[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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DDX1: A Versatile RNA Helicase

DDX1 as a versatile RNA Helicase
DDX1 (Dead-Box Helicase 1) belongs to the DEAD-Box family of ATP-dependent RNA helicases, whose members are collectively involved in almost all aspects of RNA processing: from transcription to remodeling to degradation. They are named for the central Asp-Glu-Ala-Asp (DEAD) sequence they all possess. The 35 human DEAD-Box proteins comprise the largest family of helicases known.
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Investigating RAB2 as a Vesicle Transporter & Autophagy Initiator

RAB2 Transports Membrane Bound Vesicles
RAB2 is part of the RAB family of small GTPases that regulate intracellular trafficking of membrane bound vesicles. It is highly conserved in eukaryotes, from C. elegans to humans. These GTPases influence the creation, movement, attachment, fusion, and destiny of vesicles originating in the endoplasmic reticulum (ER)/Golgi systems. Like other members of its family, RAB2
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Is PARP1 a Hero or Villain?

PARP1 as a Hero vs Villain
Not counting histones, PARP1 [Poly(ADP-ribose) Polymerase 1] is the most abundant nuclear protein in mammalian cells. While principally known for its role in various types of DNA repair, recent work expanded it’s repertoire to include genome stability maintenance, chromatin remodeling, DNA methylation/gene expression, cellular differentiation, and cell survival modulation via NAD+/ATP regulation.1 It performs Poly(ADP-ribosyl)ation
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Advancements in The Ongoing Puzzle to Understand c-SRC

Ongoing Puzzle of c-SRC in Cancer Treatment
Nearly a half-century ago, sequences from the Rous Sarcoma Virus were used to identify the first proto-oncogene and the first of a family of non-receptor tyrosine kinases: c-SRC. Unlike its viral counterpart (v-SRC), c-SRC exists in both an active and inactive state. It is produced in almost every cell type, but expressed highest in the
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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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SARM1 Forefronts Research into Major Neurological Diseases

SARM1 Causes Axonal Death
SARM1 [Sterile alpha & toll/interleukin receptor (TIR) motif-containing protein 1] consists of a N-terminal mitochondrial localization sequence (NLS), an autoinhibitory HEAT/armadillo (ARM) domain, two tandem sterile alpha motif domains (SAMs), and a C-terminal toll/interleukin receptor domain (TIR). It is a human toll like receptor (TLR) adaptor protein. TLR adaptors (MYD88, MAL, TRIF, & TRAM) usually
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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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