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 …

Protein kinase C pharmacology: refining the toolbox

AX Wu-Zhang, AC Newton - Biochemical Journal, 2013 - portlandpress.com
PKC (protein kinase C) has been in the limelight since the discovery three decades ago that
it acts as a major receptor for the tumour-promoting phorbol esters. Phorbol esters, with their …

Protein kinase C α is a central signaling node and therapeutic target for breast cancer stem cells

WL Tam, H Lu, J Buikhuisen, BS Soh, E Lim… - Cancer cell, 2013 - cell.com
The epithelial-mesenchymal transition program becomes activated during malignant
progression and can enrich for cancer stem cells (CSCs). We report that inhibition of protein …

mTORC2 controls the activity of PKC and Akt by phosphorylating a conserved TOR interaction motif

TR Baffi, G Lordén, JM Wozniak, A Feichtner… - Science …, 2021 - science.org
The complex mTORC2 is accepted to be the kinase that controls the phosphorylation of the
hydrophobic motif, a key regulatory switch for AGC kinases, although whether mTOR directly …

Equivocal, explicit and emergent actions of PKC isoforms in cancer

PJ Parker, SJ Brown, V Calleja, P Chakravarty… - Nature Reviews …, 2021 - nature.com
The maturing mutational landscape of cancer genomes, the development and application of
clinical interventions and evolving insights into tumour-associated functions reveal …

CCR2 chemokine receptors enhance growth and cell-cycle progression of breast cancer cells through SRC and PKC activation

M Yao, W Fang, C Smart, Q Hu, S Huang… - Molecular Cancer …, 2019 - AACR
Basal-like breast cancers are an aggressive breast cancer subtype, which often lack
estrogen receptor, progesterone receptor, and Her2 expression, and are resistant to …

Protein kinase C quality control by phosphatase PHLPP1 unveils loss-of-function mechanism in cancer

TR Baffi, AAN Van, W Zhao, GB Mills, AC Newton - Molecular cell, 2019 - cell.com
Protein kinase C (PKC) isozymes function as tumor suppressors in increasing contexts. In
contrast to oncogenic kinases, whose function is acutely regulated by transient …

Intramolecular conformational changes optimize protein kinase C signaling

CE Antal, JD Violin, MT Kunkel, S Skovsø… - Chemistry & biology, 2014 - cell.com
Optimal tuning of enzyme signaling is critical for cellular homeostasis. We use fluorescence
resonance energy transfer reporters in live cells to follow conformational transitions that tune …

Conventional protein kinase C in the brain: repurposing cancer drugs for neurodegenerative treatment?

G Lordén, AC Newton - Neuronal signaling, 2021 - portlandpress.com
Abstract Protein Kinase C (PKC) isozymes are tightly regulated kinases that transduce a
myriad of signals from receptor-mediated hydrolysis of membrane phospholipids. They play …

Intramolecular C2 domain-mediated autoinhibition of protein kinase C βII

CE Antal, JA Callender, AP Kornev, SS Taylor… - Cell reports, 2015 - cell.com
The signaling output of protein kinase C (PKC) is exquisitely controlled, with its disruption
resulting in pathophysiologies. Identifying the structural basis for autoinhibition is central to …