Unlocking the therapeutic potential of protein kinase inhibitors in neurodegenerative and psychiatric disorders [PDF]
Exploration of Drug ScienceProtein phosphorylation is a fundamental regulatory mechanism governing a broad spectrum of cellular processes. In the nervous system, it is critical for modulating neurotransmitter release, synaptic plasticity, neuronal excitability, and cell survival ...
Angela Asir R V +2 more
doaj +1 more source
Microwave-assisted synthesis of a MK2 inhibitor by Suzuki-Miyaura coupling for study in Werner syndrome cells [PDF]
, 2015 Microwave-assisted Suzuki-Miyaura cross-coupling reactions have been employed towards the synthesis of three different MAPKAPK2 (MK2) inhibitors to study accelerated aging in Werner syndrome (WS) cells, including the cross-coupling of a 2-chloroquinoline
Bagley, Mark C +5 more
core +3 more sources
Potential therapeutic targeting of BKCa channels in glioblastoma treatment
Molecular Oncology, EarlyView.This review summarizes current insights into the role of BKCa and mitoBKCa channels in glioblastoma biology, their potential classification as oncochannels, and the emerging pharmacological strategies targeting these channels, emphasizing the translational challenges in developing BKCa‐directed therapies for glioblastoma treatment.
Kamila Maliszewska‐Olejniczak +4 more
wiley +1 more source
Journal of Lipid Research, 1995 Inhibitors of protein kinases were screened for the ability to prevent the repression of cholesterol 7 alpha-hydroxylase mRNA by taurocholate in primary cultures of adult rat hepatocytes.
R T Stravitz +3 more
doaj +1 more source
Biological functions of CDK5 and potential CDK5 targeted clinical treatments. [PDF]
, 2017 Cyclin dependent kinases are proline-directed serine/threonine protein kinases that are traditionally activated upon association with a regulatory subunit.
Casimiro, Mathew C. +2 more
core +2 more sources
Effective therapeutic targeting of CTNNB1‐mutant hepatoblastoma with WNTinib
Molecular Oncology, EarlyView.WNTinib, a Wnt/CTNNB1 inhibitor, was tested in hepatoblastoma (HB) experimental models. It delayed tumor growth and improved survival in CTNNB1‐mutant in vivo models. In organoids, WNTinib outperformed cisplatin and showed enhanced efficacy in combination therapy, supporting its potential as a targeted treatment for CTNNB1‐mutated HB.
Ugne Balaseviciute +17 more
wiley +1 more source
A Stapled Peptide Mimic of the Pseudosubstrate Inhibitor PKI Inhibits Protein Kinase A
Molecules, 2019 Kinases regulate multiple and diverse signaling pathways and misregulation is implicated in a multitude of diseases. Although significant efforts have been put forth to develop kinase-specific inhibitors, specificity remains a challenge.
Jascha T. Manschwetus +5 more
doaj +1 more source
Computational structure‐based drug design: Predicting target flexibility [PDF]
, 2018 The role of molecular modeling in drug design has experienced a significant revamp in the last decade. The increase in computational resources and molecular models, along with software developments, is finally introducing a competitive advantage in early
Ding X. +4 more
core +2 more sources
Exploiting metabolic adaptations to overcome dabrafenib treatment resistance in melanoma cells
Molecular Oncology, EarlyView.We show that dabrafenib‐resistant melanoma cells undergo mitochondrial remodeling, leading to elevated respiration and ROS production balanced by stronger antioxidant defenses. This altered redox state promotes survival despite mitochondrial damage but renders resistant cells highly vulnerable to ROS‐inducing compounds such as PEITC, highlighting redox
Silvia Eller +17 more
wiley +1 more source
A high-throughput screen identifies that CDK7 activates glucose consumption in lung cancer cells. [PDF]
, 2019 Elevated glucose consumption is fundamental to cancer, but selectively targeting this pathway is challenging. We develop a high-throughput assay for measuring glucose consumption and use it to screen non-small-cell lung cancer cell lines against ...
Chen, Bao Ying +5 more
core +1 more source