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https://www.readbyqxmd.com/read/29667815/theranostic-pt-iv-conjugate-with-target-selectivity-for-androgen-receptor
#1
Xiaodong Qin, Lei Fang, Jian Zhao, Shaohua Gou
It is difficult to diagnose and treat castration-resistant prostate cancer (CRPC) which occurs due to the overexpression of androgen receptor (AR). Because there is a high level of AR in CRPC, we designed and prepared three Pt(IV)-based prodrugs targeting AR. Among them, compound 3, a three-in-one hybrid (an AR binding ligand, a cisplatin unit, and a coumarin moiety), was found to display satisfactory AR binding affinity and antagonist activity against androgen receptor, which could also be effectively internalized and visualized in LNCaP (AR+) cells...
April 18, 2018: Inorganic Chemistry
https://www.readbyqxmd.com/read/29666838/a-brief-history-of-intracrine-androgen-metabolism-by-castration-recurrent-prostate-cancer
#2
REVIEW
James L Mohler
This mini-review describes the evolution of the concept of intracrine androgen metabolism by prostate cancer during androgen deprivation therapy. Persistence of androgen receptor protein in the face of castrate circulating levels of testosterone could not be explained fully by hypersensitization or mutation of the androgen receptor. The hypothesis that castration-recurrent prostate cancer produced its own testosterone was proven using radioimmunoassay and mass spectrometry methods adopted for use in prostate tissue...
2018: American Journal of Clinical and Experimental Urology
https://www.readbyqxmd.com/read/29666834/androgen-action-in-prostate-function-and-disease
#3
REVIEW
Partha P Banerjee, Subhadra Banerjee, Terry R Brown, Barry R Zirkin
Benign prostatic hyperplasia (BPH) is an enlargement of the prostate gland that is frequently found in aging men. Androgens are essential for the development and differentiated function of the prostate, as well as for proliferation and survival of prostatic cells. In man, dog and rodent, there are age-related decreases in serum testosterone. Despite the lower serum testosterone levels, benign prostatic hyperplasia increases with age in men and dogs, while age-dependent prostatic hyperplasia develops in the dorsal and lateral lobes of the rat prostate...
2018: American Journal of Clinical and Experimental Urology
https://www.readbyqxmd.com/read/29666833/resolving-the-coffey-paradox-what-does-the-androgen-receptor-do-in-normal-vs-malignant-prostate-epithelial-cells
#4
REVIEW
John T Isaacs
Donald Straley Coffey completed his 85 year life's journey on November 9, 2017. In his wake, he left a legion of inspired and loyal students, fellows, and faculty colleagues from all over the world to carry on his passion both for life in general and his 50 year quest to conquer cancer. Early in his career, Dr. Coffey developed a series of animal models to study how androgen regulates the growth of both normal and abnormal prostatic epithelium. As part of these early studies, Dr. Coffey uncovered a paradox in that anti-androgen treatment given at the "wrong" time paradoxically enhanced, not inhibited, normal prostate growth...
2018: American Journal of Clinical and Experimental Urology
https://www.readbyqxmd.com/read/29666783/development-of-neuroendocrine-prostate-cancers-by-the-ser-arg-repetitive-matrix-4-mediated-rna-splicing-network
#5
Ahn R Lee, Nicole Che, Jessica M Lovnicki, Xuesen Dong
While the use of next-generation androgen receptor pathway inhibition (ARPI) therapy has significantly increased the survival of patients with metastatic prostate adenocarcinoma (AdPC), several groups have reported a treatment-resistant mechanism, whereby cancer cells can become androgen receptor (AR) indifferent and gain a neuroendocrine (NE)-like phenotype. This subtype of castration-resistant prostate cancer has been termed "treatment-induced castration-resistant neuroendocrine prostate cancer" (CRPC-NE)...
2018: Frontiers in Oncology
https://www.readbyqxmd.com/read/29666640/investigating-the-interactive-effects-of-sex-steroid-hormones-and-brain-derived-neurotrophic-factor-during-adolescence-on-hippocampal-nmda-receptor-expression
#6
Cushla R McCarthny, Xin Du, YeeWen Candace Wu, Rachel A Hill
Sex steroid hormones have neuroprotective properties which may be mediated by brain-derived neurotrophic factor (BDNF). This study sought to determine the interactive effects of preadolescent hormone manipulation and BDNF heterozygosity (+/- ) on hippocampal NMDA-R expression. Wild-type and BDNF+/- mice were gonadectomised, and females received either 17 β -estradiol or progesterone treatment, while males received either testosterone or dihydrotestosterone (DHT) treatment. Dorsal (DHP) and ventral hippocampus (VHP) were dissected, and protein expression of GluN1, GluN2A, GluN2B, and PSD-95 was assessed by Western blot analysis...
