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https://www.readbyqxmd.com/read/28105499/cx4945-suppresses-the-growth-of-castration-resistant-prostate-cancer-cells-by-reducing-ar-v7-expression
#1
Chuangzhong Deng, Jieping Chen, Shengjie Guo, Yanjun Wang, Qianghua Zhou, Zaishang Li, Xingping Yang, Xingsu Yu, Zhenfeng Zhang, Fangjian Zhou, Hui Han, Kai Yao
PURPOSE: The aberrant expression of casein kinase 2 (CK2) has been reported to be involved in the tumorigenesis and progression of prostate cancer. The inhibition of CK2 activity represses androgen-dependent prostate cancer cells by attenuating the androgen receptor (AR) signaling pathway. In this study, we examined the effect of CK2 inhibition in castration-resistant prostate cancer (CRPC) cells, in which AR variants (ARVs) play a predominant role. METHODS: A newly synthetic CK2 selective inhibitor CX4945 was utilized to study the effect of CK2 inhibition in CRPC cells by CCK8 assay and colony formation assay...
January 19, 2017: World Journal of Urology
https://www.readbyqxmd.com/read/28086774/androgenic-effects-of-aqueous-and-methanolic-extracts-of-ficus-asperifolia-in-male-wistar-rats
#2
Pierre Watcho, Hermine Meli Watio, Modeste Wankeu-Nya, Esther Ngadjui, Patrick Deeh Defo, Pepin Alango Nkeng-Efouet, Telesphore Benoit Nguelefack, Albert Kamanyi
BACKGROUND: Androgen deficiency is a clinical syndrome resulting from the inability of the testes to produce physiological levels of testosterone due to a disturbance occurring at one or more levels of the hypothalamic-pituitary-testicular axis. The present study was undertaken to evaluate the androgenic properties of aqueous and methanolic extracts of Ficus asperifolia on normal and castrated immature rats. METHODS: Normal rats were treated either per os with aqueous or methanolic extract of Ficus asperifolia (100 mg/kg or 500 mg/kg b...
January 13, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28063195/first-line-non-cytotoxic-therapy-in-chemotherapy-naive-patients-with-metastatic-castration-resistant-prostate-cancer-a-systematic-review-of-ten-randomised-clinical-trials
#3
REVIEW
Michiel H F Poorthuis, Robin W M Vernooij, R Jeroen A van Moorselaar, Theo M de Reijke
OBJECTIVE: To systematically evaluate all available treatment options in chemotherapy-naive patients with metastatic castration-resistant prostate cancer (mCRPC). METHODS: We systematically searched PubMed, EMBASE, and the Cochrane libraries up to March 1, 2016 for peer-reviewed publications on randomised clinical trials (RCTs). RCTs were included if progression-free survival (PFS), overall survival (OS), quality of life (QoL), or adverse events (AEs) were quantitatively evaluated...
January 6, 2017: BJU International
https://www.readbyqxmd.com/read/28034074/does-enzalutamide-really-reduce-the-risk-of-progression-compared-with-bicalutamide-in-patients-with-castration-resistant-prostate-cancer
#4
Mehmet Ali Nahit Şendur, Bülent Yalçın
No abstract text is available yet for this article.
January 2017: Journal of Clinical Oncology: Official Journal of the American Society of Clinical Oncology
https://www.readbyqxmd.com/read/28034067/enzalutamide-versus-bicalutamide-in-castration-resistant-prostate-cancer-the-strive-trial-there-is-no-significant-reduction-in-death-yet
#5
Jorg Michels
No abstract text is available yet for this article.
January 2017: Journal of Clinical Oncology: Official Journal of the American Society of Clinical Oncology
https://www.readbyqxmd.com/read/28011482/galectin-3-is-implicated-in-tumor-progression-and-resistance-to-anti-androgen-drug-through-regulation-of-androgen-receptor-signaling-in-prostate-cancer
#6
Tsogt-Ochir Dondoo, Tomoharu Fukumori, Kei Daizumoto, Tomoya Fukawa, Miho Kohzuki, Minoru Kowada, Yoshito Kusuhara, Hidehisa Mori, Hiroyoshi Nakatsuji, Masayuki Takahashi, Hiro-Omi Kanayama
BACKGROUND: Castration-resistant prostate cancer (CRPC)-related deaths are increasing worldwide. Therefore, clarification of the mechanisms of hormone-related tumor progression and resistance to anti-androgen drugs is useful in order to develop strategies for appropriate treatment of CRPC. Galectin-3 has been shown to be correlated with tumor progression in a variety of cancer types through the regulation of tumor proliferation, angiogenesis, and apoptosis. MATERIALS AND METHODS: We examined tumor cell invasion and migration using the xCELLigence system...
