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Advancing Drug Discovery: Co-Crystallization of Inhibitor Compounds
Published On 01/12/2025 7:07 PM
Advancing Drug Discovery: Co-Crystallization of Inhibitor Compounds
Enzalutamide: A Breakthrough in Prostate Cancer Treatment
Enzalutamide is a second-generation androgen receptor antagonist widely recognized for its significant role in prostate cancer treatment. By binding to the intracellular androgen receptor and preventing its translocation into the nucleus, Enzalutamide inhibits the transcription of genes that drive cancer progression. This compound, marketed under the trade name Xtandi®, has been approved for treating metastatic castration-resistant prostate cancer (mCRPC).
However, the development of this second-generation inhibitor was made possible through critical insights gained from studying the binding mechanisms of earlier inhibitors. Specifically, the co-crystal structure of bicalutamide, a first-generation androgen receptor inhibitor, with mutant androgen receptors provided invaluable structural data. This knowledge paved the way for the design and development of more effective next-generation inhibitors like Enzalutamide, as reported in a landmark study by Tran et al. (2009).
Structure-Based Drug Design: Unlocking New Possibilities
Co-crystallization plays a vital role in modern drug discovery, especially in understanding how inhibitors bind to target proteins. At Aurora Biolabs, a subsidiary of Structure Based Design, Inc. (SBD), we specialize in delivering comprehensive solutions for drug discovery using structure-based approaches. Our services include:
Production of crystallography-grade proteins
Assay development
Screening of potential inhibitors
Co-crystallization and structural analysis
Assay development
Screening of potential inhibitors
Co-crystallization and structural analysis
These integrated services enable researchers to accelerate the development of next-generation therapeutic compounds by providing high-quality structural insights.
Why Co-Crystallization Matters in Drug Development
Co-crystallization of inhibitors with their target proteins is essential for gaining precise structural information about binding interactions. This approach aids in:Identifying binding sites for lead compounds
Optimizing drug design through improved molecular interactions
Predicting resistance mechanisms, leading to better treatment strategies
Optimizing drug design through improved molecular interactions
Predicting resistance mechanisms, leading to better treatment strategies
Through our state-of-the-art co-crystallization services, Aurora Biolabs supports research teams in developing novel therapeutics targeting a wide range of diseases, including cancer and other genetic disorders.
Explore Our Solutions
Whether you're in the early stages of drug discovery or optimizing lead compounds, our one-stop solution ensures you receive end-to-end support for your structure-based drug design needs. [Contact Us] to discuss your project.
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