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https://www.readbyqxmd.com/read/29164633/capillarisin-blocks-prostate-specific-antigen-expression-on-activation-of-androgen-receptor-in-prostate-carcinoma-cells
#1
Ke-Hung Tsui, Ying-Ling Chang, Tsui-Hsia Feng, Chen-Pang Hou, Yu-Hsiang Lin, Pei-Shan Yang, Bing-Wei Lee, Horng-Heng Juang
BACKGROUND: Capillarisin (Cap), an active ingredient of Artemisia capillaris extracts, has known for its anti-inflammatory, antioxidant, and anticancer properties. Functions of Cap in prostate cancer are not clear. We investigate effects of Cap on downregulation of prostate specific antigen (PSA) via modulation of androgen receptor (AR) in prostate carcinoma cells. METHODS: Cell proliferation was measured by water-soluble tetrazolium-1 (WST-1) cell proliferation assays...
November 22, 2017: Prostate
https://www.readbyqxmd.com/read/29163687/stromal-regulation-of-prostate-cancer-cell-growth-by-mevalonate-pathway-enzymes-hmgcs1-and-hmgcr
#2
Shingo Ashida, Chiaki Kawada, Keiji Inoue
It has been suggested that the tumor microenvironment plays an important role in tumor progression, acquisition of androgen independence, and distant metastasis in prostate cancer (PC). However, little is known about the transcriptional basis of cellular interactions in the human PC microenvironment. To clarify the mechanism of PC progression and metastasis, we investigated the interaction of PC, epithelial, and stromal cells using genome-wide gene expression profiling. We hypothesized that PC cells could induce stromal cells to differentiate into so-called cancer-associated fibroblasts (CAFs), which might contribute to cancer invasion and metastasis...
December 2017: Oncology Letters
https://www.readbyqxmd.com/read/29163372/hyperglycemia-promotes-tmprss2-erg-gene-fusion-in-prostate-cancer-cells-via-upregulating-insulin-like-growth-factor-binding-protein-2
#3
Jeff M P Holly, Jessica Broadhurst, Rehanna Mansor, Amit Bahl, Claire M Perks
Background: Epidemiologic evidence shows that obesity is associated with a greater risk of aggressive prostate cancer (PCa) and PCa-specific mortality and this is observed mainly in men with the TMPRSS2-ERG gene fusion. Obesity is often associated with comorbid conditions such as type 2 diabetes and hyperglycemia: we investigated whether some of the exposures associated with disturbed metabolism can also affect the frequency of this gene fusion. Methods: Fusion was induced in LNCaP PCa cells in normal or high levels of glucose, with or without insulin-like growth factor binding protein-2 (IGFBP-2) silenced or the presence of insulin-like growth factor-1 (IGF-I), insulin, or epidermal growth factor (EGF)...
2017: Frontiers in Endocrinology
https://www.readbyqxmd.com/read/29158832/clinical-translation-and-first-in-human-use-of-44-sc-sc-psma-617-for-pet-imaging-of-metastasized-castrate-resistant-prostate-cancer
#4
Elisabeth Eppard, Ana de la Fuente, Martina Benešová, Ambreen Khawar, Ralph A Bundschuh, Florian C Gärtner, Barbara Kreppel, Klaus Kopka, Markus Essler, Frank Rösch
BACKGROUND: Various trivalent radiometals are well suited for labeling of DOTA-conjugated variants of Glu-ureido-based prostate-specific membrane antigen (PSMA) inhibitors. The DOTA-conjugate PSMA-617 has proven high potential in PSMA radioligand therapy (PSMA-RLT) of prostate cancer as well as PET imaging when labeled with lutetium-177 and gallium-68 respectively. Considering the relatively short physical half-life of gallium-68 this positron emitter precludes prolonged acquisition periods, as required for pre-therapeutic dosimetry or intraoperative applications...
2017: Theranostics
https://www.readbyqxmd.com/read/29156689/implications-of-pi3k-akt-inhibition-on-rest-protein-stability-and-neuroendocrine-phenotype-acquisition-in-prostate-cancer-cells
#5
Ruiqui Chen, Yinan Li, Ralph Buttyan, Xuesen Dong
Treatment-induced neuroendocrine prostate cancer (t-NEPC) is an aggressive subtype of prostate cancer (PCa) that arises as a consequence of rigorous androgen receptor (AR) pathway inhibition (ARPI) therapies. While the PI3K/AKT pathway has been investigated as a co-therapeutic target with ARPI for advanced PCa, whether this strategy can prevent tumor progression to t-NEPC remains unknown. Here, we report that PI3K/AKT inhibition alone reduces RE-1 silencing transcription factor (REST) protein expression and induces multiple NE markers in PCa cells...
