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Category: Emerging Targets

EZH2 Methyltransferase Inhibitors Hold Promise for Combating Neuropathic Pain

Friday, 21 July 2017 by Bellbrook Labs
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
AptaFluor SAH Methyltransferase AssayAssay Development ServicesEPIGEN Methyltransferase AssayLead Discovery Servicesmethyltransferase
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  • Published in Emerging Targets, Epigenetics, HTS Assays
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Sialyltransferases: Sugar Makes the Medicine Go Down?

Monday, 26 June 2017 by Bellbrook Labs
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
Assay Development ServicesLead Discovery ServicesTranscreener AMP/GMP Assay
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  • Published in Emerging Targets
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BellBrook Labs Awarded NIH Grant to Develop a High Throughput cGAS Assay for Cancer and Autoimmune Disease Drug Discovery

Wednesday, 14 June 2017 by Bellbrook Labs
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
Assay Development Servicesdrug discovery servicesLead Discovery ServicesTranscreener cGAMP cGAS Assay
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  • Published in Emerging Targets, HTS Assays, News
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Ectonucleotidases: An Outside Chance for Drug Development

Friday, 28 April 2017 by Bellbrook Labs
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:
Assay Development Servicesdrug discovery servicesLead Discovery ServicesTranscreener ADP Kinase AssayTranscreener AMP/GMP Assay
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  • Published in Emerging Targets, HTS Assays, Uncategorized
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Fighting Infection’s Ghost

Wednesday, 15 June 2016 by Robyn Perrin
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
Transcreener cGAMP cGAS Assay
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  • Published in Emerging Targets
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Viruses take the STING out of innate immunity

Thursday, 09 June 2016 by Robyn Perrin
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
Transcreener cGAMP cGAS Assay
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  • Published in Emerging Targets
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Inhibition of Methyltransferase SMYD3 Targets Ras-driven Cancers

Wednesday, 04 May 2016 by Hannah Lucas
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
AptaFluor SAH Methyltransferase AssayEPIGEN Methyltransferase Assaymethyltransferasetumor suppressor
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  • Published in Emerging Targets
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Unraveling RhoGDIα Regulation

Friday, 15 April 2016 by Hannah Lucas
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
Transcreener GDP Assay
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  • Published in Emerging Targets
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Bound for Life: The First Irreversible Inhibitor of CDK2

Tuesday, 08 March 2016 by Hannah Lucas
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
Transcreener ADP Kinase Assay
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  • Published in Emerging Targets
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SIRT6: Keeping Tumor Cells in Check

Tuesday, 01 March 2016 by Hannah Lucas
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
deacetylationPKM2SIRT6Transcreener ADP Kinase Assaytumor suppressor
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  • Published in Emerging Targets
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