January 2017: Anticancer Research
https://www.readbyqxmd.com/read/27994514/the-correlation-between-parp1-and-brca1-in-ar-positive-triple-negative-breast-cancer
#7
Jiayan Luo, Juan Jin, Fang Yang, Zijia Sun, Wenwen Zhang, Yaqin Shi, Jing Xu, Xiaoxiang Guan
Triple-negative breast cancer (TNBC) lacks estrogen receptor (ER), progesterone receptor (PR) and human epidermal growth factor receptor 2 (HER-2) expression and thus cannot benefit from conventional hormonal or anti-HER2 targeted therapies. Anti-androgen therapy has shown a certain effect on androgen receptor (AR) positive TNBC. The emerging researches have proved that poly (ADP-ribose) polymerase (PARP) inhibitor is effective in BRCA1-deficient breast cancers. We demonstrated that combination of AR antagonist (bicalutamide) and PARP inhibitor (ABT-888) could inhibit cell viability and induce cell apoptosis significantly whatever in vitro or in vivo setting in AR-positive TNBC...
2016: International Journal of Biological Sciences
https://www.readbyqxmd.com/read/27987794/bioflavonoid-hesperetin-overcome-bicalutamide-induced-toxicity-by-co-delivery-in-novel-snedds-formulations-optimization-in-vivo-evaluation-and-uptake-mechanism
#8
Abhishek Arya, Hafsa Ahmad, Sachin Tulsankar, Satish Agrawal, Naresh Mittapelly, Rajkumar Boda, Rabi S Bhatta, Kalyan Mitra, Anil K Dwivedi
In the present study, we designed Bicalutamide (BCT) and Hesperetin (HSP) co-loaded self nano-emulsifying drug delivery system (SNEDDS) to encounter the problem of BCT induced toxicity, low solubility, and bioavailability. Optimized BCT-HSP SNEDDS would produce an emulsion of globule size 30.84±1.24nm with a high encapsulation efficiency of BCT (91.29%) and HSP (88.19%), and showed rapid drug release. DPPH assay confirmed the retention of antioxidant potential of HSP in SNEDDS. DCFH-DA confirmed intense green fluorescence in HSP treated groups due to the generation of reactive oxygen species...
February 1, 2017: Materials Science & Engineering. C, Materials for Biological Applications
https://www.readbyqxmd.com/read/27979508/re-efficacy-and-safety-of-enzalutamide-versus-bicalutamide-for-patients-with-metastatic-prostate-cancer-terrain-a-randomised-double-blind-phase-2-study
#9
https://www.readbyqxmd.com/read/27943566/impact-of-androgen-deprivation-therapy-on-volume-reduction-and-lower-urinary-tract-symptoms-in-patients-with-prostate-cancer
#10
Satoshi Washino, Masaru Hirai, Kimitoshi Saito, Yutaka Kobayashi, Yoshiaki Arai, Tomoaki Miyagawa
OBJECTIVE: To evaluate the impact of androgen deprivation therapy (ADT) on prostate volume, lower urinary tract symptoms (LUTS), and LUTS-related quality of life (QOL) in patients with prostate cancer. METHODS: Patients with prostate cancer (PCa) were treated with goserelin and bicalutamide for 24 weeks. Changes in the total prostate volume (TPV), International Prostate Symptom Score (IPSS), and QOL score for urinary symptoms were assessed every 12 weeks. Of the 42 patients enrolled, 8 patients withdrew and 2 were excluded, so 32 patients were analyzed...