October 17, 2017: Oncotarget
https://www.readbyqxmd.com/read/29153549/anticancer-activities-of-emetine-prodrugs-that-are-proteolytically-activated-by-the-prostate-specific-antigen-psa-and-evaluation-of-in-vivo-toxicity-of-emetine-derivatives
#6
Emmanuel S Akinboye, Marc D Rosen, Oladapo Bakare, Samuel R Denmeade
Emetine is a small molecule protein synthesis inhibitor that is toxic to all cell types and therefore suitable for complete killing of all types of heterogeneous cancer cells within a tumor. It becomes significantly inactive (non-toxic) when derivatized at its N-2' secondary amine. This provides a strategy for targeting emetine to cancerous tumor without killing normal cells. In this report, PSA activatable peptide prodrugs of emetine were synthesized. To overcome steric hindrances and enhance protease specific cleavage, a 2-stage prodrug activation process was needed to release emetine in cancer cells...
November 10, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29151363/functional-assessment-of-human-enhancer-activities-using-whole-genome-starr-sequencing
#7
Yuwen Liu, Shan Yu, Vineet K Dhiman, Tonya Brunetti, Heather Eckart, Kevin P White
BACKGROUND: Genome-wide quantification of enhancer activity in the human genome has proven to be a challenging problem. Recent efforts have led to the development of powerful tools for enhancer quantification. However, because of genome size and complexity, these tools have yet to be applied to the whole human genome. RESULTS:  In the current study, we use a human prostate cancer cell line, LNCaP as a model to perform whole human genome STARR-seq (WHG-STARR-seq) to reliably obtain an assessment of enhancer activity...
November 20, 2017: Genome Biology
https://www.readbyqxmd.com/read/29150732/dimethylarginine-dimethylaminohydrolase-1-ddah1-is-frequently-upregulated-in-prostate-cancer-and-its-overexpression-conveys-tumor-growth-and-angiogenesis-by-metabolizing-asymmetric-dimethylarginine-adma
#8
Karthik Reddy Kami Reddy, Chandrashekhar Dasari, Divya Duscharla, Bhukya Supriya, N Sai Ram, M V Surekha, Jerald Mahesh Kumar, Ramesh Ummanni
Tissue microarray analysis confirmed higher dimethylarginine dimethylaminohydrolase-1 (DDAH1) expression in prostate cancer (PCa) compared to benign and normal prostate tissues. DDAH1 regulates nitric oxide (NO) production by degrading endogenous nitric oxide synthase (NOS) inhibitor, asymmetric dimethylarginine (ADMA). This study examined whether DDAH1 has any physiological role in PCa progression. Using overexpression of DDAH1 in PCa (PC3 and LNCaP) cell lines, we found that DDAH1 promotes cell proliferation, migration and invasion by lowering ADMA levels, as well as increasing NO production...
November 17, 2017: Angiogenesis
https://www.readbyqxmd.com/read/29136407/phospholipase-d-inhibitors-reduce-human-prostate-cancer-cell-proliferation-and-colony-formation
#9
Amanda R Noble, Norman J Maitland, Daniel M Berney, Martin G Rumsby
BACKGROUND: Phospholipases D1 and D2 (PLD1/2) hydrolyse cell membrane glycerophospholipids to generate phosphatidic acid, a signalling lipid, which regulates cell growth and cancer progression through effects on mTOR and PKB/Akt. PLD expression and/or activity is raised in breast, colorectal, gastric, kidney and thyroid carcinomas but its role in prostate cancer (PCa), the major cancer of men in the western world, is unclear. METHODS: PLD1 protein expression in cultured PNT2C2, PNT1A, P4E6, LNCaP, PC3, PC3M, VCaP, 22RV1 cell lines and patient-derived PCa cells was analysed by western blotting...
November 14, 2017: British Journal of Cancer
https://www.readbyqxmd.com/read/29136406/the-interaction-between-androgen-receptor-and-semenogelin-i-a-synthetic-lxxll-peptide-antagonist-inhibits-the-growth-of-prostate-cancer-cells
#10
Peng Li, Jinbo Chen, Eiji Kashiwagi, Taichi Mizushima, Bin Han, Satoshi Inoue, Hiroki Ide, Koji Izumi, Hiroshi Miyamoto
BACKGROUND: We previously demonstrated that a seminal plasma protein, semenogelin I (SgI), functioned as an androgen receptor (AR) coactivator. Meanwhile, several short sequence motifs in AR coregulators, such as LxxLL (L=leucine), have been shown to mediate specific interactions with AR. METHODS: We investigated the role of the LxxLL motif within SgI in the interactions with AR and cell growth in prostate cancer lines in vitro. RESULTS: A full-length SgI with mutations in the motif (i...
