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https://www.readbyqxmd.com/read/28624515/development-of-selective-androgen-receptor-modulators-sarms
#1
REVIEW
Ramesh Narayanan, Christopher C Coss, James T Dalton
The Androgen Receptor (AR), a member of the steroid hormone receptor family, plays important roles in the physiology and pathology of diverse tissues. AR ligands, which include circulating testosterone and locally synthesized dihydrotestosterone, bind to and activate the AR to elicit their effects. Ubiquitous expression of the AR, metabolism and cross reactivity with other receptors limit broad therapeutic utilization of steroidal androgens. However, the discovery of selective androgen receptor modulators (SARMs) and other tissue-selective nuclear hormone receptor modulators that activate their cognate receptors in a tissue-selective manner provides an opportunity to promote the beneficial effects of androgens and other hormones in target tissues with greatly reduced unwanted side-effects...
June 14, 2017: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/28619249/metabolism-of-sex-steroids-is-influenced-by-acquired-adiposity-a-study-of-young-adult-male-monozygotic-twin-pairs
#2
Veera Vihma, Jussi Naukkarinen, Ursula Turpeinen, Esa Hämäläinen, Jaakko Kaprio, Aila Rissanen, Sini Heinonen, Antti Hakkarainen, Jesper Lundbom, Nina Lundbom, Tomi S Mikkola, Matti J Tikkanen, Kirsi H Pietiläinen
Obesity and ageing are associated with lower serum testosterone levels in men. How fat distribution or adipose tissue metabolism, independent of genetic factors and age, are related to sex steroid metabolism is less clear. We studied the associations between adiposity and serum sex hormone concentrations, and mRNA expression of genes regulating sex hormone metabolism in adipose tissue in young adult male monozygotic (MZ) twin pairs. The subjects [n=18 pairs; mean age, 32 years; individual body mass indexes (BMIs) 22-36kg/m(2)] included 9 male MZ twin pairs discordant for BMI [intra-pair difference (Δ) in BMI ≥3kg/m(2)]...
June 12, 2017: Journal of Steroid Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/28611094/agonist-specific-protein-interactomes-of-glucocorticoid-and-androgen-receptor-as-revealed-by-proximity-mapping
#3
Joanna K Lempiäinen, Einari A Niskanen, Kaisa-Mari Vuoti, Riikka E Lampinen, Helka Göös, Markku Varjosalo, Jorma J Palvimo
Glucocorticoid receptor (GR) and androgen receptor (AR) are steroid-inducible transcription factors (TFs). GR and AR are central regulators of various metabolic, homeostatic and differentiation processes and hence important therapeutic targets, especially in inflammation and prostate cancer, respectively. Hormone binding to these steroid receptors (SRs) leads to DNA binding and activation or repression of their target genes with the aid of interacting proteins, coregulators. However, protein interactomes of these important drug targets have remained poorly defined...
June 13, 2017: Molecular & Cellular Proteomics: MCP
https://www.readbyqxmd.com/read/28610993/effects-of-a-co-micronized-composite-containing-palmitoylethanolamide-and-polydatin-in-an-experimental-model-of-benign-prostatic-hyperplasia
#4
Marika Cordaro, Daniela Impellizzeri, Rosalba Siracusa, Enrico Gugliandolo, Roberta Fusco, Antonino Inferrera, Emanuela Esposito, Rosanna Di Paola, Salvatore Cuzzocrea
Palmitoylethanolamide (PEA), a fatty acid amide-signaling molecule has well-known anti-inflammatory and neuroprotective effects. Nevertheless, PEA does not possess the ability to prevent free radicals formation. Polydatin (PLD), a biological precursor of resveratrol, has antioxidant activity. A combination of PEA and PLD could, conceivably, have beneficial effects on oxidative stress produced by inflammatory processes. In the present study we investigated the effects of a co-micronized composite containing PEA and PLD (m(PEA/PLD)) in a model of testosterone-induced benign hyperplasia (BPH)...
