Abstract
The article is principally intended to describe the recent evolutions in the field of research concerned with the metabolic actions of thyroid hormones and those of some of their metabolites or derivatives. Mitochondria, as a result of their functions, represent the principal objecti...
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PMID: 20625286
PDF is available here.
Abstract
To evaluate the efficacy, tolerability, and pharmacokinetics of bicalutamide plus anastrozole in young males with testotoxicosis.
This was a multicenter, open-label, single-arm, 12-month, Phase II pilot trial in 14 males (2-9 years) with testotoxicosis treated with bicalutamide (12.5, 25, 50, or 100...
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PMID: 21158211
PDF is available here.
Abstract
Signaling between androgen receptor (AR) and mTOR may be crucial for prostate cancer cells to endure the low androgen and suboptimal nutrient conditions produced by androgen deprivation therapy.
AR and mTOR cross-talk was examined in LNCaP cells exposed to either high or low testosterone. AR and mTO...
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PMID: 21036700
PDF is available here.
Abstract
We evaluated and compared the efficacy and toxicities of maximal androgen blockade (MAB) versus castration alone in Chinese patients with advanced prostate cancer. From 1996 to 2004, 608 patients with advanced prostate cancer were included in the study. Patients were retrospectively divided into two...
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PMID: 20694018
PDF is available here.
Abstract
We hypothesthized that nifedipine activates PPARgamma, inhibits vascular remodeling, and improves vascular function in hypertension.
Stroke-prone spontaneously hypertensive rats (SHRSP) were treated with vehicle, nifedipine, and PPARgamma selective antagonist GW9662 with nifedipine.
Systolic blood p...
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PMID: 20460829
PDF is available here.
Abstract
Prostate cancer remains a leading cause of cancer death in American men. Androgen deprivation therapy (ADT) is the most common treatment for advanced prostate cancer patients; however, ADT fails in nearly all cases resulting in castration resistant or androgen-insensitive (AI) disease. In many cases...
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PMID: 20589722
PDF is available here.
Abstract
Administration of telmisartan, losartan, GW9662 and these AT1 receptor blockers with GW9662 had no significant effect on blood pressure. KK-Ay mice exhibited a significant increase in the ischemic area compared with C57BL6 mice. Treatment with telmisartan decreased the ischemic area and improved the...
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PMID: 20498620
PDF is available here.
Abstract
We show that virulent M. tuberculosis and its cell wall mannose-capped lipoarabinomannan induce PPARgamma expression through a macrophage mannose receptor-dependent pathway. When activated, PPARgamma promotes IL-8 and cyclooxygenase 2 expression, a process modulated by a PPARgamma agonist or antagon...
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PMID: 20554962
PDF is available here.
Abstract
We report our use of androgen blockade (AB) to suppress nocturnal erections as an alternative treatment for HFP.
A retrospective review of all patients treated at our institution for HFP was undertaken. Included in this study were any patients treated with single- or combination-agen...
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PMID: 20456623
PDF is available here.
Abstract
We report our use of androgen blockade (AB) to suppress nocturnal erections as an alternative treatment for HFP.
A retrospective review of all patients treated at our institution for HFP was undertaken. Included in this study were any patients treated with single- or combination-agen...
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PMID: 20456623
PDF is available here.
Shuang S Liu,
Yanfeng Y Qi,
Yubin Y Ge,
Tamika T Duplessis,
Brian G BG Rowan,
Clement C Ip,
Helen H Cheng,
Paul S PS Rennie,
Izumi I Horikawa,
Arthur J AJ Lustig,
Qun Q Yu,
Haitao H Zhang and
Yan Y Dong
Abstract
We found that the combination of MSA and bicalutamide produced a robust downregulation of prostate-specific antigen and a recently identified AR target, telomerase, and its catalytic subunit, human telomerase reverse transcriptase. The downregulation of hTERT occurs mainly at the transcriptional lev...
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PMID: 20571066
PDF is available here.
Abstract
We selectively measured the Ca(2+) permeability of the apical membrane of fura-2-loaded IMCD-3 cells using the Mn(2+) quench technique. Mn(2+) influx across the apical membrane was increased 12- to 16-fold by apical ATP and was blocked by the pyrazole derivative BTP2, a known inhibitor of TRPC3 chan...
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PMID: 20410214
PDF is available here.
Abstract
Solvent-free reaction conditions facilitate a range of aromatic C-H functionalisations that traditionally require acidic or disfavoured solvents. These reactions include selective ortho- and meta-arylation of aryl carbamates and anilides and selective halogenation reactions.
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PMID: 20424748
PDF is available here.
Abstract
We investigated the roles of brain-derived neurotrophic factor (BDNF) and nerve growth factor (NGF) in the dysregulation of transcription factors and histone modifying enzymes induced by 3-NP in primary cortical neurons. BDNF prevented the 3-NP-induced decrease in cAMP response-element binding prote...
