Protein Kinases as Drug Development Targets for Heart Disease Therapy
Protein kinases are intimately integrated in different signal transduction pathways for the regulation of cardiac function in both health and disease.
Alison L. Müller, Naranjan S. Dhalla
doaj +1 more source
Regulation of signal duration and the statistical dynamics of kinase activation by scaffold proteins [PDF]
Scaffolding proteins that direct the assembly of multiple kinases into a spatially localized signaling complex are often essential for the maintenance of an appropriate biological response. Although scaffolds are widely believed to have dramatic effects on the dynamics of signal propagation, the mechanisms that underlie these consequences are not well ...
arxiv +1 more source
Phosphorylation and inactivation of glycogen synthase kinase 3 by protein kinase A.
Glycogen synthase kinase 3 (GSK-3) is implicated in multiple biological processes including metabolism, gene expression, cell fate determination, proliferation, and survival. GSK-3 activity is inhibited through phosphorylation of serine 21 in GSK-3 alpha
Xianjun Fang+5 more
semanticscholar +1 more source
The Role of Cyclic AMP Signaling in Cardiac Fibrosis
Myocardial stress and injury invariably promote remodeling of the cardiac tissue, which is associated with cardiomyocyte death and development of fibrosis. The fibrotic process is initially triggered by the differentiation of resident cardiac fibroblasts
Marion Delaunay+3 more
doaj +1 more source
Oncogenic PKA signaling increases c-MYC protein expression through multiple targetable mechanisms
Genetic alterations that activate protein kinase A (PKA) are found in many tumor types. Yet, their downstream oncogenic signaling mechanisms are poorly understood.
Gary KL Chan+19 more
doaj +1 more source
Role of AMP-activated protein kinase in mechanism of metformin action.
Metformin is a widely used drug for treatment of type 2 diabetes with no defined cellular mechanism of action. Its glucose-lowering effect results from decreased hepatic glucose production and increased glucose utilization. Metformin's beneficial effects
Gaochao Zhou+13 more
semanticscholar +1 more source
Regulatory role of some protein kinases in signal transduction pathways in heart health and disease [PDF]
Various protein kinases including protein kinase A (PKA), Ca2+-calmodulin kinase (CaMK), phosphoinositide 3-kinase (PI3K), protein kinase C (PKC) and mitogen-activated protein kinase (MAPK: ERK1/2, p38-MAPK and JNK) are integral part of different signal ...
Nusier Mohamad+4 more
doaj
Resolving the binding-kinase discrepancy in bacterial chemotaxis: A nonequilibrium allosteric model and the role of energy dissipation [PDF]
The Escherichia coli chemotaxis signaling pathway has served as a model system for studying the adaptive sensing of environmental signals by large protein complexes. The chemoreceptors control the kinase activity of CheA in response to the extracellular ligand concentration and adapt across a wide concentration range by undergoing methylation and ...
arxiv +1 more source
Suppression of Raf-1 kinase activity and MAP kinase signalling by RKIP [PDF]
Raf-1 phosphorylates and activates MEK-1, a kinase that activates the extracellular signal regulated kinases (ERK). This kinase cascade controls the proliferation and differentiation of different cell types.
A Minden+25 more
core +1 more source
The many-faced KSR1: a tumor suppressor in breast cancer [PDF]
Emerging evidence supports the dual function of kinase suppressor of Ras 1 (KSR1) as an active kinase and a scaffold, although it has been extensively referred as a pseudokinase, due to the absence of key residues in its catalytic domain [1, 2].
Giamas, Georgios+2 more
core +2 more sources