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Bicalutamide

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https://www.readbyqxmd.com/read/28981251/development-of-5n-bicalutamide-a-high-affinity-reversible-covalent-antiandrogen
#1
Felipe de Jesus Cortez, Phuong Nguyen, Charles Truillet, Boxue Tian, Kristopher M Kuchenbecker, Michael J Evans, Paul Webb, Matthew P Jacobson, Robert J Fletterick, Pamela M England
Resistance to clinical antiandrogens has plagued the evolution of effective therapeutics for advanced prostate cancer. As with the first-line therapeutic bicalutamide (Casodex), resistance to newer antiandrogens (enzalutamide, ARN-509) develops quickly in patients, despite the fact that these drugs have ~10-fold better affinity for androgen receptor than bicalutamide. Improving affinity alone is often not sufficient to prevent resistance and alternative strategies are needed to improve antiandrogen efficacy...
October 5, 2017: ACS Chemical Biology
https://www.readbyqxmd.com/read/28971491/plumbagin-improves-the-efficacy-of-androgen-deprivation-therapy-in-prostate-cancer-a-pre-clinical-study
#2
Parisa Abedinpour, Véronique T Baron, Adrian Chrastina, Gaelle Rondeau, Jennifer Pelayo, John Welsh, Per Borgström
BACKGROUND: Plumbagin is a candidate drug for the treatment of prostate cancer. Previous observations indicated that it may improve the efficacy of androgen deprivation therapy (ADT). This study evaluates the effectiveness of treatment with combinations of plumbagin and alternative strategies for ADT in mouse models of prostate cancer to support its clinical use. METHODS: Plumbagin was administered per oral in a new sesame oil formulation. Standard toxicology studies were performed in rats...
October 2, 2017: Prostate
https://www.readbyqxmd.com/read/28943399/testosterone-bicalutamide-antagonism-at-the-predicted-extracellular-androgen-binding-site-of-zip9
#3
Ahmed Bulldan, Viveka Nand Malviya, Neha Upmanyu, Lutz Konrad, Georgios Scheiner-Bobis
ZIP9 is a Zn(2+) transporter, testosterone receptor, and mediator of signaling events through G-proteins. Despite these pivotal properties, however, its physiological and pathophysiological significance has not yet been comprehensively addressed. Using a cell line that lacks the classical androgen receptor we show that ZIP9-mediated phosphorylation of Erk1/2, CREB, or ATF-1 and expression of claudin-5 and zonula occludens-1 by testosterone can be completely antagonized by bicalutamide (Casodex), an anti-androgen of significant clinical impact...
September 21, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28875700/one-pot-synthesis-of-%C3%AE-hydroxysulfones-and-its-application-in-the-preparation-of-anticancer-drug-bicalutamide
#4
Yajun Wang, Wei Jiang, Congde Huo
An efficient one-pot multistep strategy has been developed, comprising auto-oxidative difunctionalization of alkenes, oxidation of sulfides, and a further reduction of peroxides for the synthesis of complex β-hydroxysulfone derivatives from phenthiols and alkenes. This method has several advantageous characteristics, including readily available substrates, low-cost and environmental benign reagents, nontoxic and renewable solvents, and mild reaction conditions. The application of this transformation to the multigram-scale preparation of the anticancer drug bicalutamide is accomplished...
September 14, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28851578/moving-towards-precision-urologic-oncology-targeting-enzalutamide-resistant-prostate-cancer-and-mutated-forms-of-the-androgen-receptor-using-the-novel-inhibitor-darolutamide-odm-201
#5
Hendrik Borgmann, Nada Lallous, Deniz Ozistanbullu, Eliana Beraldi, Naman Paul, Kush Dalal, Ladan Fazli, Axel Haferkamp, Pascale Lejeune, Artem Cherkasov, Martin E Gleave
Darolutamide (ODM-201) is a novel androgen receptor (AR) antagonist with a chemical structure distinctly different from currently approved AR antagonists that targets both wild-type and mutated ligand binding domain variants to inhibit AR nuclear translocation. Here, we evaluate the activity of darolutamide in enzalutamide-resistant castration resistant prostate cancer (CRPC) as well as in AR mutants detected in patients after treatment with enzalutamide, abiraterone, or bicalutamide. Darolutamide significantly inhibited cell growth and AR transcriptional activity in enzalutamide-resistant MR49F cells in vitro, and led to decreased tumor volume and serum prostate-specific antigen levels in vivo, prolonging survival in mice bearing enzalutamide-resistant MR49F xenografts...