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PMID: 19779956
PDF is available here.
Takeshi Yuasa,
Shinya Maita,
Norihiko Tsuchiya,
Zhiyong Ma,
Shintaro Narita,
Yohei Horikawa,
Shinya Yamamoto,
Junji Yonese,
Iwao Fukui,
Shunji Takahashi,
Kiyohiko Hatake and
Tomonori Habuchi
Abstract
Our cross-sectional study confirmed that both ADT-treated and hormone-naive Japanese patients with prostate cancer have low rates of osteoporosis. These findings are different from those of studies in western countries. Genetic and hormonal or other environmental factors may result in population dif...
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PMID: 20163839
PDF is available here.
Abstract
We report that N(2),N(6)-bis(4-nitrophenyl)pyridine-2,6-dicarboxamide, which is related to known isophthalic acid dianilides, transports Cl(-) ions through phospholipid bilayer membranes and shows clear evidence of channel activity.
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PMID: 20369200
PDF is available here.
Abstract
CHI's 17th International Tri-Conference on Molecular Medicine, held in San Francisco, included topics covering new developments in the field of medicinal chemistry. This conference report highlights selected presentations on fragment-based drug discovery, quantum mechanical energy decomposition for...
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PMID: 20373245
PDF is available here.
Abstract
Carbonyl ylide cycloaddition strategy was employed in the synthesis of platensimycin analogs. 7-Phenylplatensimycin and 11-methyl-7-phenylplatensimycin are more potent analogs of platensimycin.
2010 Elsevier Ltd. All rights reserved.
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PMID: 20207542
PDF is available here.
Abstract
Bicalutamide (Casodex) reportedly improves high-risk prostate cancer survival as an adjuvant treatment following radiotherapy. However, biological data for the interaction between bicalutamide and ionizing radiation in concomitant association are lacking.
To explore t...
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PMID: 19902473
PDF is available here.
Abstract
Bicalutamide (Casodex) reportedly improves high-risk prostate cancer survival as an adjuvant treatment following radiotherapy. However, biological data for the interaction between bicalutamide and ionizing radiation in concomitant association are lacking.
To explore t...
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PMID: 19902473
PDF is available here.
Abstract
Bicalutamide (Casodex) reportedly improves high-risk prostate cancer survival as an adjuvant treatment following radiotherapy. However, biological data for the interaction between bicalutamide and ionizing radiation in concomitant association are lacking.
To explore t...
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PMID: 19902473
PDF is available here.
Abstract
Bicalutamide (Casodex) reportedly improves high-risk prostate cancer survival as an adjuvant treatment following radiotherapy. However, biological data for the interaction between bicalutamide and ionizing radiation in concomitant association are lacking.
To explore t...
|
PMID: 19902473
PDF is available here.
Abstract
Bicalutamide (Casodex) reportedly improves high-risk prostate cancer survival as an adjuvant treatment following radiotherapy. However, biological data for the interaction between bicalutamide and ionizing radiation in concomitant association are lacking.
To explore t...
|
PMID: 19902473
PDF is available here.
Abstract
Bicalutamide (Casodex) reportedly improves high-risk prostate cancer survival as an adjuvant treatment following radiotherapy. However, biological data for the interaction between bicalutamide and ionizing radiation in concomitant association are lacking.
To explore t...
|
PMID: 19902473
PDF is available here.
Abstract
Bicalutamide (Casodex) reportedly improves high-risk prostate cancer survival as an adjuvant treatment following radiotherapy. However, biological data for the interaction between bicalutamide and ionizing radiation in concomitant association are lacking.
To explore t...
|
PMID: 19902473
PDF is available here.
Abstract
Bicalutamide (Casodex) reportedly improves high-risk prostate cancer survival as an adjuvant treatment following radiotherapy. However, biological data for the interaction between bicalutamide and ionizing radiation in concomitant association are lacking.
To explore t...
|
PMID: 19902473
PDF is available here.
Abstract
Bicalutamide (Casodex) reportedly improves high-risk prostate cancer survival as an adjuvant treatment following radiotherapy. However, biological data for the interaction between bicalutamide and ionizing radiation in concomitant association are lacking.
To explore t...
|
PMID: 19902473
PDF is available here.
Abstract
Bicalutamide (Casodex) reportedly improves high-risk prostate cancer survival as an adjuvant treatment following radiotherapy. However, biological data for the interaction between bicalutamide and ionizing radiation in concomitant association are lacking.
To explore t...
|
PMID: 19902473
PDF is available here.
Abstract
Bicalutamide (Casodex) reportedly improves high-risk prostate cancer survival as an adjuvant treatment following radiotherapy. However, biological data for the interaction between bicalutamide and ionizing radiation in concomitant association are lacking.
