METTL3 is a Significant Focus in Cancer Research

METTL3 Acts as a Tumor Promoter
Methyltransferase-like 3 (METTL3) is a 70 kDa protein, 580 amino acids in length. It is the principal catalytic agent for most of the N6– methyladenosine (m6A) modifications that occur in eukaryotic cell mRNA. METTL3 typically places methyl adducts at the adenosine in motifs, such as DRACH, RAC, or RRACH. As such, it influences mRNA splicing,
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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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DDX6 Regulates mRNA Transcription & Translation Pathways

DDX6 regulates RNA transcription and translation
DDX6 (RCK/p54) was first isolated from the RC-K8 B-cell lymphoma line over 30 years ago. This 472 amino acid, 53.2 kDa “DEAD-Box” ATP-dependent RNA helicase bears the signature Asp-Glu-Ala-Asp motif, characteristic of all DEAD box proteins. Dead box proteins contain both ATPase and helicase activity, and are known for their particular protein-protein and RNA-protein interactions
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Transcreener ADP2 Assay Helps Uncover the Mechanics of Oncogenic PIK3CA Mutations

Scientist using Transcreener Assay to Study PIK3CA Mutation
The PIK3CA gene codes for the 110 kDa catalytic subunit (p110α) of phosphoinositide 3-kinase (PI3Ka). Together with its regulatory component, p85α (encoded by PIK3R), they comprise the powerful PI3Ka heterodimer. This heterodimer conducts growth impulses from multiple cell surface receptor tyrosine kinases (RTKs) to the interior of the cell. It is known that individual missense
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Targeting DDX5 Inhibitors to Battle Cancers & Viral Infections

DDX5 Inhibitors Targeting Colon Cancer
DDX5 (Dead-Box 5 or p68) is a member of a family of 37 “DEAD-Box” ATP-dependent RNA helicases that play a role in nearly all aspects of RNA processing and also act as nucleic acid recognition receptors for viral immunity. Dysregulation and/or overexpression of DDX5 can lead to tumor progression. It can also be hijacked by
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[Webinar] Targeting DNA Damage Repair for Drug Discovery Using the Transcreener ADPR® Assay

Preview of DNA Damage Repair Webinar
Interested in DNA damage repair pathways for drug discovery? Join us for a live webinar, where Ha Pham, senior scientist at BellBrook Labs, will be sharing her expertise on using the Transcreener ADPR Assay, a biochemical HTS assay, to study enzymes involved in DNA damage repair. She will use CD38 and PARG as target examples
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Transcreener® ADP2 Assay Delivers Precise Measurement of Functional MAPK14 Residence Time

Calculating MAPK14 Residence Time
Researchers at the University of Tubingen use Transcreener to uncover how residence time works on a molecular level with p38α MAPK Inhibitors – Many factors affect the effectiveness of ligand-substrate or drug-target interactions. Conformational docking and stearic considerations help inform optimal “fits.” Ligand moiety solubility, both in free and bound forms, is also a consideration
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The Challenging Search for BTK Inhibitors

BTK's Involved in Systemic lupus erythematosus
Bruton’s Tyrosine Kinase (BTK) is a 76kDa non-receptor Tec kinase that plays numerous diverse roles in B-cell development, immunity, autoimmunity, infection, and cancer. From stem to stern, it consists of an N-terminal plekstrin homology (PH) domain, a TEC homology (TH) domain, two SRC homology (SH2 and SH3) domains, and a C-terminal kinase domain. Unlike SRC,
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SIRT2 Isoforms in Neurodegenerative Diseases & Cancer

SIRT2 Affects Neurodegenerative Diseases
Silent information regulator type 2 (Sirtuin 2 or SIRT2) is a highly evolutionarily conserved NAD+ dependent deacetylase. SIRT2 is the only Sirtuin that acts in the cytosol. It expresses in almost all tissues, but most abundantly in the central nervous system. While SIRT2 is classified as a type III histone deacetylase, it is also capable
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Can WRN Helicase Inhibitors Treat MSI-H Cancers?

Patient With WRN Helicase Syndrome
Over 100 years ago, Otto Werner first characterized a recessive autosomal disorder that caused premature, but largely typical, aging in adults, starting by the 3rd decade and resulting in death by the 6th decade via myocardial infarction or cancer. This disease, now known as Werner syndrome, is caused by specific alterations in the 162 KDa
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