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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 2015,29 Sep 2016

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New York University New York 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 initiated our study by successfully synthesizing a set of conjugates with anti-androgens linked to the peptidomimetic backbone at variable intervals along the molecular chain. We have evaluated these compounds and established that some conjugates can block androgen-dependent prostate cancer cell growth. The compounds have demonstrated efficacy through in vivo studies of prostate cancer tumor growth. We have recently published these important initial findings in the journal Cancer Research.

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  • Medicine and Medical Research
  • Biochemistry

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