November 14, 2017: British Journal of Cancer
https://www.readbyqxmd.com/read/29134684/enhanced-radiosensitization-of-enzalutamide-via-schedule-dependent-administration-to-androgen-sensitive-prostate-cancer-cells
#11
Maryam Ghashghaei, Miltiadis Paliouras, Mitra Heravi, Hamed Bekerat, Mark Trifiro, Tamim M Niazi, Thierry Muanza
BACKGROUND: Prostate cancer (PCa) is a progressive disease and the most diagnosed cancer in men. The current standard of care for high-risk localized PCa is a combination of androgen deprivation therapy (ADT) and radiation (XRT). The majority of these patients however become resistant due to incomplete responses to ADT as a result of selective cells maintaining androgen receptor (AR) activity. Improvement can be made if increasing radiosensitivity is realized. Therefore, the aim of this study is to investigate the efficacy of the next-generation PCa drug Enzalutamide (ENZA), as a radiosensitizer in XRT therapy...
November 14, 2017: Prostate
https://www.readbyqxmd.com/read/29121805/prostate-cancer-xenograft-inhibitory-activity-and-pharmacokinetics-of-decursinol-a-metabolite-of-angelica-gigas-pyranocoumarins-in-mouse-models
#12
Wei Wu, Su-Ni Tang, Yong Zhang, Manohar Puppala, Timothy K Cooper, Chengguo Xing, Cheng Jiang, Junxuan Lü
We have previously shown that the ethanol extract of dried Angelica gigas Nakai (AGN) root exerts anticancer activity against androgen receptor (AR)-negative human DU145 and PC-3 prostate cancer xenografts and primary carcinogenesis in the transgenic adenocarcinoma of mouse prostate (TRAMP) model. The major pyranocoumarin isomers decursin (D) and decursinol angelate (DA), when provided at equi-molar intake to that provided by AGN extract, accounted for the inhibitory efficacy against precancerous epithelial lesions in TRAMP mice...
November 9, 2017: American Journal of Chinese Medicine
https://www.readbyqxmd.com/read/29117897/exploring-the-tetrahydroisoquinoline-thiohydantoin-scaffold-blockade-the-androgen-receptor-as-potent-anti-prostate-cancer-agents
#13
Xi Xu, Raoling Ge, Lei Li, Jubo Wang, Xiaoyu Lu, Siqi Xue, Xijing Chen, Zhiyu Li, Jinlei Bian
Prostate cancer (PC) is a major cause of cancer-related male death in worldwide and the identification of new and improved potent anti-PC molecules is constantly required. A novel scaffold of tetrahydroisoquinoline thiohydantoin was rationally designed based on the enzalutamide structures and our pre-work, leading to the discovery of a series of new antiproliferative compounds. Several new analogues displayed improved androgen receptor (AR) antagonistic activity, while maintaining the higher selective toxicity toward LNCaP cells (AR-rich) versus DU145 cells (AR-deficient) compared to enzalutamide...
October 14, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29115533/effects-of-leptin-on-leptin-receptor-isoform-expression-and-proliferative-activity-in-human-normal-prostate-and-prostate-cancer-cell-lines
#14
Marta Szyszka, Marianna Tyczewska, Paulina Milecka, Karol Jopek, Piotr Celichowski, Ludwik K Malendowicz, Marcin Rucinski
Results of studies on the expression of leptin and its receptors in the human prostate gland and human prostate cell lines are contradictory. Regarding this, we carefully reinvestigated this issue using human normal prostate (PrEC, PrSC, PrSMC) and prostate cancer (DU145, LNCaP, PC3) cell lines. Expression of leptin receptor isoforms was assessed by qPCR while the effects of leptin on cell proliferative activity was determined by real-time cell analyzer (RTCA). Expression of the leptin receptor variant 1 was not detected in LNCaP and PrSMC cell lines, but it was found in the remaining cell lines...
November 1, 2017: Oncology Reports
https://www.readbyqxmd.com/read/29115463/ganoderma-lucidum-polysaccharide-inhibits-prostate-cancer-cell-migration-via-the-protein-arginine-methyltransferase-6-signaling-pathway
#15
Xiaohui Zhao, Dayu Zhou, Yunen Liu, Chun Li, Xiaoguang Zhao, Ying Li, Wei Li
Prostate cancer is one of the most common types of malignant tumor of men worldwide and the incidence and mortality rate is gradually increasing. At present, the molecular mechanisms of growth and migration in human prostate cancer have not been completely elucidated. Studies have demonstrated that Ganoderma lucidum polysaccharides (GLP) can inhibit cancer. Therefore the present study investigated the effect and molecular mechanism of GLP on cell growth and migration of LNCaP human prostate cancer cells. LNCaP cells were transfected with either a protein arginine methyltransferase 6 (PRMT6) overexpression plasmid or PRMT6 small interfering (si)RNA...