December 12, 2016: Lower Urinary Tract Symptoms
https://www.readbyqxmd.com/read/27942507/impact-of-enzalutamide-on-patient-related-outcomes-in-metastatic-castration-resistant-prostate-cancer-current-perspectives
#11
REVIEW
Jia Luo, Julie N Graff
Prostate cancer claims the lives of more than 25,000 men in the United States yearly, most from metastatic disease. In the past decade, several new medications have been approved for the treatment of metastatic prostate cancer including the antiandrogen enzalutamide. In addition, there has been mounting interest in evaluating health-related quality of life (QoL) in patients with cancer including new more detailed recommendations released by the Prostate Cancer Working Group 3 on how to evaluate patient-related outcomes in clinical trials...
2016: Research and Reports in Urology
https://www.readbyqxmd.com/read/27919966/multimodal-primary-treatment-of-metastatic-prostate-cancer-with-androgen-deprivation-and-radiation
#12
Timo Joensuu, Greetta Joensuu, Kalevi Kairemo, Timo Kiljunen, Maigo Riener, Aili Aaltonen, Martti Ala-Opas, Aki Kangasmäki, Tuomo Alanko, Lauri Taipale, Petteri Hervonen, Anna Bützow, Irene Virgolini, Akseli Hemminki
AIM: We combined anti-androgen therapy with radiotherapy in a first-line setting for metastatic prostate cancer aiming to cause maximal cancer-cell death to delay the emergence of castration-resistant disease. MATERIALS AND METHODS: In this non-randomized retrospective series of 46 patients, the initial median prostate-specific antigen (PSA) was 98.5 μg/l (range=6.7-15,500), median Gleason score 9 and most men had at least T3N1M1 disease. All patients received luteinizing hormone releasing hormone analog or degarelix with bicalutamide...
2016: Anticancer Research
https://www.readbyqxmd.com/read/27870564/risk-associated-with-high-dose-bicalutamide
#13
Charles G Drake
No abstract text is available yet for this article.
November 21, 2016: Journal of Clinical Oncology: Official Journal of the American Society of Clinical Oncology
https://www.readbyqxmd.com/read/27848066/molecular-mechanism-of-r-bicalutamide-switching-from-androgen-receptor-antagonist-to-agonist-induced-by-amino-acid-mutations-using-molecular-dynamics-simulations-and-free-energy-calculation
#14
Hongli Liu, Rui Han, Jiazhong Li, Huanxiang Liu, Lifang Zheng
R-bicalutamide, a first generation antiandrogen, was used to treat prostate cancer for decades. Although it is very effective at the beginning, resistance appears after 2-3 years of treatment. Mutation of androgen receptor (AR) is considered a main reason for drug resistance. It is reported that AR W741C, W741L, W741C_T877A, T877A, F876L, F876L_T877A and L701H mutations can convert R-bicalutamide from AR antagonist to agonist, but the switching mechanisms are not clear. In this study, molecular dynamics simulations and molecular mechanics generalized Born surface area (MM-GBSA) calculations were performed to analyze the interaction mechanisms between R-bicalutamide and wild type/mutant ARs...
December 2016: Journal of Computer-aided Molecular Design
https://www.readbyqxmd.com/read/27771244/a-study-of-combination-bicalutamide-and-raloxifene-for-patients-with-castration-resistant-prostate-cancer
#15
Thai H Ho, Rafael Nunez-Nateras, Yue-Xian Hou, Alan H Bryce, Donald W Northfelt, Amylou C Dueck, Bryan Wong, Melissa L Stanton, Richard W Joseph, Erik P Castle
BACKGROUND: Prostate tissue expresses 2 estrogen receptor (ER) isoforms, ER-α and ER-β, and estrogen-based therapies have shown activity in preclinical studies. Raloxifene, a selective ER modulator, has inhibited the growth of prostate cancer xenograft models and was tested in a phase II trial of castration-resistant prostate cancer (CRPC), with some patients achieving stable disease. However, no studies have examined the safety of the combination of bicalutamide plus raloxifene for CRPC...
