EZH2 Methyltransferase Inhibitors Hold Promise for Combating Neuropathic Pain
Friday, 21 July 2017
When people experience neuropathic pain, they often describe “pins and needles” sensations or burning, shooting, or stabbing pain that can be agonizing and difficult to bear. In some cases, neuropathic pain is so intense that the pressure of clothing or the weight of a bed sheet can cause misery. Chronic neuropathic pain can be caused
- Published in Emerging Targets, Epigenetics, HTS Assays
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Sialyltransferases: Sugar Makes the Medicine Go Down?
Monday, 26 June 2017
Glycan structures decorate a wide variety of cell types—dotting the surface of blood cells, linked to lipid moieties on neurons, and studding the membrane of tumor cells. These carbohydrate structures create a cellular language that is translated by binding partners, eliciting specific downstream effects. And for some cancers, the effects can be devastating. Consider
- Published in Emerging Targets
BellBrook Labs Awarded NIH Grant to Develop a High Throughput cGAS Assay for Cancer and Autoimmune Disease Drug Discovery
Wednesday, 14 June 2017
BellBrook Labs was recently awarded a $288,000 SBIR Phase I grant from the National Institutes of General Medical Sciences (NIGMS) to develop an HTS assay for cyclic GAMP synthase, an enzyme that triggers immune responses to viruses and tumors. The new assay will be used in an effort to screen for cGAS enzyme modulators as
- Published in Emerging Targets, HTS Assays, News
Ectonucleotidases: An Outside Chance for Drug Development
Friday, 28 April 2017
Sometimes, the most intriguing cellular processes happen outside of the cell. Case in point: purinergic signaling pathways, in which extracellular receptors sense levels of purines in the extracellular milieu. The result? A wide array of effects on neuronal signaling, vascular tone, thrombosis, and immune function. But what controls the level of extracellular purines? Enter ectonucleotidases:
- Published in Emerging Targets, HTS Assays, Uncategorized
Fighting Infection’s Ghost
Wednesday, 15 June 2016
Aicardi–Goutières syndrome (AGS) is a rare and brutal genetic condition. Most infants born with the syndrome are asymptomatic at birth, but about 1 in 5 have enlarged spleen and liver, elevated liver enzymes in the blood, decreased platelet level, and abnormal neurological responses. Over the first year of life, things get much worse: episodes of
- Published in Emerging Targets
Viruses take the STING out of innate immunity
Thursday, 09 June 2016
Viral trespassers leave traces of themselves as they overtake cells. The presence of hallmark viral molecules—called PAMPs, for pathogen-associated molecular patterns—allows innate immune system sensors to detect the trail of viral substances as effectively as Sherlock Holmes in miniature. Some of these sensors, or pattern recognition receptors (PRRs), nose out viral DNA and RNA. When
- Published in Emerging Targets
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
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