August 26, 2017: European Urology
https://www.readbyqxmd.com/read/28840192/androgen-receptor-as-a-mediator-and-biomarker-of-radioresistance-in-triple-negative-breast-cancer
#6
Corey Speers, Shuang G Zhao, Ben Chandler, Meilan Liu, Kari Wilder-Romans, Eric Olsen, Shyam Nyati, Cassandra Ritter, Prasanna G Alluri, Vishal Kothari, Daniel F Hayes, Theodore S Lawrence, Daniel E Spratt, Daniel R Wahl, Lori J Pierce, Felix Y Feng
Increased rates of locoregional recurrence have been observed in triple-negative breast cancer despite chemotherapy and radiation therapy. Thus, approaches that combine therapies for radiosensitization in triple-negative breast cancer are critically needed. We characterized the radiation therapy response of 21 breast cancer cell lines and paired this radiation response data with high-throughput drug screen data to identify androgen receptor as a top target for radiosensitization. Our radiosensitizer screen nominated bicalutamide as the drug most effective in treating radiation therapy-resistant breast cancer cell lines...
2017: NPJ Breast Cancer
https://www.readbyqxmd.com/read/28835168/structure-activity-relationship-analysis-of-carbobicyclo-and-oxabicyclo-succinimide-analogues-as-potential-androgen-receptor-antagonists
#7
Lingyan Wang, Jiazhong Li
Prostate cancer (PCa) is a frequently diagnosed male cancer and the second leading cause of cancer-related death in many countries. Due to various amino acid mutations occurred in the ligand binding domain of androgen receptor (AR), the patients were observed insensitive, even resistant to the marketed antiandrogens such as bicalutamide and enzalutamide, which emphasizes the urgent need for novel antiandrogens to solve drug resistance problem. Recently a series of carbobicyclo and oxabicyclo succinimide analogues were reported to effectively antagonize AR...
August 23, 2017: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/28827103/efficacy-and-safety-of-enzalutamide-vs-bicalutamide-in-younger-and-older-patients-with-metastatic-castration-resistant-prostate-cancer-in-the-terrain-trial
#8
D Robert Siemens, Laurence Klotz, Axel Heidenreich, Simon Chowdhury, Arnauld Villers, Benoit Baron, Steve van Os, Nahla Hasabou, Fong Wang, Ping Lin, Neal D Shore
PURPOSE: Enzalutamide significantly prolonged median progression-free survival vs bicalutamide in chemotherapy-naïve metastatic castration-resistant prostate cancer in TERRAIN. A post hoc analysis investigated the influence of age on efficacy and safety of enzalutamide vs bicalutamide in this population. MATERIALS AND METHODS: Patients were randomized 1:1 to enzalutamide 160 mg/day or bicalutamide 50 mg/day. Progression-free survival, time to prostate-specific antigen progression and safety were analyzed post hoc in younger (<75 years) and older (≥75 years) subgroups...
August 18, 2017: Journal of Urology
https://www.readbyqxmd.com/read/28816284/-predictive-factor-analysis-of-time-to-progression-of-castration-resistant-prostate-cancer-after-androgen-deprivation-therapy
#9
G J Ji, C Huang, G Song, X S Li, Y Song, L Q Zhou
OBJECTIVE: To explore risk factors including prostate-specific antigen (PSA) kinetics for the prediction of castration-resistant prostate cancer (CRPC), and to build a practical model for predicting the progression to CRPC after androgen deprivation therapy (ADT) so as to facilitate clinicians in decision-making for prostate cancer patients receiving ADT. METHODS: A total of 185 patients with prostate cancer who had received ADT as the primary therapy in Department of Urology of Peking University First Hospital from 2003 to 2014 were enrolled retrospectively...
August 18, 2017: Beijing da Xue Xue Bao. Yi Xue Ban, Journal of Peking University. Health Sciences
https://www.readbyqxmd.com/read/28757136/iminoenamine-based-novel-androgen-receptor-antagonist-exhibited-anti-prostate-cancer-activity-in-androgen-independent-prostate-cancer-cells-through-inhibition-of-akt-pathway
#10
S Divakar, K Saravanan, P Karthikeyan, R Elancheran, S Kabilan, K K Balasubramanian, Rajlakshmi Devi, J Kotoky, M Ramanathan
Treatment by androgen receptor (AR) antagonists is one of the regimens for prostate cancer. The prolonged treatment with AR antagonist leads to the expression of point mutation in the ligand binding domain of the AR. This point mutation causes resistance to AR antagonist by converting them into an agonist. The T887A mutated AR was frequently expressed in androgen independent prostate cancer (AIPC) patients. Through literature survey and molecular modelling, we have identified a novel AR antagonist having a bulky β-iminoenamine BF2 complex scaffold...