2018: International Journal of Endocrinology
https://www.readbyqxmd.com/read/29666302/targeting-galectin-1-impairs-castration-resistant-prostate-cancer-progression-and-invasion
#7
Tsung-Chieh Shih, Ruiwu Liu, Chun-Te Wu, Xiaocen Li, Wenwu Xiao, Xiaojun Deng, Zsofia Kiss, Ting Wang, Xiaojia Chen, Randy P Carney, Hsing-Jien Kung, Yong Duan, Paramita M Ghosh, Kit S Lam
PURPOSE: The majority of prostate cancer (PCa) patients who are treated with androgen deprivation therapy (ADT) will eventually develop fatal metastatic castration-resistant prostate cancer (mCRPC). Currently, there are no effective durable therapies for patients with mCRPC. High expression of Galectin-1 (Gal-1) is associated with PCa progression and poor clinical outcome. The role of Gal-1 in tumor progression are largely unknown. Here we characterized Gal-1 functions and evaluated the therapeutic effects of a newly developed Gal-1inhibitor, LLS30, in mCRPC...
April 17, 2018: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/29663669/preliminary-efficacy-and-tolerability-of-chemohormonal-therapy-in-metastatic-hormone-na%C3%A3-ve-prostate-cancer-the-first-real-life-experience-in-asia
#8
Darren M C Poon, Tim Chan, Kuen Chan, Michelle Chan, Eric K C Lee, Kitty Law, Daisy Lam
INTRODUCTION: A substantial survival benefit with chemohormonal therapy has been proven by the CHAARTED and STAMPEDE studies, and this clinical approach has emerged as the standard of care for patients with metastatic hormone-naïve prostate cancer (mHSPC). However, because its clinical efficacy and tolerability in Asian patients remains uncertain, this study aims to evaluate preliminary results of its use in Hong Kong. METHODS: The clinical records of mHSPC patients treated with chemohormonal therapy from all six public oncology centers in Hong Kong between January 2015 and July 2016 were reviewed...
April 16, 2018: Asia-Pacific Journal of Clinical Oncology
https://www.readbyqxmd.com/read/29663110/neutrophil-lymphocyte-and-platelet-counts-and-risk-of-prostate-cancer-outcomes-in-white-and-black-men-results-from-the-search-database
#9
Adriana C Vidal, Lauren E Howard, Amanda de Hoedt, Matthew R Cooperberg, Christopher J Kane, William J Aronson, Martha K Terris, Christopher L Amling, Emanuela Taioli, Jay H Fowke, Stephen J Freedland
PURPOSE: Systemic inflammation, as measured by C-reactive protein, has been linked with poor prostate cancer (PC) outcomes, predominantly in white men. Whether other immune measures like white blood cell counts are correlated with PC progression and whether results vary by race is unknown. We examined whether complete blood count (CBC) parameters were associated with PC outcomes and whether these associations varied by race. METHODS: Analyses include 1,826 radical prostatectomy patients from six VA hospitals followed through medical record review for biochemical recurrence (BCR)...
April 17, 2018: Cancer Causes & Control: CCC
https://www.readbyqxmd.com/read/29662636/analysis-of-hematological-parameters-as-prognostic-markers-for-toxicity-and-survival-of-223-radium-treatment
#10
Asha Leisser, Marzieh Nejabat, Markus Hartenbach, Reza Agha Mohammadi Sareshgi, Shahrokh Shariat, Gero Kramer, Michael Krainer, Marcus Hacker, Alexander R Haug
223 Radium (223 Ra) has emerged as treatment prolonging survival in patients with metastatic castration-resistant prostate cancer (CRPC). As 223 Ra can cause hematotoxicity (HT), pre-existing hematopoiesis might influence the efficacy of 223 Ra and the rate of hematotoxicity, but as to our knowledge such data has not been published yet, we retrospectively conducted an analysis on patients receiving 223 Ra. 54 patients treated with 223 Ra had a median survival of 67 weeks, which was significantly reduced in patients with pre-existing Hb toxicity (Tox) grade 2 (48 weeks P = 0...
