of their phosphorylation activity is associated with several diseases, including cancer, diabetes, and inflammatory disorders.
Nicolas Bosc, Fabrice Carles, Jade Fogha, Blandine Baratte, Stéphane Bach, Samia Aci-Sèche, Stéphane Bourg, Sylvain Routier, Sandrine Ruchaud, Frédéric Buron, Pascal Bonnet   +10 more
doaj   +1 more source

Organizing the interface—Plasma membrane architecture and receptor dynamics in virus‐cell interactions

FEBS Letters, EarlyView.
Plasma membranes contain dynamic nanoscale domains that organize lipids and receptors. Because viruses operate at similar scales, this architecture shapes early infection steps, including attachment, receptor engagement, and entry. Using influenza A virus and HIV‐1 as examples, we highlight how receptor nanoclusters, multivalent glycan interactions ...
Jan Schlegel, Christian Sieben
wiley   +1 more source

The pyrazolo[4,3-c]pyrazole core as a novel and versatile scaffold for developing dual DYRK1A-CLK1 inhibitors targeting key processes of Alzheimer's disease pathology

European Journal of Medicinal Chemistry Reports
In the current study, we designed, synthesized, and characterized a series of substituted pyrazolo[4,3-c]pyrazoles. These novel compounds were evaluated in vitro for their inhibitory activity over a panel of protein kinases to determine their potential ...
Vaia-Argyro Bakalakou, Barbara Mavroidi, Amalia D. Kalampaliki, Béatrice Josselin, Stéphane Bach, Alexios-Leandros Skaltsounis, Panagiotis Marakos, Nicole Pouli, Maria Pelecanou, Vassilios Myrianthopoulos, Sandrine Ruchaud, Ioannis K. Kostakis   +11 more
doaj   +1 more source

Aurora kinases as targets in drug-resistant neuroblastoma cells.

PLoS ONE, 2014
Aurora kinase inhibitors displayed activity in pre-clinical neuroblastoma models. Here, we studied the effects of the pan-aurora kinase inhibitor tozasertib (VX680, MK-0457) and the aurora kinase inhibitor alisertib (MLN8237) that shows some specificity ...
Martin Michaelis, Florian Selt, Florian Rothweiler, Nadine Löschmann, Benedikt Nüsse, Wilhelm G Dirks, Richard Zehner, Jindrich Cinatl   +7 more
doaj   +1 more source

Exploring kinase family inhibitors and their moiety preferences using deep SHapley additive exPlanations

BMC Bioinformatics, 2022
Background While it has been known that human protein kinases mediate most signal transductions in cells and their dysfunction can result in inflammatory diseases and cancers, it remains a challenge to find effective kinase inhibitor as drugs for these ...
You-Wei Fan, Wan-Hsin Liu, Yun-Ti Chen, Yen-Chao Hsu, Nikhil Pathak, Yu-Wei Huang, Jinn-Moon Yang   +6 more
doaj   +1 more source