September 25, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28745319/the-androgen-receptor-is-a-negative-regulator-of-eif4e-phosphorylation-at-s209-implications-for-the-use-of-mtor-inhibitors-in-advanced-prostate-cancer
#11
L S D'Abronzo, S Bose, M E Crapuchettes, R E Beggs, R L Vinall, C G Tepper, S Siddiqui, M Mudryj, F U Melgoza, B P Durbin-Johnson, R W deVere White, P M Ghosh
The antiandrogen bicalutamide is widely used in the treatment of advanced prostate cancer (PCa) in many countries, but its effect on castration-resistant PCa (CRPC) is limited. We previously showed that resistance to bicalutamide results from activation of mechanistic target of rapamycin (mTOR). Interestingly, clinical trials testing combinations of the mTOR inhibitor RAD001 with bicalutamide were effective in bicalutamide-naïve CRPC patients, but not in bicalutamide-pretreated ones. Here we investigate causes for their difference in response...
July 24, 2017: Oncogene
https://www.readbyqxmd.com/read/28743076/lc-ms-ms-esi-method-for-simultaneous-quantification-of-darolutamide-and-its-active-metabolite-orm-15341-in-mice-plasma-and-its-application-to-a-pharmacokinetic-study
#12
Sreekanth Dittakavi, Pavan Kumar V S P Nagasuri, Suresh P Sulochana, Syed Mohd Saim, Sadanand R Mallurwar, Mohd Zainuddin, Purushottam Dewang, Sriram Rajagopal, Ramesh Mullangi
A sensitive and rapid LC-MS/MS method was developed and validated for the simultaneous quantitation of darolutamide and its active metabolite i.e. ORM-15341 in 50μL mice plasma using bicalutamide as an internal standard (I.S.) as per regulatory guidelines. Sample processing was accomplished through liquid-liquid extraction. Chromatographic separation was achieved using an Atlantis C18 column with an isocratic mobile phase comprising 0.2% formic acid:acetonitrile (35:65, v/v) at a flow rate of 0.8mL/min within 2...
October 25, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28734596/developments-in-urologic-oncology-%C3%A2-oncoforum%C3%A2-the-best-of-2016
#13
F Gómez-Veiga, A Alcaraz-Asensio, J Burgos-Revilla, J M Cózar-Olmo
OBJECTIVE: To put forth new findings of urologic oncology with impact on clinical practice presented during 2016 in the main annual meetings. ACQUISITION OF EVIDENCE: This document reviews abstracts on prostate, kidney and bladder cancer presented at the congresses of 2016 (EAU, AUA, ASCO, ESMO and ASTRO) and publications with the highest impact in this period valued with the highest scores by the OncoForum committee. SYNTHESIS OF EVIDENCE: In High-Risk Renal-Cell carcinoma after nephrectomy, disease-free survival was significantly greater for sunitinib than placebo group, with adverse events more frequents...
July 19, 2017: Actas Urologicas Españolas
https://www.readbyqxmd.com/read/28716370/a-systematic-review-and-framework-for-the-use-of-hormone-therapy-with-salvage-radiation-therapy-for-recurrent-prostate-cancer
#14
REVIEW
Daniel E Spratt, Robert T Dess, Zachary S Zumsteg, Daniel W Lin, Phuoc T Tran, Todd M Morgan, Emmanuel S Antonarakis, Paul L Nguyen, Charles J Ryan, Howard M Sandler, Matthew R Cooperberg, Edwin Posadas, Felix Y Feng
CONTEXT: Salvage radiotherapy (SRT) is a standard of care for men who recur postprostatectomy, and recent randomized trials have assessed the benefit and toxicity of adding hormone therapy (HT) to SRT with differing results. OBJECTIVE: To perform a systematic review of randomized phase III trials of the use of SRT ± HT and generate a framework for the use of HT with SRT. EVIDENCE ACQUISITION: Systematic literature searches were conducted on February 15, 2017 in three databases (MEDLINE [via PubMed], EMBASE, and ClinicalTrials...
July 14, 2017: European Urology
https://www.readbyqxmd.com/read/28704421/transcriptional-role-of-androgen-receptor-in-the-expression-of-long-non-coding-rna-sox2ot-in-neurogenesis
#15
Valentina Tosetti, Jenny Sassone, Anna L M Ferri, Michela Taiana, Gloria Bedini, Sara Nava, Greta Brenna, Chiara Di Resta, Davide Pareyson, Anna Maria Di Giulio, Stephana Carelli, Eugenio A Parati, Alfredo Gorio
The complex architecture of adult brain derives from tightly regulated migration and differentiation of precursor cells generated during embryonic neurogenesis. Changes at transcriptional level of genes that regulate migration and differentiation may lead to neurodevelopmental disorders. Androgen receptor (AR) is a transcription factor that is already expressed during early embryonic days. However, AR role in the regulation of gene expression at early embryonic stage is yet to be determinate. Long non-coding RNA (lncRNA) Sox2 overlapping transcript (Sox2OT) plays a crucial role in gene expression control during development but its transcriptional regulation is still to be clearly defined...
