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 …
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 …
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
Excessive mitochondrial fission is associated with the pathology of a number of
neurodegenerative diseases. Therefore, inhibitors of aberrant mitochondrial fission could …
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 …
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 …
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
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 …
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 …
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
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 …
historically harnessed for the treatment of cancer, cardiovascular disease, and a growing …
[HTML][HTML] Intracellular peptides: From discovery to function
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 …
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 …
functional regulator of cell death and proliferation. Studies in PKCδ−/− mice have confirmed …