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Tobias A Mattei, Carlos R Goulart, Shawn S Rai, Azeem A Rehman, Michelle Williams, Ehud Mendel
BACKGROUND: Previous studies have described the association of spinal epidural lipomatosis with several conditions including chronic steroid therapy, Cushing's syndrome, obesity, Paget's disease, and hypothyroidism. We present a report of rapid development of spinal epidural lipomatosis after treatment with second-generation anti-androgen therapy, a new strategy for treatment of metastatic castration-resistant prostate cancer which has been increasingly employed in the past few years...
February 11, 2019: World Neurosurgery
Tokutaro Yamaguchi, Joo-Ho Lee, A-Rang Lim, Eun-Ji Yu, Tae-Jin Oh
Recently, studies on the steroidal hormone activity in the brain have attracted attention, and the influences of the varied glucosides and their artificial derivatives have been discussed; additionally, it has been suggested that glucosides are the synthetic precursors of glucuronide as a label molecule. However, glucosides are formed with 11α-hydroxyprogesterone (1), which is important as a blood pressure regulator, but anti-androgen activity remains unknown. Using UDP-glucosyltransferase, glucoside synthesis was successful in linking β-D -glucopyranose and β-D -laminaribiose to 11α oxygen of 1 at a high conversion ratio, and full assignment structure was analyzed for the two glucosides by high-resolution quadrupole-time flight electrospray ionization-mass spectrometry, 1D (1 H and 13 C) NMR and 2D (COSY, ROESY, HSQC-DEPT and HMQC) NMR...
February 9, 2019: Steroids
Sahar Kandil, Kok Yung Lee, Laurie Davies, Sebastiano A Rizzo, D Alwyn Dart, Andrew D Westwell
Deshydroxy propioanilides were synthesised by Michael addition reaction between substituted thiophenols onto four different phenylacrylamide derivatives to give twenty-three novel deshydroxy bicalutamide derivatives lacking the central hydroxyl group. The antiproliferative activities of these compounds were evaluated against human prostate cancer cell lines and thirteen compounds showed better inhibitory activities (IC50  = 2.67-13.19 μM) compared to bicalutamide (IC50  = 20.44 μM) in LNCaP. Remarkably, novel double branched bicalutamide analogues (27 and 28) were isolated as major by-products and found to have the best activity across three human prostate cancer cell lines (LNCaP, VCaP and PC3)...
February 2, 2019: European Journal of Medicinal Chemistry
Taro Iguchi, Satoshi Tamada, Minoru Kato, Sayaka Yasuda, Taiyo Otoshi, Kosuke Hamada, Takeshi Yamasaki, Tatsuya Nakatani
BACKGROUND: Alternative anti-androgen therapy (AAT) with flutamide after combined androgen blockade (CAB) therapy with bicalutamide for metastatic prostate cancer is common. However, no studies have compared enzalutamide without AAT with enzalutamide after AAT with flutamide as treatment for castration-resistant prostate cancer (CRPC). We aimed to compare the efficacies of flutamide and enzalutamide for CRPC. METHODS: In our hospital, 55 patients were diagnosed with CRPC after CAB therapy and administered flutamide or enzalutamide between May 2014 and December 2017...
February 11, 2019: International Journal of Clinical Oncology
Vibha Singh, Praveen Kumar Jaiswal, Ishita Ghosh, Hari K Koul, Xiuping Yu, Arrigo De Benedetti
Standard therapy for advanced Prostate Cancer (PCa) consists of anti-androgens, which provide respite from disease progression, but ultimately fail resulting in the incurable phase of the disease: mCRPC. Targeting PCa cells before their progression to mCRPC would greatly improve the outcome. Combination therapy targeting the DNA Damage Response (DDR) has been limited by general toxicity, and a goal of clinical trials is how to target the DDR more specifically. We now show that androgen deprivation therapy (ADT) of LNCaP cells results in increased expression of TLK1B, a key kinase upstream of NEK1 and ATR and mediating the DDR that typically results in a temporary cell cycle arrest of androgen responsive PCa cells...
