ABC Transporter MsbA Inhibitors Discovered to Help Fight Against Gram-Negative Bacteria

ABC Transporter Inhibitor Klebsiella Treatment
Gram-negative bacterial pathogens pose grave dangers in clinical and environmental settings alike. They include foodborne disease pathogens such as E. coli 0157:H7, waterborne pathogens such as Vibrio cholera, vector-borne pathogens such as Yersinia pestis, and a disturbingly large number of Gram-negative pathogens that now display resistance to multiple antimicrobial agents.1 Resistant Gram-negative pathogens include some
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NIH Awards BellBrook Labs Phase II Grant to Develop HTS Assays Targeting the cGAS-STING Pathway for Autoimmune Diseases and Cancer

Autoimmune Disease News
The National Institutes of General Medical Sciences (NIGMS) recently awarded BellBrook Labs a $1 million phase II Small Business Innovative Research (SBIR) grant to develop new assays to detect cyclic GMP-AMP (cGAMP) levels in biological samples. The assays will be used to discover, develop, and monitor new treatments for autoimmune diseases and cancer by targeting
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EZH2 Methyltransferase Inhibitors Hold Promise for Combating Neuropathic Pain

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
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Sialyltransferases: Sugar Makes the Medicine Go Down?

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
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BellBrook Labs Awarded NIH Grant to Develop a High Throughput cGAS Assay for Cancer and Autoimmune Disease Drug Discovery

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
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Ectonucleotidases: An Outside Chance for Drug Development

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:
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Fighting Infection’s Ghost

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
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Viruses take the STING out of innate immunity

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
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Inhibition of Methyltransferase SMYD3 Targets Ras-driven Cancers

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
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Unraveling RhoGDIα Regulation

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
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