![]() ![]() In addition, all pages on Bizapedia will be served to you completely ad freeĪnd you will be granted access to view every profile in its entirety, even if the company chooses to hide the private information on their profile from the general public. Philadelphia (PA): AACR Cancer Res 2023 83(7_Suppl):Abstract nr 3078.Your entire office will be able to use your search subscription. In: Proceedings of the American Association for Cancer Research Annual Meeting 2023 Part 1 (Regular and Invited Abstracts) 2023 Apr 14-19 Orlando, FL. YIV-818-A enhanced apalutamide, darolutamide and enzalutamide action for prostate cancer treatment by down-regulating androgen receptor protein, inhibiting glucocorticoid receptor function and epigenetic regulation. Given R.C.’s safety profile, YIV-818-A also could be developed as a chemoprevention agent and/or anti-cancer prostate cancer drug.Ĭitation Format: Wing Lam, Mohammad Arammash, Wei Cai, Rong Hu, Shwu-Huey Liu, Peikwen Cheng, Yung-chi Cheng. R.C has a long history of safe, human usage in Asia as a dietary supplement for improving health. YIV-818-A and compound X could enhance anti-prostate cancer drug action against CRPC. In conclusion, YIV-818-A and compound X could overcome drug resistance caused by AR variants and GR by down-regulating AR protein, inhibiting GR function and epigenetic regulation. Most importantly, YIV-818-A and compound X showed synergies with apalutamide, darolutamide and enzalutamide to inhibit AR activity and growth of 22RV1 cells. YIV-818-A and compound X had the potential to affect epigenetics of 22RV1 cells by down-regulating Brd2 and Brd4 (BET: bromodomain and extra-terminal proteins which could serve as epigenetic readers to promote AR or GR-dependent gene transcription) and reduce histone 3 lysine 27 acetylation (H3K27Ac), which is required for BRDs binding, but not H3K9Ac or K14Ac. YIV-818-A and compound X could also inhibit KLK2, and PSA (AR target genes) mRNA expression induced by DHT or SGK (GR target gene) mRNA expression induced by DEX. YIV-818-A and compound X could down regulate both AR (full length) and AR-V (splice variants) protein but not GR protein of 22RV1 cells. Using activity guided purification of YIV-818-A, compound X was identified as the key active compound for inhibiting AR and GR activities. YIV-818-A was able to inhibit DHT or Dexamethasone (DEX) induced luciferase activity of 22RV1 cells which were harboring ARE luciferase reporter. The amount of compound X of R.C could be correlated to the potency of AR inhibition. R.C collected from different sources had different quantities of compound X. YIV-818-A was developed as a novel drug candidate based on optimized water extracts of Rubia cordifolia (R.C). Through our STAR (Signal, Transduction, Activity, and Response) Drug Discovery Platform, we studied the effects of three hundred medicinal plant extracts across 25 signaling pathways to identify a drug candidate. Developing a multi-targeted drug that can inhibit both the AR variant and GR action could help overcome drug resistance, increase durability, and improve the therapeutic outcome for prostate cancer patients. ![]() AR variants and glucocorticoid receptor (GR) (replacing AR function) are two key factors to promote resistance to AR-targeting therapies in CRPC patients. Androgen or Androgen receptor (AR) targeted therapy is a strategy for the treatment of prostate cancer, however, long-term treatment with androgen deprivation therapy inevitably leads to the development of Castration-Resistant Prostate Cancer (CRPC). Prostate cancer is the second leading cause of cancer death among men in the United States.
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