2017: PloS One
https://www.readbyqxmd.com/read/28698198/abcb1-mediates-cabazitaxel-docetaxel-cross-resistance-in-advanced-prostate-cancer
#16
Alan P Lombard, Chengfei Liu, Cameron M Armstrong, Vito Cucchiara, Xinwei Gu, Wei Lou, Christopher P Evans, Allen C Gao
Advancements in research have added several new therapies for castration-resistant prostate cancer (CRPC), greatly augmenting our ability to treat patients. However, CRPC remains an incurable disease due to the development of therapeutic resistance and the existence of cross-resistance between available therapies. Understanding the interplay between different treatments will lead to improved sequencing and the creation of combinations that overcome resistance and prolong survival. Whether there exists cross-resistance between docetaxel and the next-generation taxane cabazitaxel is poorly understood...
October 2017: Molecular Cancer Therapeutics
https://www.readbyqxmd.com/read/28672724/anticancer-drugs-in-portuguese-surface-waters-estimation-of-concentrations-and-identification-of-potentially-priority-drugs
#17
Mónica S F Santos, Helena Franquet-Griell, Silvia Lacorte, Luis M Madeira, Arminda Alves
Anticancer drugs, used in chemotherapy, have emerged as new water contaminants due to their increasing consumption trends and poor elimination efficiency in conventional water treatment processes. As a result, anticancer drugs have been reported in surface and even drinking waters, posing the environment and human health at risk. However, the occurrence and distribution of anticancer drugs depend on the area studied and the hydrological dynamics, which determine the risk towards the environment. The main objective of the present study was to evaluate the risk of anticancer drugs in Portugal...
October 2017: Chemosphere
https://www.readbyqxmd.com/read/28666849/the-indications-of-tautomeric-conversion-in-amorphous-bicalutamide-drug
#18
Marzena Rams-Baron, Patryk Wlodarczyk, Mateusz Dulski, Agnieszka Wlodarczyk, Danuta Kruk, Adam Rachocki, Renata Jachowicz, Marian Paluch
No abstract text is available yet for this article.
June 27, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28660504/distribution-of-six-anticancer-drugs-and-a-variety-of-other-pharmaceuticals-and-their-sorption-onto-sediments-in-an-urban-japanese-river
#19
Takashi Azuma, Natsumi Arima, Ai Tsukada, Satoru Hirami, Rie Matsuoka, Ryogo Moriwake, Hirotaka Ishiuchi, Tomomi Inoyama, Yusuke Teranishi, Misato Yamaoka, Mao Ishida, Kanae Hisamatsu, Ayami Yunoki, Yoshiki Mino
The distributions of 31 pharmaceuticals grouped into nine therapeutic classes, including six anticancer drugs, were investigated in the waters and sediments of an urban river in Japan. The coefficients of sorption (logK d) to the river sediments were also determined from the results of a field survey and laboratory-scale experiment. Three anticancer drugs-bicalutamide, doxifluridine, and tamoxifen-were detected in the river sediments at maximum concentrations of 391, 392, and 250 ng/kg, respectively. In addition, the transformation products of psychotropic carbamazepine (2-hydroxy carbamazepine, acridine, and acridone) were detected in the range of 108 ng/kg (2-hydroxy carbamazepine) to 2365 ng/kg (acridine), and the phytoestrogen glycitein was detected in the range of N...
June 28, 2017: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/28645652/androgen-inhibits-key-atherosclerotic-processes-by-directly-activating-adtrp-transcription
#20
Chunyan Luo, Elisabeth Pook, Bo Tang, Weiyi Zhang, Sisi Li, Kirsten Leineweber, Shing-Hu Cheung, Qiuyun Chen, Martin Bechem, Jing-Shan Hu, Volker Laux, Qing Kenneth Wang
Low androgen levels are associated with an increased risk of coronary artery disease (CAD), thrombosis and myocardial infarction (MI), suggesting that androgen has a protective role. However, little is known about the underlying molecular mechanism. Our genome-wide association study identified the ADTRP gene encoding the androgen-dependent TFPI regulating protein as a susceptibility gene for CAD and MI. The expression level of ADTRP was regulated by androgen, but the molecular mechanism is unknown. In this study, we identified the molecular mechanism by which androgen regulates ADTRP expression and tested the hypothesis that androgen plays a protective role in cardiovascular disease by activating ADTRP expression...
June 20, 2017: Biochimica et Biophysica Acta
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