June 10, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28604137/effects-of-dihydrotestosterone-administration-on-the-expression-of-reproductive-and-body-weight-regulatory-factors-in-ovariectomized-and-estradiol-treated-female-rats
#5
Takeshi Iwasa, Toshiya Matsuzaki, Kiyohito Yano, Yiliyasi Mayila, Minoru Irahara
To clarify the direct effects of androgens, the changes in the hypothalamic levels of reproductive and appetite regulatory factors induced by chronic dihydrotestosterone (DHT) administration were evaluated in female rats. DHT treatment increased the BW and food intake of the ovariectomized rats, but not the estradiol (E2)-treated rats. DHT administration suppressed the expression of a hypothalamic anorexigenic factor. Although the kisspeptin (Kiss1) mRNA levels of the anterior hypothalamic block (the anteroventral periventricular nucleus, AVPV) were increased in the E2-treated rats, DHT administration did not affect the Kiss1 mRNA levels of the AVPV in the ovariectomized or E2-treated rats...
June 11, 2017: Gynecological Endocrinology
https://www.readbyqxmd.com/read/28596723/the-11s-proteasomal-activator-reg%C3%AE-impacts-polyglutamine-expanded-androgen-receptor-aggregation-and-motor-neuron-viability-through-distinct-mechanisms
#6
Jill M Yersak, Heather L Montie, Erica S Chevalier-Larsen, Yuhong Liu, Lan Huang, Martin Rechsteiner, Diane E Merry
Spinal and bulbar muscular atrophy (SBMA) is caused by expression of a polyglutamine (polyQ)-expanded androgen receptor (AR). The inefficient nuclear proteasomal degradation of the mutant AR results in the formation of nuclear inclusions containing amino-terminal fragments of the mutant AR. PA28γ (also referred to as REGγ) is a nuclear 11S-proteasomal activator with limited proteasome activation capabilities compared to its cytoplasmic 11S (PA28α, PA28β) counterparts. To clarify the role of REGγ in polyQ-expanded AR metabolism, we carried out genetic and biochemical studies in cell models of SBMA...
2017: Frontiers in Molecular Neuroscience
https://www.readbyqxmd.com/read/28595942/multicomponent-access-to-androstano-arylpyrimidines-under-microwave-conditions-and-evaluation-of-their-anti-cancer-activity-in-vitro
#7
Ádám Baji, Tamás Kiss, János Wölfling, Dávid Kovács, Nóra Igaz, Mohana Krishna Gopisetty, Mónika Kiricsi, Éva Frank
Novel ring D- and A-fused pyrimidines in the androstane series were efficiently synthesized within 10-15min in polar protic solvents under microwave irradiation via two kinds of multicomponent heterocyclization reactions followed by spontaneous or promoted oxidation. The rates of the one-pot catalyst-free transformations of steroidal β-ketoaldehydes, ammonium acetate and substituted benzaldehydes in EtOH were found to be affected slightly by the steric and electronic feature of the substituents on the aromatic ring of the arylaldehyde component and the different reactivities of rings D and A of the sterane core...
June 5, 2017: Journal of Steroid Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/28594074/testosterone-and-dihydrotestosterone-levels-in-the-transition-zone-correlate-with-prostate-volume
#8
Tomislav Pejčić, Tomislav Tosti, Živoslav Tešić, Borivoj Milković, Dejan Dragičević, Milutin Kozomara, Milica Čekerevac, Zoran Džamić
BACKGROUND: There is still no consensus regarding intraprostatic androgen levels and the accumulation of androgens in the hyperplastic prostatic tissue. The current opinion is that intraprostatic dihydrotestosterone (DHT) concentrations are maintained but not elevated in benign prostatic hyperplasia (BPH), while there is no similar data concerning intraprostatic testosterone (T). METHODS: Tissue T (tT) and tissue DHT (tDHT) concentration were determined in 93 patients scheduled for initial prostate biopsy...