February 9, 2019: International Journal of Cancer. Journal International du Cancer
Hee-Seok Lee, Seok-Hee Lee, Yooheon Park
Endocrine-disrupting chemicals (EDCs) interfere with the biological activity of hormones. Among EDC's, (anti-)androgenic compounds potentially cause several androgen-related diseases. To improve the accuracy of an in vitro transactivation assay (TA) for detection of (anti-)androgenic compounds, We established the glucocorticoid receptor (GR) knockout 22Rv1/MMTV cell line by using an RNA-guided engineered nuclease (RGEN)-derived CRISPR/Cas system. The 22Rv1/MMTV GRKO cell line was characterized and validated by androgen receptor (AR)-mediated TA assay compared with the AR-TA assay using 22Rv1/MMTV...
January 11, 2019: Environmental Research
C Mary Schooling, Jie V Zhao
Bromodomain and extra-terminal (BET) inhibitors, acting via epigenetic mechanisms, have been developed recently as potential new treatments for cancer, including prostate cancer, and inflammatory conditions. Some BET inhibitors, such as RVX-208, also raise high-density lipoprotein cholesterol (HDL-C) and apolipoprotein A-1 levels. A recent meta-analysis of three small trials (n = 798) found that RVX-208 protected against major adverse cardiovascular events (MACE), raising the question as to whether this protective effect was an artefact, a chance finding, or mediated by HDL-C, anti-inflammatory pathways, or other factors...
January 29, 2019: American Journal of Cardiovascular Drugs: Drugs, Devices, and Other Interventions
Karin Purshouse, Andrew S Protheroe
More than a million men worldwide are diagnosed with prostate cancer every year. After androgen deprivation therapy (ADT), chemotherapy has been the only subsequent intervention to improve survival in the metastatic setting but has limitations for patients who may not tolerate its toxicity profile or are not candidates on the basis of comorbidities. Novel anti-androgens such as abiraterone acetate have shown promise for such patients. This review draws on clinical evidence and experience to identify abiraterone as a well-tolerated, effective alternative to docetaxel...
January 2019: Therapeutic Advances in Urology
Aennes Abbas, Ilona Schneider, Anna Bollmann, Jan Funke, Jörg Oehlmann, Carsten Prasse, Ulrike Schulte-Oehlmann, Wolfram Seitz, Thomas Ternes, Marcus Weber, Henning Wesely, Martin Wagner
The assessment of water quality is crucial for safeguarding drinking water resources and ecosystem integrity. To this end, sample preparation and extraction is critically important, especially when investigating emerging contaminants and the toxicity of water samples. As extraction methods are rarely optimised for bioassays but rather adopted from chemical analysis, this may result in a misrepresentation of the actual toxicity. In this study, surface water, groundwater, hospital and municipal wastewater were used to characterise the impacts of common sample preparation techniques (acidification, filtration and solid phase extraction (SPE)) on the outcomes of eleven in vitro bioassays...
January 2, 2019: Water Research
Nirmish Singla, Rashed A Ghandour, Ganesh V Raj
The treatment and management of prostate cancer continues to evolve; newer classes of agents and combination therapies are being developed and some are being investigated in early phase clinical trials. Areas covered: We discuss investigational hormonal agents for the treatment of prostate cancer and focus primarily on luteinizing hormone releasing hormone (LHRH) agonists in early stage trials. We look at agents that target the hormonal axis, including anti-androgens, gonadotropins, estrogenic agents and progestogenic agents and other non-hormonal agents often used in combination with LHRH agonists...