March 23, 2018: Oncotarget
https://www.readbyqxmd.com/read/29662635/establishment-and-characterization-of-two-cabazitaxel-resistant-prostate-cancer-cell-lines
#11
Kazuaki Machioka, Kouji Izumi, Yoshifumi Kadono, Hiroaki Iwamoto, Renato Naito, Tomoyuki Makino, Suguru Kadomoto, Ariunbold Natsagdorj, Evan T Keller, Jian Zhang, Atsushi Mizokami
Once castration-resistant prostate cancer (CRPC) become resistant for cabazitaxel treatment, the patients are obliged to best supportive care. Therefore, the elucidation of the mechanism of the cabazitaxel-resistance and the conquest are important themes to improve the prognosis of the patients. Then we tried to establish cabazitaxel-resistant CRPC cell lines and characterized them. We established two cabazitaxel-resistant cell lines, PC-3-TxR/CxR and DU145-TxR/CxR from PC-3-TxR and DU145-TxR cell lines previously we established...
March 23, 2018: Oncotarget
https://www.readbyqxmd.com/read/29661653/radium-223-in-the-treatment-of-bone-metastasis-in-patients-with-castration-resistant-prostate-cancer-review-and-procedure
#12
J Orcajo-Rincon, A P Caresia-Aróztegui, M Del Puig Cózar-Santiago, J R García-Garzón, M de Arcocha-Torres, R C Delgado-Bolton, M J García-Velloso, S Alvarez-Ruiz, A M García-Vicente
Bone metastatic disease is the main cause of morbidity / mortality in patients with prostate cancer, presenting frequently as bone pain, pathological fractures or spinal cord compression, which requires early and timely therapy. Although, for the moment, the therapeutic window for its use has not been definitively established, radium-223 (223 Ra), an alpha particle emitter, has proved to be an effective therapeutic tool, pre or post-chemotherapy, in patients with castration-resistant prostate cancer with symptomatic bone metastases and absence of visceral metastases, significantly modifying the prognosis of the disease...
April 13, 2018: Revista Española de Medicina Nuclear e Imagen Molecular
https://www.readbyqxmd.com/read/29660779/clinical-findings-and-diagnostic-procedures-in-270-small-ruminants-with-obstructive-urolithiasis
#13
Anna-Katharina Riedi, Gabriela Knubben-Schweizer, Mireille Meylan
BACKGROUND: Details of the clinical signs of obstructive urolithiasis in male small ruminants have not been documented in a large population. OBJECTIVE: To describe the clinical presentation and diagnostic procedures in a large group of small ruminants with urolithiasis. ANIMALS: Two hundred and seventy small ruminants (158 sheep and 112 goats). METHODS: Retrospective study of 270 cases identified based on clinical records...
April 16, 2018: Journal of Veterinary Internal Medicine
https://www.readbyqxmd.com/read/29660154/local-mepivacaine-before-castration-of-horses-under-medetomidine-isoflurane-balanced-anaesthesia-is-effective-to-reduce-perioperative-nociception-and-cytokine-release
#14
M Abass, S Picek, J F Glaus Carzòn, C Kühnle, A Zaghlou, R Bettschart-Wolfensberger
BACKGROUND: In horses castration with primary intention healing is usually performed under balanced inhalation anaesthesia. To optimise analgesia, the use of local anaesthesia was tested. OBJECTIVES: To investigate the effect of local mepivacaine before castration with first intention healing under balanced medetomidine-isoflurane anaesthesia and flunixin meglumine, morphine analgesia on perioperative cytokine levels and pain in horses. STUDY DESIGN: Prospective blinded clinical study...
April 16, 2018: Equine Veterinary Journal
https://www.readbyqxmd.com/read/29658587/androgen-receptor%C3%A2-mediated-upregulation-of-quaking-affects-androgen-receptor%C3%A2-related-prostate-cancer-development-and-anti%C3%A2-androgen-receptor-therapy
#15
Keke Zhang, Fei Yan, Xiaoying Lei, Di Wei, Huanyu Lu, Zheng Zhu, An Xiang, Zichen Ye, Li Wang, Wanxiang Zheng, Xi'an Li, Jiarui Yuan, Zifan Lu, Jianlin Yuan
The androgen receptor (AR) has a crucial role in prostate cancer. RNA‑binding protein‑mediated post‑transcriptional regulation is important in the initiation and development of cancer. The present study attempted to elucidate the mutual association of AR and RNA‑binding protein quaking (QKI) in the development of prostate cancer. Dual‑luciferase reporter demonstrated that AR can positively regulate the expression of QKI in prostate cancer cell lines due to its effective transcription regulating function...