June 8, 2017: Prostate
https://www.readbyqxmd.com/read/28589573/in-vitro-and-in-vivo-effect-of-flutamide-on-steroid-hormone-secretion-in-canine-and-human-inflammatory-breast-cancer-cell-lines
#9
S Caceres, B Monsalve, L Peña, P J de Andres, A Alonso-Diez, M J Illera, W A Woodward, J M Reuben, G Silvan, J C Illera
The aim was to study the effects of flutamide on cell proliferation, in vivo tumour growth and steroid production in canine and human IBC cell lines. IPC-366 and SUM149 cell cultures were exposed to flutamide concentrations for 72 hours. Additionally, IPC-366 and SUM149 xenotransplanted mice were treated subcutaneously with flutamide 3 times a week for 2 weeks. Steroid hormones determination in culture media, serum and tumour homogenates (pregnenolone, progesterone, androstenedione, testosterone, dihydrotestosterone, 17β-oestradiol and oestrone sulphate) were assayed by EIA...
June 6, 2017: Veterinary and Comparative Oncology
https://www.readbyqxmd.com/read/28582536/is-dihydrotestosterone-a-classic-hormone
#10
Bradley D Anawalt
No abstract text is available yet for this article.
June 1, 2017: Endocrine Reviews
https://www.readbyqxmd.com/read/28558869/triptolide-reduces-prostate-size-and-androgen-level-on-testosterone-induced-benign-prostatic-hyperplasia-in-sprague-dawley-rats
#11
Yu-Rong Wang, Yuan Xu, Zhen-Zhou Jiang, Lu-Yong Zhang, Tao Wang
Benign prostatic hyperplasia (BPH) is an age-related disease of unknown etiology, characterized by prostatic enlargement coincident with distinct alterations in tissue histology. In the present study, we investigated whether triptolide can prevent testosterone-induced prostatic hyperplasia in rats. Castration was performed via the scrotal route after urethane aesthesia. BPH was induced in experimental groups by daily subcutaneous injections of testosterone propionate (TP) for two weeks. Triptolide was administered daily by oral gavage at a dose of 100 and 50 μg·kg(-1) for 2 weeks, along with the TP injections...
May 2017: Chinese Journal of Natural Medicines
https://www.readbyqxmd.com/read/28555252/the-perinatal-effects-of-maternal-caffeine-intake-on-fetal-and-neonatal-brain-levels-of-testosterone-estradiol-and-dihydrotestosterone-in-rats
#12
S Karaismailoglu, M Tuncer, S Bayrak, G Erdogan, E L Ergun, A Erdem
Testosterone, estradiol, and dihydrotestosterone are the main sex steroid hormones responsible for the organization and sexual differentiation of brain structures during early development. The hypothalamo-pituitary-adrenocortical axis, adrenal cells, and gonads play a key role in the production of sex steroids and express adenosine receptors. Caffeine is a non-selective adenosine antagonist; therefore, it can modulate metabolic pathways in these tissues. Besides, the proportion of pregnant women that consume caffeine is ∼60%...
May 29, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28554725/substrate-inhibition-of-17beta-hsd1-in-living-cells-and-regulation-of-17beta-hsd7-by-17beta-hsd1-knockdown
#13
Hui Han, Jean-François Thériault, Guang Chen, Sheng-Xiang Lin
This study addresses first the role of human 17beta-hydroxysteroid dehydrogenase type 1 (17β-HSD1) in breast cancer (BC). The enzyme has a high estrone-activating activity that is subject to strong substrate inhibition as shown by enzyme kinetics at the molecular level. We used BC cells to verify this phenomenon in living cells: estrone concentration increase did reduce the reaction with 0.025 to 4μM substrate. Moreover, 5α-dihydrotestosterone (DHT) demonstrated some inhibition of estrogen activation at both the molecular and cellular level...
May 26, 2017: Journal of Steroid Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/28552457/butylated-hydroxyanisole-alters-rat-5%C3%AE-reductase-and-3%C3%AE-hydroxysteroid-dehydrogenase-implications-for-influences-of-neurosteroidogenesis
#14
Jingjing Guo, Lili Li, Songyi Zhou, Ying Su, Xiaoheng Li, Jianliang Sun, Ren-Shan Ge
Butylated hydroxyanisole is a synthetic antioxidant. It may affect the function of the nerve system. The objective of the present study is to investigate the direct effects of butylated hydroxyanisole on rat brain neurosteroidogenic 5α-reductase 1 (SRD5A1), 3α-hydroxysteroid dehydrogenase (AKR1C14), and retinol dehydrogenase 2 (RDH2). Rat SRD5A1, AKR1C14, and RDH2 were cloned and expressed in COS1 cells, and the effects of butylated hydroxyanisole on these enzyme activities were measured. Butylated hydroxyanisole inhibited SRD5A1, AKR1C14, and RDH2 with IC50 values of 4...