October 26, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/29111484/self-calibrated-fluorescent-probe-resembled-as-an-indicator-of-the-lysosomal-phosphatase-pertaining-to-the-cancer-cells
#16
Arup Podder, Susan M Alex, Mrinmoy Maiti, Kaustabh Kumar Maiti, Sankarprasad Bhuniya
A self-calibrated fluorescent probe Lyso-Phos has synthesized followed by a straightforward synthetic pathway. Lyso-Phos acts as an indicator for lysosomal phosphatase. Its photophysical property including cellular imaging was described. Lyso-Phos showed ratiometric UV-Vis- absorption changes from λabs 370nm to λabs 450nm in the presence of alkaline phosphatase (ALP). On the other hand, fluorescence intensity λem 560nm of Lyso-Phos has increased around 45-fold in the presence of ALP. The probe Lyso-Phos was found to be highly chemoselective toward the phosphatase compared with other ubiquitous entities in cellular milieu...
October 18, 2017: Journal of Photochemistry and Photobiology. B, Biology
https://www.readbyqxmd.com/read/29110315/nad-p-h-quinone-oxidoreductase-1-silencing-aggravates-hormone-induced-prostatic-hyperplasia-in-mice
#17
H-T Kim, Y-J Kim, S-R Park, S-Y Ryu, J-Y Jung
NAD(P)H-quinone oxidoreductase 1 (NQO1) is a highly inducible flavoprotein known to involve in various cellular defence mechanisms. In this study, we explored whether NQO1 deletion affects hormone-induced prostatic hyperplasia. Testosterone propionate (3 mg/kg, IP) was injected into wild-type (WT) and NOQ1 knockout C57BL/6 mice (NQO1(-/-) ) for 14 consecutive days, and the samples were collected for biological and histochemical studies. The testosterone-treated NQO1(-/-) showed about 140% higher prostate weight than the testosterone-treated WT, with enhanced connective tissue and hyperplastic glands formations...
November 6, 2017: Andrologia
https://www.readbyqxmd.com/read/29109383/synthesis-and-antitumor-activity-of-novel-arylpiperazine-derivatives-containing-the-saccharin-moiety
#18
Hong Chen, Bing-Bing Xu, Tao Sun, Zhan Zhou, Hui-Yuan Ya, Mu Yuan
Prostate cancer is a major public health problem worldwide. For the development of potential anti-prostate cancer agents, a series of novel arylpiperazine derivatives containing the saccharin moiety based on previous studies was designed, synthesized, and evaluated in prostate (PC-3, LNCaP, and DU145) cancer cell lines for their anticancer activities. The majority of the compounds exhibited excellent selective activity for the tested cancer cells. Compounds 4 and 12 exhibited strong cytotoxic activities against DU145 cells (half maximal inhibitory concentration (IC50) < 2 μM)...
October 29, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29105806/the-orally-active-pterocarpanquinone-lqb-118-exhibits-cytotoxicity-in-prostate-cancer-cell-and-tumor-models-through-cellular-redox-stress
#19
Thiago Martino, Tarana A Kudrolli, Binod Kumar, Isis Salviano, André Mencalha, Marsen Garcia P Coelho, Graça Justo, Paulo R Ribeiro Costa, Kátia C Carvalho Sabino, Shawn E Lupold
BACKGROUND: The targeted induction of reactive oxygen species (ROS) is a developing mechanism for cancer therapy. LQB-118 is a pterocarpanquinone and ROS-inducing agent with proven antineoplastic activity. Here, LQB-118 efficacy and mechanism of activity, were examined in Prostate Cancer (PCa) cell and tumor models. METHODS: PC3, LNCaP, and LAPC4 PCa cells were applied. Dicoumarol treatment was used to inhibit quinone reductase activity. N-acetylcysteine (NAC) was applied as a ROS scavenger...
November 6, 2017: Prostate
https://www.readbyqxmd.com/read/29100388/sirtuin-7-a-new-marker-of-aggressiveness-in-prostate-cancer
#20
Romain Haider, Fabienne Massa, Lisa Kaminski, Stephan Clavel, Zied Djabari, Guillaume Robert, Kathiane Laurent, Jean-François Michiels, Matthieu Durand, Jean-Ehrland Ricci, Jean-François Tanti, Frédéric Bost, Damien Ambrosetti
Predictive biomarkers for advanced prostate cancer (PCa) are still missing. The sirtuin 7 (SIRT7) has been linked to tumorogenesis but its role in prostate cancer is poorly documented. To determine if SIRT7 can be a biomarker for aggressive prostate cancer and plays a role in PCa aggressiveness. We analyzed the expression of SIRT7 by immunohistochemistry in 57 patients comparing healthy with adjacent cancer tissue. SIRT7 levels were significantly elevated in tumors and its expression was positively associated with the grade...
September 29, 2017: Oncotarget
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