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Multivalent Peptidomimetic Conjugates as Inhibitors of Androgen Receptor Function in Therapy-Resistant Prostate Cancer

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Technical Report,30 Sep 2016,29 Sep 2017

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Scripps Florida Jupiter United States

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Androgens are hormones that play a critical role in stimulating prostate cancer growth. Androgens activate a protein called the androgen receptor AR, which regulates genes involved in cell growth. Although powerful anti-androgen drugs can be administered to block AR action and have been used successfully to treat patients with prostate cancer, over time the tumors become resistant to the drugs, leaving few treatment options. The goal of this proposal is to develop a new approach to block AR activity and stop prostate cancer growth using a new family of molecules called multivalent peptidomimetic conjugates. We have previously demonstrated that a conjugate with two ethisterone steroidal groups arrayed with eight intervening monomers, MPC6, had the greatest anti-proliferative effect in LNCaP-abl cells a cellular model advanced disease that express AR, and proliferates in the absence of androgen, with more or less intervening monomers in between the ethisterone ligands diminishing compound activities. We are now creating a set of MPC6 variants, and evaluating if they block androgen-dependent prostate cancer cell growth. To understand how these molecule blocks AR function, we will determine the three-dimensional structure of AR bound to MPC6. These studies will be used to guide our ability to tailor the conjugates for optimal interactions with the AR.

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  • Medicine and Medical Research

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