Researchers Use Transcreener Assay to Identify New PDE5 Inhibitor

Researchers Identify PDE5 Inhibitor Using Transcreener Assay
Phosphodiesterase 5 (PDE5) is most familiar in connection to sildenafil (Viagra), a popular pharmaceutical PDE5 inhibitor. In response to nitric acid-activated soluble guanylyl cyclase production of cGMP, dimeric PDE5 binds and hydrolyzes cGMP in vascular smooth muscles cells, lung, kidney, brain, cardiac myocytes, and platelets to create 5′-GMP. This is accomplished by cGMP binding to
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Exploring the Use of NUDT5 Inhibitors to Treat Breast Cancer

malignant adenocarcinoma could be treated by NUDT5 Inhibitors
NUDT5 is found to be overexpressed in certain cancers in humans Could NUDT5 inhibitors lead to new cancer treatments? NUDIX hydrolases are a superfamily of enzymes are found in all classes of organisms and are responsible for hydrolyzing modified nucleoside diphosphates. One of the most well-studied NUDIX hydrolases is NUDT1 (also known as MTH1); it
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The Role of CD38 Activity in the Impaired Immune Response

Scientist Working on CD38 Discovery
Cluster of differentiation 38 (CD38) is a multifaceted protein contributing to immune response, cell adhesion, and signal transduction. Furthermore, it plays a vital role in calcium signaling, which is necessary for further cell signaling. Calcium acts as a second messenger regulating muscle contraction, cell growth, fertilization, and cellular motility, to name a few areas of
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New Publication by the Scientists at BellBrook Labs – Development of a High-Throughput Assay to Identify Inhibitors of ENPP1

Inhibitors of ENPP1 SLAS Discovery
BellBrook scientist Meera Kumar and Robert Lowery were recently published in SLAS Discovery for their work entitled Development of a High-Throughput Assay to Identify Inhibitors of ENPP1. Ectonucleotide pyrophosphatase/phosphodiesterase 1 or ENNP1 has recently become a target for cancer immunotherapy. ENNP1 hydrolyzes nucleotides such as cGAMP and ATP. Cytosolic DNA is a trigger for the
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Using a Universal GMP Assay for PDE Research

GMP Assay for PDE Inhibitor Discovery
A universal GMP assay to aid in PDE research and potential COVID-19 disruption. – Phosphodiesterase enzymes (PDEs) modulate pathways throughout the body. Since unregulated PDEs contribute to disease in many cases, it makes sense therapies that inhibit these enzymes have the potential to treat several different ailments. These include cardiovascular and respiratory issues, diabetes, fibrotic
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ST6GAL1 Drug Discovery to Combat Cancer

ST6GAL1 Drug Discovery
The number of cancer hallmarks has increased as the knowledge and understanding of the disease progress. As many of us already know, the basic characteristic is a mutation that causes uncontrollable cell growth causing a tumor. Cancer is truly a multi-step development that enables cells to survive, proliferate and metastasize. Other hallmarks of the disease
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Helping Fight Ovarian Cancer with ST3GAL1 Inhibitors

Fighting Ovarian Cancer ST3GAL1 Inhibitors
Important functions such as cell–cell recognition, protein targeting, and cell adhesion taking place in the human body get carried out through a process known as sialylation. Sialylation is a common reaction that is catalyzed by a sialyltransferase (ST) enzyme with the goal of adding a sialic acid (monosaccharide) to a growing oligosaccharide forming a glycolipid
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ENPP1 Inhibitors, Assays, and Innate Immunity

ENPP1 Inhibitors Improve Innate Immunity
The human immune response is incredible. Unlike the adaptive immune response, the innate response acts quickly and is considered the first line of defense against pathogens and foreign DNA such as tumor cells. To be effective, the innate immune response relies on several cell types and a multitude of proteins such as interferons (INFs). This
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How A PDE Activity Assay Might Help Find New Treatments for Individuals Suffering from Heart Disease

PDE Activity Assay Heart Disease
Heart Disease: The Role of PDEs and a PDE Activity Assay Heart disease is often misunderstood due to confusion with terminology and the different types of heart disease that exist. While a heart attack can occur quickly, heart failure is a slower progression where the heart weakens over time. One thing is certain; heart disease
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Ubiquitin Ligase Assay: A Handy Tool for Drug Discovery

Ubiquitin Ligase Assay Tool for Drug Discovery
Can one cellular pathway contribute to many different types of disease? Research has shown that Ubiquitination is one such pathway due to its role in the regulation of protein degradation within homeostasis, cell cycle, and DNA repair. It has been established that at least the following diseases are among those affected from alterations in this
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