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
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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
Targeting Oncogenic Ras: Hope on the Horizon
Friday, 22 August 2014
Mutations in the small GTPase K-Ras are one of the most common known molecular drivers of cancer; approximately 30% of all human cancers contain the oncogenic mutant of K-Ras. Tumors containing oncogenic K-Ras are generally less responsive to therapies than other biological subtypes and consequently, patients with these tumors tend to have poorer outcomes. Directly
- Published in Emerging Targets
Overcoming the Blood-Brain Barrier: Increasing Access for Therapeutic Agents
Tuesday, 08 July 2014
The blood-brain barrier (BBB), a layer of endothelial cells lining the blood vessels leading to the brain, is one of the brain’s greatest assets. Responsible for determining what molecules are allowed to cross from the bloodstream into the brain, the BBB protects the brain from the invasion of infectious and toxic agents. However, this barrier
- Published in Emerging Targets
Targeting Host Kinases for Hepatitis C Treatment
Thursday, 12 June 2014
Traditionally, treatment of viruses has focused on targeting the viral proteins, however recent research has given rise to the idea of treating viruses by targeting host factors. The most advanced of these for Hepatitis C virus (HCV) is Alispovir, currently in Phase III clinical trials, which inhibits the peptidyl-prolyl isomerase activity of cyclophilin A. Building
- Published in Emerging Targets
