Inhibition of Methyltransferase SMYD3 Targets Ras-driven Cancers
Wednesday, 04 May 2016
The methyltransferase SMYD3 is overexpressed in several tumor types, and its overexpression correlates with aggressiveness in breast carcinoma. Its epigenetic role has been investigated extensively: SMYD3 methylates histone H4 at K5, stimulating expression of critical oncogenic proteins that drive cell proliferation, invasion and metastasis. However, it has recently been discovered that SMYD3 also methylates non-histone
- Published in Emerging Targets
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Unraveling RhoGDIα Regulation
Friday, 15 April 2016
Rho proteins are small, monomeric GTPases in the Ras superfamily that control cell shape and motility by regulating cytoskeletal dynamics. They cycle between a GDP-bound inactive state and a GTP-bound active state. When in the active state, Rho proteins bind to effectors at the plasma membrane, which regulate cellular processes such as cell architecture, intracellular
- Published in Emerging Targets
Bound for Life: The First Irreversible Inhibitor of CDK2
Tuesday, 08 March 2016
Drugs targeting cyclin-dependent kinases (CDKs) have been a hot topic in the development of cancer treatments. Kinases in the CDK family play a significant role in the cell cycle and transcription, and thus in tumor development. The first drug targeting a CDK, a CDK4 inhibitor called palbociclib (Pfizer), was approved in February of 2015 for
- Published in Emerging Targets
SIRT6: Keeping Tumor Cells in Check
Tuesday, 01 March 2016
When pyruvate kinase is discussed, cancer is not the usual topic of conversation. This ubiquitous enzyme catalyzes the final rate-limiting step in glycolysis; transferring a phosphoryl group from phosphoenolpyruvate to ADP, generating ATP and pyruvate. The M2 isoform (PKM2) is exclusively expressed in embryonic or adult dividing cells. Before cell division, glycolysis levels are down-regulated
- Published in Emerging Targets
Lung Cancer Cells Use NF-κB Pathway to Subvert Third Generation EGFR Kinase Inhibitors
Tuesday, 16 February 2016
The epidermal growth factor receptor (EGFR) was the first extracellular receptor identified as a tyrosine kinase and the first target of selective small molecule tyrosine kinase inhibitors. One of these, gefitinib, was the second kinase inhibitor to be approved by the FDA, in 2003, for the treatment of non-small-cell lung cancer (NSCLC); a second EGFR
- Published in Emerging Targets
Digging into Dopamine Signaling: Arginine Methylation Regulates GPCRs
Monday, 25 January 2016
The neurotransmitter dopamine is one of the most fascinating substances regulating behavior, with both delightful and dark qualities. Affecting a mere 20,000 dopamine-responsive neurons out of 100 billion neurons in the human brain, dopamine nonetheless governs critical aspects of our existence including voluntary movement, psychosis, and addiction. Disrupted dopamine signaling is involved in maladies ranging
- Published in Emerging Targets
New Target for Heart Disease and Cancer: Glucosylceramide Synthase (GCS)
Tuesday, 20 October 2015
Two recent publications have indicated that an unassuming glycosphingolipid that has long been associated with rare metabolic disorders may contribute to heart disease and cancer, the two leading causes of death in the United States. Glycosphingolipids (GSLs) are complex membrane lipids that play diverse roles in cell communication, especially during development. Patients with Gaucher or
- Published in Emerging Targets
Validation of a GEF Inhibitor in Murine Models of Major Osteolytic Diseases
Tuesday, 22 September 2015
Healthy bones are strong, but forming healthy bones requires a delicate balance between bone-building osteoblasts and bone-degrading osteoclasts. If the action of osteoclasts prevails and bone resorption exceeds bone deposition, bone-diminishing diseases such as osteoporosis occur. The answer seems simple: target osteoclasts as the enemy. But drugs currently available to rein in excessive osteoclast activity
- Published in Emerging Targets
Nanoparticles Target Cancer’s Sweet Spot
Thursday, 05 February 2015
Nearly half a century ago it was discovered that the overexpression of sialic acid sugars on the surface of cancer cells aided their ability to metastasize, and thus, sialic acid sugars became a potential therapeutic target. Recent advances in glycobiology and cancer research have helped to elucidate the exact roles sialic acid sugars play in
- Published in Emerging Targets
