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As a leading CRO in the pharmaceutical field, BOC Sciences is dedicated to the design, discovery, synthesis and optimization of effective PROTACs to assist our customers’ new drug development. With our comprehensive and advanced platform, we provide PROTAC molecules design services for treating Huntington disease.
Many neurodegenerative diseases are characterized by dysregulation of protein quality control mechanisms in neuronal cells to form intracellular protein aggregates. The accumulation of various pathogenic proteins leads to the development of different neurodegenerative diseases, including Huntington disease (HD). HD is an autosomal dominant, lethal disease resulting in a diverse range of behavioural, cognitive and physical symptoms. HD is caused by the N-terminal polyglutamine expansion of huntingtin protein (Htt). Promoting the degradation of mutant Htt (mHtt) via the ubiquitin-proteasome system (UPS) prior to aggregation would be a therapeutic strategy to delay or prevent the HD.
The UPS has been shown to play an important role in mHtt degradation. The ability of PROTACs to utilize the natural UPS in cells to promote the degradation of pathogenic proteins shows promising prospects for their HD treatment. PROTAC is a heterobifunctional compound consisting of two different ligands joined by a linker, one of the ligands recruits mHtt, the other ligand is specific for a E3 ubiquitin ligase.
The discovery of novel PROTAC protein degraders is one of the most promising approaches for neurologic diseases. PROTACs have important advantages with respect to other therapies, including:
PROTACs bring mHtt and the E3 ubiquitin ligase to a relative position that allows mHtt to be ubiquitinated and subsequently degraded by the proteasome. clAP1-based PROTAC has been reported, whose composition includes a specific ligand that can bind cellular inhibitor of apoptosis protein 1 (cIAP1). These PROTAC compounds would recruit cIAP1 to mHtt and induce selective degradation .
BOC Sciences provides custom protein expression and purification services covering a variety of ubiquitin ligases, such as cIAP1. Our extensive product portfolio also includes PROTAC, E3 ligase ligand-linker conjugate, ligand for E3 ligase, ligand for target protein and PROTAC Linker. If you are interested in our related products, please click to learn more.
* PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
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