September 8, 2016: Clinical Genitourinary Cancer
https://www.readbyqxmd.com/read/27756786/a-phase-ii-randomized-open-label-study-of-neoadjuvant-degarelix-versus-lhrh-agonist-in-prostate-cancer-patients-prior-to-radical-prostatectomy
#16
Rashid Sayyid, Andrew Evans, Karen Hersey, Ranjena Maloni, Antonio Hurtado-Coll, Girish Kulkarni, Antonio Finelli, Alexandre R Zlotta, Robert Hamilton, Martin Gleave, Neil Fleshner
PURPOSE: Degarelix, a new GnRH receptor antagonist with demonstrated efficacy as first-line treatment in the management of high-risk prostate cancer, possesses some theoretical advantages over LHRH analogues in terms of avoiding "testosterone flare" and lower FSH levels. We set out to determine if pre-operative degarelix influenced surrogates of disease control in a randomized phase II study. EXPERIMENTAL DESIGN: 39 patients were randomly assigned to one of 3 different neo-adjuvant arms: degarelix only, degarelix/bicalutmaide, or LHRH agonist/bicalutamide...
October 18, 2016: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/27749325/androgen-receptor-and-beyond-targeting-androgen-signaling-in-castration-resistant-prostate-cancer
#17
Zachery R Reichert, Maha Hussain
The development of metastatic castration-resistant prostate cancer (mCRPC) signals the terminal disease phase. The preceding hormone-dependent disease setting is effectively managed with androgen deprivation therapy. This foundation of treatment has a high rate of biochemical and clinical response and meaningful clinical benefit but is finite in duration as most cancers will progress to castration resistance. Historically, treatment for mCRPC entailed androgen receptor (AR) inhibitors (nilutamide, flutamide, bicalutamide), nonspecific steroidal biosynthesis inhibitors (ketoconazole, itraconazole), steroids (prednisone, diethylstilbesterol, dexamethasone), or palliative chemotherapy (mitoxantrone, estramustine), but none of these strategies impacted survival...
September 2016: Cancer Journal
https://www.readbyqxmd.com/read/27726308/selective-androgen-receptor-modulators-comparative-excretion-study-of-bicalutamide-in-bovine-urine-and-faeces
#18
Dante Rojas, Gaud Dervilly-Pinel, Nora Cesbron, Mylène Penot, Alexandre Sydor, Stéphanie Prévost, Bruno Le Bizec
Besides their development for therapeutic purposes, non-steroidal selective androgen receptor modulators (non-steroidal SARMs) are also known to impact growth-associated pathways as ligands of androgenic receptors (AR). They present a potential for abuse in sports and food-producing animals as an interesting alternative to anabolic androgenic steroids (AAS). These compounds are easily available and could therefore be (mis)used in livestock production as growth promoters. To prevent such practices, dedicated analytical strategies should be developed for specific and sensitive detection of these compounds in biological matrices...
October 11, 2016: Drug Testing and Analysis
https://www.readbyqxmd.com/read/27699828/high-content-screening-identifies-src-family-kinases-as-potential-regulators-of-ar-v7-expression-and-androgen-independent-cell-growth
#19
Adam T Szafran, Cliff Stephan, Michael Bolt, Maureen G Mancini, Marco Marcelli, Michael A Mancini
BACKGROUND: AR-V7 is an androgen receptor (AR) splice variant that lacks the ligand-binding domain and is isolated from prostate cancer cell lines. Increased expression of AR-V7 is associated with the transition from hormone-sensitive prostate cancer to more advanced castration-resistant prostate cancer (CRPC). Due to the loss of the ligand-binding domain, AR-V7 is not responsive to traditional AR-targeted therapies, and the mechanisms that regulate AR-V7 are still incompletely understood...
January 2017: Prostate
https://www.readbyqxmd.com/read/27697998/targeting-hypoxic-prostate-tumours-using-the-novel-hypoxia-activated-prodrug-oct1002-inhibits-expression-of-genes-associated-with-malignant-progression
#20
Heather Nesbitt, Niall Maurice Byrne, Nicole Williams, Louise Ming, Jenny Worthington, Rachel J Errington, Laurence H Patterson, Paul Smith, Stephanie R McKeown, Declan J McKenna
Purpose To understand the role of hypoxia in prostate tumor progression, and to evaluate the ability of the novel unidirectional hypoxia-activated prodrug OCT1002 to enhance the anti-tumor effect of bicalutamide. Experimental Design The effect of OCT1002 on prostate cancer cells (LNCaP, 22Rv1, PC3) was measured in normoxia and hypoxia in vitro. In vivo, tumor growth and lung metastases were measured in mice treated with bicalutamide, OCT1002, or a combination. Dorsal skin fold chambers were used to image tumor vasculature in vivo...
October 3, 2016: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
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