cGMP-Dependent Protein Kinase Inhibitors in Health and Disease
cGMP-dependent protein kinases (PKG) exhibit diverse physiological functions in the mammalian system e.g., in vascular and gastrointestinal smooth muscles, in platelets, in kidney, in bone growth, nociception and in the central nervous system ...
Jens Schlossmann+2 more
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Involvement of Protein Kinase C and Protein Kinase A in the Enhancement of L-type Calcium Current by GABA\u3csub\u3eB\u3c/sub\u3e Receptor Activation in Neonatal Hippocampus [PDF]
In the early neonatal period activation of GABAB receptors attenuates calcium current through N-type calcium channels while enhancing current through L-type calcium channels in rat hippocampal neurons.
Bray, Jennifer Grace, Mynlieff, Michelle
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Selective inhibition of the kinase DYRK1A by targeting its folding process
Kinase inhibitors are important drugs and usually target the ATP binding pocket of kinases. Here, Kii et al.report a completely new type of kinase inhibitor that specifically targets the protein folding intermediate state, but not the mature form, of the
Isao Kii+14 more
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Potential and limitations of PKA/ PKG inhibitors for platelet studies
Cyclic nucleotides (cAMP and cGMP) and corresponding protein kinases, protein kinase A (PKA) and protein kinase G (PKG), are the main intracellular mediators of endothelium-derived platelet inhibitors. Pharmacological PKA/PKG inhibitors are often used to
Valentina Shpakova+3 more
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Identification and characterization of an irreversible inhibitor of CDK2 [PDF]
Irreversible inhibitors that modify cysteine or lysine residues within a protein kinase ATP binding site offer, through their distinctive mode of action, an alternative to ATP-competitive agents.
Anscombe, Elizabeth+16 more
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T cell recognition of antigens displayed on the surface of antigen presenting cell results in rapid activation of protein tyrosine kinases and kinase C.
Almeida Célia A, Goes Alfredo M
doaj
Protein kinase inhibitors from Indonesian Sponge Axynissa sp.
A research about inhibitory activity on various cancer related protein kinases of several marine sponges collected in Indonesia was performed. This study aims were to isolate and to identify structures of biologically active sponge metabolites.
Triana Hertiani,+4 more
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Mutations in Leucine-rich repeat kinase 2 gene (LRRK2) are associated with familial and sporadic Parkinson’s disease (PD). LRRK2 is a complex protein that consists of multiple domains executing several functions, including GTP hydrolysis, kinase activity
Maria Daniela Cirnaru+19 more
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Targeting Brutons Tyrosine Kinase in Chronic Lymphocytic Leukemia at the Crossroad between Intrinsic and Extrinsic Pro-survival Signals [PDF]
Chemo immunotherapies for chronic lymphocytic leukemia (CLL) showed a positive impact on clinical outcome, but many patients relapsed or become refractory to the available treatments.
Facco, Monica+7 more
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Targeting the phosphatidylinositol 3-kinase/Akt/mechanistic target of rapamycin signaling pathway in B-lineage acute lymphoblastic leukemia: An update [PDF]
Despite considerable progress in treatment protocols, B-lineage acute lymphoblastic leukemia (B-ALL) displays a poor prognosis in about 15–20% of pediatric cases and about 60% of adult patients. In addition, life-long irreversible late effects from chemo-
Capitani, Silvano+6 more
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