To explore t...
|
PMID: 19902473
PDF is available here.
Abstract
Bicalutamide (Casodex) reportedly improves high-risk prostate cancer survival as an adjuvant treatment following radiotherapy. However, biological data for the interaction between bicalutamide and ionizing radiation in concomitant association are lacking.
To explore t...
|
PMID: 19902473
PDF is available here.
Abstract
Bicalutamide (Casodex) reportedly improves high-risk prostate cancer survival as an adjuvant treatment following radiotherapy. However, biological data for the interaction between bicalutamide and ionizing radiation in concomitant association are lacking.
To explore t...
|
PMID: 19902473
PDF is available here.
Abstract
Bicalutamide (Casodex) reportedly improves high-risk prostate cancer survival as an adjuvant treatment following radiotherapy. However, biological data for the interaction between bicalutamide and ionizing radiation in concomitant association are lacking.
To explore t...
|
PMID: 19902473
PDF is available here.
Abstract
Bicalutamide (Casodex) reportedly improves high-risk prostate cancer survival as an adjuvant treatment following radiotherapy. However, biological data for the interaction between bicalutamide and ionizing radiation in concomitant association are lacking.
To explore t...
|
PMID: 19902473
PDF is available here.
Abstract
Bicalutamide (Casodex) reportedly improves high-risk prostate cancer survival as an adjuvant treatment following radiotherapy. However, biological data for the interaction between bicalutamide and ionizing radiation in concomitant association are lacking.
To explore t...
|
PMID: 19902473
PDF is available here.
Abstract
Bicalutamide (Casodex) reportedly improves high-risk prostate cancer survival as an adjuvant treatment following radiotherapy. However, biological data for the interaction between bicalutamide and ionizing radiation in concomitant association are lacking.
To explore t...
|
PMID: 19902473
PDF is available here.
Abstract
Bicalutamide (Casodex) reportedly improves high-risk prostate cancer survival as an adjuvant treatment following radiotherapy. However, biological data for the interaction between bicalutamide and ionizing radiation in concomitant association are lacking.
To explore t...
|
PMID: 19902473
PDF is available here.
Abstract
Bicalutamide (Casodex) reportedly improves high-risk prostate cancer survival as an adjuvant treatment following radiotherapy. However, biological data for the interaction between bicalutamide and ionizing radiation in concomitant association are lacking.
To explore t...
|
PMID: 19902473
PDF is available here.
Abstract
Bicalutamide (Casodex) reportedly improves high-risk prostate cancer survival as an adjuvant treatment following radiotherapy. However, biological data for the interaction between bicalutamide and ionizing radiation in concomitant association are lacking.
To explore t...
|
PMID: 19902473
PDF is available here.
Abstract
We tested the hypothesis that relaxin signaling through RXFP1 would activate PPARgamma activity. In cells overexpressing RXFP1 (HEK-RXFP1), relaxin increased transcriptional activity through a PPAR response element (PPRE) in a concentration-dependent manner. In cells lacking RXFP1, relaxin had no ef...
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PMID: 19712722
PDF is available here.
Abstract
We report that the expression of COX-2 and glial fibrillary acidic protein were enhanced and that of peroxisome proliferator-activated receptor gamma (PPARgamma) was decreased in Abeta(25-35)-treated astrocytes. In line with these results, nuclear factor-kappaB translocation was increased in the pre...
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PMID: 20413894
PDF is available here.
Abstract
Platensimycin, an active metabolite of Streptomyces platensis, was initially discovered by a combination of RNA interferin induced gene-silencing and library screening to microbial extracts. Platensimycin selectively inhibits beta - ketoacyl-acyl carrier protein (ACP) synthase II (FabF) that is reco...
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PMID: 20158476
PDF is available here.
Abstract
Hedgehog signaling is activated in a variety of solid tumors and hematologic malignancies by point mutations in hedgehog pathway members or autocrine or paracrine ligand secretion. Several hedgehog inhibitors were developed to block hedgehog pathway activity on the level of the activating receptor,...
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PMID: 20072843
PDF is available here.
Abstract
We report that nesfatin-1 is also anti-hyperglycemic. It was found that the intravenous injection of nesfatin-1 significantly reduced blood glucose in hyperglycemic db/db mice. This anti-hyperglycemic effect of nesfatin-1 was time-, dose-, insulin-dependent and peripheral.
Copyright 2009 Elsevier In...
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PMID: 19995555
PDF is available here.
Abstract
We report a case of a 60-year-old white man who was admitted in our department with ecchymoses and haematuria secondary to a DIC associated with metastatic prostate cancer. A review of this clinical scenario is also reported....
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PMID: 20608143
PDF is available here.