April 13, 2018: Molecular Medicine Reports
https://www.readbyqxmd.com/read/29658567/hepacam-inhibits-the-malignant-behavior-of-castration-resistant-prostate-cancer-cells-by-downregulating-notch-signaling-and-pf-3084014-a-%C3%AE-secretase-inhibitor-partly-reverses-the-resistance-of-refractory-prostate-cancer-to-docetaxel-and-enzalutamide-in-vitro
#16
Zhongbo Du, Luo Li, Wei Sun, Xiao Wang, Yao Zhang, Zhixiong Chen, Mengjuan Yuan, Zhen Quan, Nanjing Liu, Yanni Hao, Ting Li, Jinhua Wang, Chunli Luo, Xiaohou Wu
Castration-resistant prostate cancer (CRPC) continues to be a major challenge in the treatment of prostate cancer (PCa). The expression of hepatocyte cell adhesion molecule (HepaCAM), a novel tumor suppressor, is frequently downregulated or lost in PCa. Overactivated Notch signaling is involved in the development and progression of PCa, including CRPC. In this study, we found that the activities of Notch signaling were elevated, while HepaCAM expression was decreased in CRPC tissues compared with matched primary prostate cancer (PPC) tissues...
April 12, 2018: International Journal of Oncology
https://www.readbyqxmd.com/read/29656854/radical-prostatectomy-in-metastatic-castration-resistant-prostate-cancer-feasibility-safety-and-quality-of-life-outcomes
#17
Chad A Reichard, Justin R Gregg, Mary F Achim, Ana M Aparicio, Curtis A Pettaway, Louis L Pisters, John F Ward, John W Davis, Brian F Chapin
Ongoing prospective studies are evaluating treatment of the primary tumor in men with de novo metastatic prostate cancer (PCa). One potential benefit is prevention of morbidity from local progression. Thus, local therapy may be best applied selectively to men with local progression once resistance to first-line therapies has occurred. Here, we gather support for the hypothesis that radical prostatectomy (RP) is safe and preserves quality of life (QOL) when applied in men with metastatic castration-resistant PCa (mCRPC)...
April 12, 2018: European Urology
https://www.readbyqxmd.com/read/29656769/population-control-in-small-animals
#18
REVIEW
Margaret V Root Kustritz
Optimal age for ovariohysterectomy or castration has not been defined in the scientific literature. Bitches and queens are significantly less likely to develop mammary neoplasia, which has a high incidence and potentially high morbidity and mortality, if spayed when young. Tom cats exhibit undesirable behaviors that preclude them being good pets and should be castrated young. There is no compelling reason to castrate male dogs when young unless it is needed to control reproductive behaviors or prevent indiscriminate breeding...
April 12, 2018: Veterinary Clinics of North America. Small Animal Practice
https://www.readbyqxmd.com/read/29651807/editorial-comment-to-influence-of-prior-oral-ethinylestradiol-use-on-the-efficacy-of-enzalutamide-for-the-treatment-of-castration-resistant-prostate-cancer-in-men
#19
Kouji Izumi
No abstract text is available yet for this article.
April 12, 2018: International Journal of Urology: Official Journal of the Japanese Urological Association
https://www.readbyqxmd.com/read/29651569/external-radiation-exposure-excretion-and-effective-half-life-in-177-lu-psma-targeted-therapies
#20
J Kurth, B J Krause, S M Schwarzenböck, L Stegger, M Schäfers, K Rahbar
BACKGROUND: Prostate-specific membrane antigen (PSMA)-targeted therapy with 177 Lu-PSMA-617 is a therapeutic option for patients with metastatic castration-resistant prostate cancer (mCRPC). To optimize the therapy procedure, it is necessary to determine relevant parameters to define radiation protection and safety necessities. Therefore, this study aimed at estimating the ambient radiation exposure received by the patient. Moreover, the excreted activity was quantified. RESULTS: In total, 50 patients with mCRPC and treated with 177 Lu-PSMA-617 (mean administered activity 6...
April 12, 2018: EJNMMI Research
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