Aryl Hydantoin Heterocycle Compounds that Target the Androgen Receptor for Prostate Cancer Treatment

Prostate cancer is the most prevalent form of cancer among all men in the United States (US). It is also the second leading cause of cancer-related deaths in the US among men, largely due to the progressively treatment resistant nature of the disease. Treatment options for early stage prostate cancer include watchful waiting, radical prostatectomy, radiation therapy, and importantly androgen-deprivation therapy (ADT). Prostate cancer is dependent on androgen hormones, such as testosterone, for sustaining and promoting growth. Androgen hormones bind to the Androgen receptor (AR), causing AR localization to the nucleus where a complex is formed that regulates the transcription of critical genes. ADT is accomplished through administering an antagonist to the AR that blocks androgen ligands, or by castration (physical or chemical) to reduce the amount of testosterone. However, the disease frequently advances to castration resistant prostate cancer (CRPC), becoming resistant to these therapies by overexpressing AR. Additional anti-androgens have been developed, though these have had limited improvements in patient outcomes and are not effective against the refractory forms of prostate cancer.  Recently, antiandrogenic diaryl thiohydantoin compounds have been shown to be more promising prostate cancer therapeutics. These compounds have shown success in clinical trials, though still with only mild improvement of patient outcomes. Therefore, more potent forms of these compounds ...
Source: NIH OTT Licensing Opportunities - Category: Research Authors: Source Type: research

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This study found some support for a causal association between elevated serum IGF‐1 levels and increased risk of colorectal cancer. There was inconclusive or no evidence of a causal association of IGF‐1 levels with prostate, breast, and other cancers.
Source: Cancer Medicine - Category: Cancer & Oncology Authors: Tags: ORIGINAL RESEARCH Source Type: research
ConclusionHigh likelihood of MRI within the oncologic context represents important distinction criteria for neuromodulation as patients may benefit from implantation of an MR conditional system.
Source: Neuromodulation: Technology at the Neural Interface - Category: Biotechnology Authors: Tags: Review Article Source Type: research
n Many breast and prostate cancers are driven by the action of steroid hormones on their cognate receptors in primary tumors and in metastases, and endocrine therapies that inhibit hormone production or block the action of these receptors provide clinical benefit to many but not all of these cancer patients. Because it is difficult to predict which individuals will be helped by endocrine therapies and which will not, positron emission tomography (PET) imaging of estrogen receptor (ER) and progesterone receptor (PgR) in breast cancer, and androgen receptor (AR) in prostate cancer can provide useful, often functional, in...
Source: Cancers - Category: Cancer & Oncology Authors: Tags: Review Source Type: research
Voltage-gated sodium channels (VGSCs), which are abnormally expressed in various types of cancers such as breast cancer, prostate cancer, lung cancer, and cervical cancer, are involved in the metastatic process of invasion and migration. Nav1.5 is a pore-forming α subunit of VGSC encoded by SCN5A. Various studies have demonstrated that Nav1.5, often as its neonatal splice form, is highly expressed in metastatic breast cancer cells. Abnormal activation and expression of Nav1.5 trigger a variety of cellular mechanisms, including changing H+ efflux, promoting epithelial-to-mesenchymal transition (EMT) and the expression...
Source: Frontiers in Pharmacology - Category: Drugs & Pharmacology Source Type: research
Using a particular low-energy radiotherapy approach with a radiolabeled antibody...Read more on AuntMinnie.comRelated Reading: SNMMI 2020: PET tracer could image, treat glioblastoma SPECT agent could help spot DNA damage from radiotherapy PSMA-PET/CT again shows prowess for prostate cancer PET rules out need for radiotherapy in lymphoma patients Childhood radiotherapy, chemo boost breast cancer risk
Source: AuntMinnie.com Headlines - Category: Radiology Source Type: news
AbstractObjectivesTetrandrine, a natural bisbenzylisoquinoline alkaloid, possesses promising anticancer activities on diverse tumours. This review provides systematically organized information on cancers of tetrandrinein vivo andin vitro, discuss the related molecular mechanisms and put forward some new insights for the future investigations.Key findingsAnticancer activities of tetrandrine have been reported comprehensively, including lung cancer, colon cancer, bladder cancer, prostate cancer, ovarian cancer, gastric cancer, breast cancer, pancreatic cancer, cervical cancer and liver cancer. The potential molecular mechani...
Source: Journal of Pharmacy and Pharmacology - Category: Drugs & Pharmacology Authors: Tags: Review Source Type: research
AbstractAs standard treatments for cancer, DNA-damaging chemotherapeutic agents and irradiation therapy improve survival in patients with various cancers. Wee1, a kinase associated with the cell cycle, causes G2/M cell cycle arrest to allow repair of injured DNA in cancer cells, and a Wee1 inhibitor has been confirmed to lead to apoptosis in cancer cells. Recently, there has been renewed interest in exploring the immune environment which plays a significant role in tumour suppression. A Wee1 inhibitor combined with radiotherapy has been tested in lung, pancreatic, and prostate cancer and melanoma in vivo or in vitro. There...
Source: Medical Oncology - Category: Cancer & Oncology Source Type: research
Abstract Uncontrolled regulation of cyclin dependent kinases (CDKs) has negative implications in many cancers and malignancies and has recently led to the approval of select CDK inhibitors. Herein we present data reporting that xanthones, a class of compounds isolated from the purple mangosteen (Garcinia mangostana) fruit, can inhibit CDK2/CyclinE1. We evaluated nine different xanthones, including α-mangostin, β-mangostin, γ-mangostin, gartanin, 8-desoxygartanin, garcinone C, garcinone D, 9-hydroxycalabaxanthone, and 3-isomangostin for toxicity in 22Rν1 (prostate cancer cells) and MDA-MB-231 (b...
Source: Natural Product Research - Category: Biochemistry Authors: Tags: Nat Prod Res Source Type: research
ConclusionIn this study, we identified aBRCA2 c.8827C>T nonsense mutation with a truncated BRCA2 protein in a consanguineous Chinese Han family, suggesting individuals with this mutation should be regularly screened for malignancies such as breast, prostate, and ovarian cancer. Our study verified the function of thisBRCA2 mutation site and provided a new target for the precise treatment of such patients.
Source: Molecular Genetics & Genomic Medicine - Category: Genetics & Stem Cells Authors: Tags: ORIGINAL ARTICLE Source Type: research
CONCLUSION: Around 5% of French general practice consultations include cancer screening or follow-up. Socio-economical inequalities demand further research. PMID: 32674614 [PubMed - in process]
Source: European Journal of General Practice - Category: Primary Care Tags: Eur J Gen Pract Source Type: research
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