March 2019: Expert Opinion on Investigational Drugs
Manhai Long, Mandana Ghisari, Lisbeth Kjeldsen, Maria Wielsøe, Bent Nørgaard-Pedersen, Erik Lykke Mortensen, Morsi W Abdallah, Eva C Bonefeld-Jørgensen
Background: Evidence has indicated that some non-inherited factors such as exposure to environmental pollutants are associated with neurodevelopment disorders like autism spectrum disorder (ASD). Studies report that endocrine disrupting compounds (EDCs), including polychlorinated biphenyls, organochlorine pesticides, perfluoroalkyl substances (PFAS), and some metals, have adverse effects on the fetal neurodevelopment. The aim of this study was to measure the amniotic fluid (AF) levels of EDCs and metals as well as the receptor transactivities induced by AF and investigate the possible link between prenatal exposure to EDCs and heavy metals and ASD risk...
2019: Molecular Autism
Stefan Pj van Leeuwen, Toine Fh Bovee, Mohamad Awchi, Mirjam D Klijnstra, Astrid Rm Hamers, Ron Lap Hoogenboom, Liza Portier, Arjen Gerssen
Information on the occurrence and endocrine potencies of analogues of bisphenol A (BPA) and diglycidyl ester derivatives (BDGEs) of BPA and BPF is limited. Such information is, however, important as the current debate on BPA and the lowered BPA migration limit in Europe may provide an incentive for application of structural analogues. A new sensitive multi-analyte LC-ESI-MS/MS method was developed to measure 17 bisphenols (BPs) and 6 BDGEs in food, beverages and drinkware. Yeast based bioassays were used to determine the in vitro (anti)estrogenic and (anti)androgenic properties of these and 7 additional BPs and BDGEs...
December 28, 2018: Chemosphere
J M Molina-Molina, I Jiménez-Díaz, M F Fernández, A Rodriguez-Carrillo, F M Peinado, V Mustieles, R Barouki, C Piccoli, N Olea, C Freire
Bisphenol A (BPA) is a high-production-volume chemical with endocrine disrupting properties commonly used as color developer in thermal paper. Concerns about the potential hazards of human BPA exposure have led to the increasing utilization of alternatives such as bisphenol S (BPS) and bisphenol F (BPF). This study was designed to assess: (i) BPA, BPS, and BPF concentrations in 112 thermal paper receipts from Brazil, France, and Spain by liquid chromatography coupled to mass spectrometry (LC-MS); and (ii) hormone-like activities of these receipts using two receptor-specific bioassays, the E-Screen for (anti-)estrogenicity and PALM luciferase assay for (anti-)androgenicity...
December 21, 2018: Environmental Research
Jerilynn C Prior
Background: Although the 2017 Endocrine Society Guidelines for gender dysphoria stipulated that cross-sex hormone therapy (CHT) achieve gonadal steroid levels equivalent to those of a cis-person of the chosen sex, for transwomen (male-to-female gender dysphoria) current gonadal therapy is usually estradiol. Accumulated evidence indicates that normally ovulatory menstrual cycles are necessary for ciswomen's current fertility as well as for later life bone and cardiovascular health and the prevention of breast and endometrial cancers...
January 3, 2019: Journal of Clinical Endocrinology and Metabolism
Jung Kwon Kim, Jung Jun Kim, Taek Won Gang, Tae Kyun Kwon, Hong Sup Kim, Seung Chul Park, Jae-Shin Park, Jong-Yeon Park, Seok Joong Yoon, Youn-Soo Jeon, Jin Seon Cho, Kwan Joong Joo, Sung-Hoo Hong, Seok-Soo Byun
We aimed to evaluate the current nationwide trend, efficacy, safety, and quality of life (QoL) profiles of hormone treatment in real-world practice settings for prostate cancer (PCa) patients in Korea. A total of 292 men with any biopsy-proven PCa (TanyNanyMany) from 12 institutions in Korea were included in this multi-institutional, observational study of prospectively collected data. All luteinizing hormone-releasing hormone (LHRH) agonists were allowed to be investigational drugs. Efficacy was defined as (1) the rate of castration (serum testosterone ≤50 ng dl-1 ) at 4-week visit and (2) breakthrough (serum testosterone >50 ng dl-1 after castration)...
