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PROTAC has shown utility as a targeted protein degradation technology in prostate cancer treatment. A key advantage of PROTAC is that it can be used for more than one round of degradation. Unlike conventional inhibitors, PROTAC repeats the transient binding process of the target protein to the E3 ligase multiple times. As a leading CRO, BOC Sciences has expertise in PROTAC and is able to provide comprehensive PROTAC design and development services for prostate cancer drug discovery.
The prostate is a gland found only in men and it is located below the bladder and in front of the rectum. Almost all prostate cancers are adenocarcinomas, and these develop from the cells of the gland. Prostate cancer has the second highest incidence among cancers in men worldwide and is the second leading cause of cancer deaths of men in the United States.
Although the etiology of disease progression may be complex, it is believed that inhibition of AR signaling and AR levels will hopefully lead to tumor regression and treatment of the disease. In addition, inhibitors of bromodomain and extra-terminal (BET) family proteins have been reported to show tumor growth inhibitory activity.
BET inhibitors can disrupt the direct binding of BET proteins 2, 3 and 4 (BRD2/3/4) to the AR, resulting in the abrogation of AR-mediated transcription. Therefore, BET proteins may be attractive targets for prostate cancer therapy.
PROTAC is a three-part molecule: a ligand that interacts with the protein of interest, another ligand that binds to the E3 ligase, and a linker that connects the two ligands. PROTACs utilize a ubiquitin-mediated degradation system as a therapeutic strategy for prostate cancer. The development of ligands targeting AR has yielded a series of PROTACs with preclinical activity. By tagging AR with ubiquitin to block the AR signaling axis on which prostate cancer depends so that it can shuttle to the proteasome for degradation. Other ligands have since been developed, such as BET inhibitors. BET-PROTAC has been studied in indications such as prostate cancer, and it offers therapeutic opportunities to target transcription, particularly to some transcription factors that are considered undruggable targets.
Among a series of biologically active PROTAC molecules targeting AR, several PROTAC drugs are currently in early clinical development. They are disclosed to be ARV-110, ARV-766, and CC-94676, all of which target the nuclear receptor AR, as well as administered via the oral route. As an example, ARV-110 is consist of an AR ligand on one end and recruits a specific ubiquitin E3 ligase on the other end, as well as a linker to help localize the target protein and the ligase. According to its clinical data, ARV-110 has shown some efficacy in men with metastatic castration-resistant prostate cancer (mCRPC), and is well tolerated.
As a CRO with expertise in PROTAC, BOC Sciences is committed to designing, discovering and optimizing PROTACs for the treatment of prostate cancer and assisting clients in developing effective PROTAC molecules. Our well-established PROTAC platform technology can provide services in all aspects of drug discovery, including:
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* PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
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