Abstract
We report the use of anastrozole and bicalutamide in a 5 year-old boy with familial male-limited precocious puberty. Clinical response showed decreased advancement of skeletal maturation, secondary sexual characteristics and aggressiveness with no short-term side effects. The combination seems a bet...
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PMID: 20333877
PDF is available here.
Abstract
Platensimycin and platencin are inhibitors of FabF and FabF/H bacterial fatty acid synthesis enzymes, respectively. Discovery of natural congeners provides one of the ways to understand the relationship of chemical structure and biological function. Efforts to discover the natural analogs of platens...
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PMID: 19911028
PDF is available here.
Jia-Jun Liu,
Yun-Wei Guo,
Zhi-Gang Fang,
Xiao-Ning Si,
Xiang-Yuan Wu,
Pei-Qing Liu,
Dong-Jun Lin,
Ruo-Zhi Xiao,
Yan Xu,
Chun-Zhi Wang,
Xu-Dong Li,
Yi He and
Ren-Wei Huang
Abstract
We investigated the in vitro apoptosis inducing effects of peroxisome proliferator-activated receptor-gamma (PPAR-gamma) ligand ciglitazone (CGZ) on acute promyelocytic leukemia (APL) NB4 cells and its mechanisms of action. The results revealed that CGZ (10-50 micromol/l) inhibited the growth of leu...
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PMID: 19787196
PDF is available here.
Abstract
TARP will be the first study to evaluate the effects of dutasteride and an antiandrogen in patients failing GnRH analogue and help elucidate the potential role of a dual 5ARI in reducing the rate of progression in non-metastatic CRPC....
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PMID: 19796455
PDF is available here.
Abstract
Several studies have evaluated thiazolidinedione therapy as medical treatments for some central nervous system disorders, such as cognitive deficits associated with neurodegenerative disorders. However, there is limited data to support a direct role for peroxisome proliferator-activated receptor-γ...
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PMID: 19745723
PDF is available here.
Abstract
In adult Ascaris suum (roundworm) mitochondrial membrane-bound complex II acts as a rhodoquinol-fumarate reductase, which is the reverse reaction to that of mammalian complex II (succinate-ubiquinone reductase). The adult A. suum rhodoquinol-fumarate reductase was crystallized in the presence of oct...
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PMID: 19724139
PDF is available here.
Abstract
The aggressive reduction of LDL-cholesterol levels by treatment with statins is a key component of preventive cardiovascular care; however, additional therapies to prevent atherosclerosis and the associated clinical sequelae are still needed. Thyromimetic compounds selective for the liver or for the...
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PMID: 19705333
PDF is available here.
H Wong,
J Z Chen,
B Chou,
J S Halladay,
J R Kenny,
H La,
J C Marsters,
E Plise,
P J Rudewicz,
K Robarge,
Y Shin,
S Wong,
C Zhang and
S C Khojasteh
Abstract
GDC-0449 (2-chloro-N-(4-chloro-3-(pyridin-2-yl)phenyl)-4-(methylsulfonyl)benzamide) is a potent, selective Hedgehog (Hh) signalling pathway inhibitor being developed for the treatment of various cancers. The in vivo clearance of GDC-0449 was estimated to be 23.0, 4.65, 0.338, and 19.3 ml min(-1) kg(...
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PMID: 19845436
PDF is available here.
Abstract
We have developed a general method for directing-group-containing arene arylation by aryl iodides. Using palladium acetate as the catalyst, we arylated anilides, benzamides, benzoic acids, benzylamines, and 2-substituted pyridine derivatives under nearly identical conditions. We have also developed...
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PMID: 19552413
PDF is available here.
Abstract
A mild and cost-efficient chemo-enzymatic method for the synthesis of C-terminal arylamides of amino acid and peptides is described. Using the industrial serine protease Alcalase under near-anhydrous conditions, C-terminal arylamides of N-Cbz-protected amino acids and peptides could be obtained from...
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PMID: 19534522
PDF is available here.
Abstract
Clinical data and models of human disease indicate that androgen receptor (AR) activity is essential for prostate cancer development, growth, and progression. The dependence of prostatic adenocarcinoma on AR signaling at all stages of disease has thereby been exploited in the treatment of disseminat...
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PMID: 19638458
PDF is available here.
Abstract
We have recently shown that transcriptional, translational and post-translational processes contribute to the selective loss of beta1C integrin during prostate malignant transformation. Here, we investigated whether androgen deprivation therapy (ADT) may affect beta1C mRNA expression in prostate can...
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PMID: 19578773
PDF is available here.
Abstract
Our results show that androgenic -regulation of SOCS-3 leads to inhibition of prolif-eration and secretion in human prostate cancer....
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PMID: 19634073
PDF is available here.