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Target Based Assays

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Targeting Transcription Factors in Drug Discovery

Transcription factors (TFs) play a crucial role in regulating gene expression and controlling a wide range of biological processes. Despite their significance, targeting transcription factors in drug discovery has traditionally been challenging. These proteins typically lack well-defined binding pockets, making it difficult to design small molecules that can modulate their activity effectively. Additionally, the complex interactions between transcription factors and DNA, as well as their involvement in multiprotein complexes, add layers of difficulty to developing targeted therapies. However, recent advancements in screening technologies, and computational modeling have revitalized interest in this field, opening new avenues for therapeutic interventions. 

At ICE Bioscience, we specialize in addressing challenging drug targets that were once considered undruggable and have developed a comprehensive suite of assays to evaluate the potency and efficacy of compounds across various transcription factors. These factors influence human tumor suppression, the inflammatory stress response, and essential cellular processes necessary for homeostasis.

Features

✅ An expanding collection of over 30 transcription factors, backed by more than 50 engineered cell lines that are readily available for use.

✅ A diverse array of assays spanning various disciplines, including biochemical, biophysical, cell-based, DMPK (drug metabolism and pharmacokinetics), and in vivo pharmacology assays.

✅ Comprehensive historical data detailing compound interactions with various transcription factors.

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Sample Assay List for p53, the Guardian of the Genome

p53, often referred to as the "guardian of the genome," is a crucial tumor suppressor protein that regulates cell cycle progression, apoptosis, and DNA repair. Its role in maintaining genomic stability is paramount, as it activates DNA Damage Response (DDR) pathways upon detecting DNA damage. The DDR involves a series of signaling cascades that halt cell cycle progression, allowing time for DNA repair or triggering apoptosis if the damage is irreparable. Mutations or dysregulation of p53 are implicated in numerous cancers, making it a prime target for therapeutic interventions aimed at restoring its normal function or mimicking its activity in p53-deficient tumors.

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The table below outlines our comprehensive assays for p53. We offer approximately 10 engineered cell lines specifically designed for TP53 pathway assessments, along with 4 types of p53 recombinant proteins. Additionally, the figure presents select biochemical and biophysical data related to p53. Our capabilities extend to systematically supporting the integrated drug discovery process, particularly for challenging-to-drug targets in oncology and immunology. Feel free to connect with our experts to explore how we can assist with your projects.

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Learn more from our poster presented at the 7th Annual DDR Inhibitor Summit

A Comprehensive p53 Drug Discovery Platform: From Target-Base Assays to In Vivo Models 

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We value your inquiries and are here to provide you with tailored solutions for your drug discovery and development needs. Whether you have questions, require more information, or are interested in discussing potential collaborations, our team of experts is just a message away.
Feel free to reach out to us.

We are a CRO service organization, not a hospital