MIT Researchers to Uncover More Potent Version of Kl-Arv-03 against Prostate Cancer Cell Lines

Release Date: 20-Nov-2020

Prostate cancer is among the most diagnosed cancer type in men, which is majorly driven by male sex hormone. A group of researchers have inclined their focus towards developing a small molecule that could target an important protein that is found to be stabilization of androgen receptor molecules. The group of researchers have identified an inhibitor of CDK9 which is believed to have high potency against prostate cancer cell lines and also some other types of cancers.  According to the researchers indulged in the respective clinical study, their developed compound will be able to end the resistance that most of the cancer cells developed during the prostate cancer treatment. 


The researchers used the small molecule microarray platform to study 50,000 compounds for interactions with androgen receptor variants. Among all the compounds that were tested by the researchers KI-ARv-03 was able to work against the cancer cell lines. As per the researchers, the lead compound found by them was able to cause a decline in the androgen receptor activity by reducing levels of both androgen receptor and the chemoresistance-associated variant of androgen receptor in CPRC models.


It was found by the researchers that the compound developed by them was binding to the cofactor cyclin-dependent kinase 9, which is considered to be important for the regulation of the cell cycle and also in stabilizing the androgen receptor molecule. It was observed that by binding to CDK9, their lead compound was able to destabilizes androgen receptor proteins and curbs the expression of oncogene. It was evaluated by the researchers that the inhibitor o CDK9 identified by them had potential in getting designed as an efficient cancer therapy. Also, it was observed that the compound KI-ARv-03 is only selective for Cyclin dependent kinase 9 and not any other family of CDKs. Therefore, the main focus was to develop a stronger version of the compound Kl-ARV-03 that is now called as KB-0742. It was found that the novel compound is able to deliver more potent anti-cancer activity when compared with other traditional therapies.


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