Protein kinase C (PKC) isozymes as diagnostic and prognostic biomarkers and therapeutic targets for cancer

T Kawano, J Inokuchi, M Eto, M Murata, JH Kang - Cancers, 2022 - mdpi.com
… roles in the proliferation, differentiation, survival, migration, … the PKC inhibitor staurosporine
or the NF-κB inhibitor BAY 11-… phenotypes of pancreatic adenocarcinoma cells [251]. PKCζ …

An Update on Protein Kinases as Therapeutic Targets—Part I: Protein Kinase C Activation and Its Role in Cancer and Cardiovascular Diseases

S Silnitsky, SJS Rubin, M Zerihun, N Qvit - International Journal of …, 2023 - mdpi.com
… is a more selective PKC inhibitor compared to staurosporine, … and was found to inhibit
proliferation, induce differentiation, and … PKC412 or CGP 41251) is a staurosporine analog …

Protein kinase C at the crossroad of mutations, cancer, targeted therapy and immune response

A Aquino, N Bianchi, A Terrazzan, O Franzese - Biology, 2023 - mdpi.com
… , aiming to discover the selective inhibitors of PKC, mostly … as a PKC inhibitor analogous
to staurosporine, midostaurin … has been reported following kinase neutralization [251]. …

[HTML][HTML] Pre-clinical characterization of PKC412, a multi-kinase inhibitor, against colorectal cancer cells

JP Li, ZJ Huang, XS Lu, YC Zhou, Y Shao, XP He… - Oncotarget, 2016 - ncbi.nlm.nih.gov
… developed as a small-molecular inhibitor of protein kinase C (PKC) [7]. … also inhibit multiple
class III tyrosine kinases, including vascular endothelial growth factor receptor 2 (VEGFR-2), c

Novel Small Molecule Probes and Quantification of Binding to C1 Domains of Protein Kinase C in Living Cells

Y Yin - 2021 - search.proquest.com
selective small molecule modulators, we report in this dissertation the synthesis of a series
of novel carbamate derivatives of … derivatives is hydrophobicity- dependent and inhibition of …

Effect of glucuronidation on the potential of kaempferol to inhibit serine/threonine protein kinases

K Beekmann, LHJ De Haan… - Journal of agricultural …, 2016 - ACS Publications
kinase to bind ATP are in general less selective than allosteric inhibitors which usually show
very high selectivity … of the broad-spectrum protein kinase inhibitor staurosporine, result in a …

Studies on the Mechanism of Action of Selectively Cytotoxic Glycosylated Polyketides

BJ Reisman - 2021 - ir.vanderbilt.edu
… products and methods for finding new compounds which exhibit selective cytotoxicity. In
order to place this work in context, it is necessary to consider how the concept of selective

Midostaurin in acute myeloid leukemia: an evidence-based review and patient selection

HA Abbas, M Alfayez, T Kadia… - Cancer management …, 2019 - Taylor & Francis
… broad, non-selective multikinase inhibitors such as midostaurin and … -staurosporine), a novel
oral protein kinase C inhibitor, … To request a reprint or commercial or derivative permissions …

Midostaurin/PKC412 for the treatment of newly diagnosed FLT3 mutation-positive acute myeloid leukemia

MR Luskin, DJ DeAngelo - Expert Review of Hematology, 2017 - Taylor & Francis
… , more potent and selective FLT3 inhibitors are also in … Midostaurin (PKC412) is a derivative
of staurosporine (from the … due to its ability to reversibly inhibit protein kinase C (PKC). Drug …

A simple and improved active loading method to efficiently encapsulate staurosporine into lipid-based nanoparticles for enhanced therapy of multidrug resistant …

WL Tang, WC Chen, A Roy, E Undzys, SD Li - Pharmaceutical research, 2016 - Springer
Staurosporine (STS), a universal kinase inhibitor, exhibits potent activity … of selectivity, which
result in significant side effects (2). To improve the solubility and specificity, STS derivatives