December 25, 2018: Asian Journal of Andrology
Yu-Chiao Chiu, Tzu-Hung Hsiao, Li-Ju Wang, Yidong Chen, Yu-Hsuan Joni Shao
BACKGROUND: Single-cell RNA sequencing (scRNA-Seq) is an emerging technology that has revolutionized the research of the tumor heterogeneity. However, the highly sparse data matrices generated by the technology have posed an obstacle to the analysis of differential gene regulatory networks. RESULTS: Addressing the challenges, this study presents, as far as we know, the first bioinformatics tool for scRNA-Seq-based differential network analysis (scdNet). The tool features a sample size adjustment of gene-gene correlation, comparison of inter-state correlations, and construction of differential networks...
December 21, 2018: BMC Systems Biology
Mónica Aquilino, Paloma Sánchez-Argüello, Marta Novo, José-Luis Martínez-Guitarte
The fungicide vinclozolin (Vz) is an endocrine disruptor with known anti-androgenic activity in vertebrates. However, there is a lack of information about the Vz mode of action in invertebrates, although some studies have shown that this compound can produce alterations in different species. Transcriptional activity was analyzed in the freshwater snail Physella acuta in order to elucidate putative cellular processes altered by this chemical during a response. In order to identify potential molecular biomarkers, a de novo transcriptome was generated for this species that constitutes a valuable source for future studies...
December 18, 2018: Ecotoxicology and Environmental Safety
Krittika Krishnan, Shafaqat Rahman, Asbiel Hasbum, Daniel Morales, Lindsay M Thompson, David Crews, Andrea C Gore
Endocrine-disrupting chemicals (EDCs) can act upon a developing organism to change its endocrine health and behavior in adulthood. Beyond actions on the exposed individuals, transgenerational effects of several EDCs have been reported. This study assessed the combinatorial impact of EDC-altered maternal care and transgenerational inheritance on F3 male and female offspring. Pregnant rats were exposed to EDCs with different modes of action: the weakly estrogenic polychlorinated biphenyl (PCB) mixture Aroclor 1221, the anti-androgenic fungicide vinclozolin (VIN), or the vehicle (6% dimethylsulfoxide in sesame oil; VEH) during embryonic development...
December 18, 2018: Hormones and Behavior
Alexia Bossan, Richard Ottman, Thomas Andl, Md Faqrul Hasan, Nupam Mahajan, Domenico Coppola, Ratna Chakrabarti
BACKGROUND: FGD4 (Frabin) is an F-actin binding protein with GTP/GDP exchange activity specific for CDC42. It is involved in reorganization of the actin cytoskeleton, which requires both actin binding and CDC42 activating function of FGD4. Expression of FGD4 is altered in patients with heterogeneous hereditary motor and sensory neuropathies as a result of demyelination of peripheral nerves. METHODS: In this study, we examined the expression of FGD4 in prostate cancer specimens using immunohistochemistry and studied the function of FGD4 in maintaining cell phenotype, behavior and drug sensitivity using overexpression and siRNA-based silencing approaches...
December 17, 2018: BMC Cancer
Harsh Shah, Ulka Vaishampayan
With the decrease in PSA screening based on the 2011 United States Preventive Services Task Force guidelines and the potential approval of highly sensitive imaging techniques over the next few years, we are likely to see an increasing trend of metastatic prostate cancer diagnosis. Traditional therapy for nonmetastatic prostate cancer (nmPC) has consisted of androgen deprivation therapy (ADT) followed by other hormonal therapy maneuvers, such as anti-androgen withdrawal, herbal preparations, low dose steroids, or ketoconazole...
December 7, 2018: Targeted Oncology
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