Protein kinase C, an elusive therapeutic target?

D Mochly-Rosen, K Das, KV Grimes - Nature reviews Drug discovery, 2012 - nature.com
Protein kinase C (PKC) has been a tantalizing target for drug discovery ever since it was first
identified as the receptor for the tumour promoter phorbol ester in 1982. Although initial …

Evolving mechanisms of vascular smooth muscle contraction highlight key targets in vascular disease

Z Liu, RA Khalil - Biochemical pharmacology, 2018 - Elsevier
Vascular smooth muscle (VSM) plays an important role in the regulation of vascular function.
Identifying the mechanisms of VSM contraction has been a major research goal in order to …

A novel Drp1 inhibitor diminishes aberrant mitochondrial fission and neurotoxicity

X Qi, N Qvit, YC Su… - Journal of cell …, 2013 - journals.biologists.com
Excessive mitochondrial fission is associated with the pathology of a number of
neurodegenerative diseases. Therefore, inhibitors of aberrant mitochondrial fission could …

Peptides and peptidomimetics as regulators of protein–protein interactions

AD Cunningham, N Qvit, D Mochly-Rosen - Current opinion in structural …, 2017 - Elsevier
Highlights•Protein–protein interactions are essential for almost all cell processes.•Peptides
are ideal candidates for targeting protein–protein interactions (PPIs).•We survey screening …

Protein kinase C as regulator of vascular smooth muscle function and potential target in vascular disorders

HC Ringvold, RA Khalil - Advances in pharmacology, 2017 - Elsevier
Vascular smooth muscle (VSM) plays an important role in maintaining vascular tone. In
addition to Ca 2+-dependent myosin light chain (MLC) phosphorylation, protein kinase C …

A selective inhibitor of mitofusin 1-βIIPKC association improves heart failure outcome in rats

JCB Ferreira, JC Campos, N Qvit, X Qi… - Nature …, 2019 - nature.com
We previously demonstrated that beta II protein kinase C (βIIPKC) activity is elevated in
failing hearts and contributes to this pathology. Here we report that βIIPKC accumulates on …

Glyceraldehyde-3-phosphate dehydrogenase (GAPDH) phosphorylation by protein kinase Cδ (PKCδ) inhibits mitochondria elimination by lysosomal-like structures …

G Yogalingam, S Hwang, JCB Ferreira… - Journal of Biological …, 2013 - ASBMB
After cardiac ischemia and reperfusion or reoxygenation (I/R), damaged mitochondria
propagate tissue injury by promoting cell death. One possible mechanism to protect from I/R …

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
Protein kinases are one of the most significant drug targets in the human proteome,
historically harnessed for the treatment of cancer, cardiovascular disease, and a growing …

[HTML][HTML] Intracellular peptides: From discovery to function

ES Ferro, V Rioli, LM Castro, LD Fricker - EuPA Open Proteomics, 2014 - Elsevier
Peptidomics techniques have identified hundreds of peptides that are derived from proteins
present mainly in the cytosol, mitochondria, and/or nucleus; these are termed intracellular …

Multifunctional roles of PKCδ: Opportunities for targeted therapy in human disease

ME Reyland, DNM Jones - Pharmacology & therapeutics, 2016 - Elsevier
The serine–threonine protein kinase, protein kinase C-δ (PKCδ), is emerging as a bi-
functional regulator of cell death and proliferation. Studies in PKCδ−/− mice have confirmed …