May 24, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/28552345/effect-of-propofol-on-androgen-receptor-activity-in-prostate-cancer-cells
#15
Kenichiro Tatsumi, Akiko Hirotsu, Hiroki Daijo, Tomonori Matsuyama, Naoki Terada, Tomoharu Tanaka
Androgen receptor is a nuclear receptor and transcription factor activated by androgenic hormones. Androgen receptor activity plays a pivotal role in the development and progression of prostate cancer. Although accumulating evidence suggests that general anesthetics, including opioids, affect cancer cell growth and impact patient prognosis, the effect of those drugs on androgen receptor in prostate cancer is not clear. The purpose of this study was to investigate the effect of the general anesthetic propofol on androgen receptor activity in prostate cancer cells...
May 25, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28549802/design-synthesis-and-biological-evaluation-of-novel-androst-3-5-diene-3-carboxylic-acid-derivatives-as-inhibitors-of-5%C3%AE-reductase-type-1-and-2
#16
Kejing Lao, Jie Sun, Chong Wang, Weiting Lyu, Boshen Zhou, Ruheng Zhao, Qian Xu, Qidong You, Hua Xiang
5α-Reductase is a key enzyme responsible for dihydrotestosterone biosynthesis and has been recognized as an important target for discovering new drugs against benign prostatic hyperplasia (BPH). In this study, a series of novel steroidal androst-3,5-diene-3-carboxylic acids have been designed and synthesized. Biological evaluations were performed on their 5α-reductase inhibitory activities by both in vitro enzyme inhibition assay and in vivo by prostate weighing method. Results showed that most of them displayed excellent 5α-reductase inhibitory potency...
May 24, 2017: Steroids
https://www.readbyqxmd.com/read/28549324/salinity-and-sensitivity-to-endocrine-disrupting-chemicals-a-comparison-of-reproductive-endpoints-in-small-bodied-fish-exposed-under-different-salinities
#17
Thijs Bosker, Giacomo Santoro, Steven D Melvin
The influence of salinity on toxicity outcomes has been demonstrated for various contaminants, but has received limited attention for endocrine disrupting chemicals (EDCs). Short-term laboratory tests using small-bodied fish are an important tool for evaluating impacts of EDCs on reproduction. Tests have been developed for both freshwater and estuarine/marine species, providing an opportunity to assess whether concentrations at which small-bodied fish respond to EDCs may be influenced by salinity. We conducted a semi-quantitative review of short-term laboratory tests with small-bodied fish exposed to EDCs, including 59 studies under freshwater conditions (7 species) and 23 studies conducted under saline conditions (5 species)...
May 16, 2017: Chemosphere
https://www.readbyqxmd.com/read/28511915/altered-ionic-currents-and-amelioration-by-igf-1-and-pacap-in-motoneuron-derived-cells-modelling-sbma
#18
Aura M Jiménez Garduño, Leon J Juárez-Hernández, María J Polanco, Laura Tosatto, Daniela Michelatti, Daniele Arosio, Manuela Basso, Maria Pennuto, Carlo Musio
Spinal and bulbar muscular atrophy (SBMA), also known as Kennedy's disease, is a motor neuron disease caused by the expansion of a polymorphic CAG tandem repeat encoding a polyglutamine (polyQ) tract in the androgen receptor (AR) gene. SBMA is triggered by the binding of mutant AR to its natural ligands, testosterone and dihydrotestosterone (DHT). To investigate the neuronal alterations of motor neuron cell models of SBMA, we applied patch-clamp methods to verify how polyQ expansions in the AR alter cell ionic currents...
May 10, 2017: Biophysical Chemistry
https://www.readbyqxmd.com/read/28501574/androgen-production-in-pediatric-adrenocortical-tumors-may-occur-via-both-the-classic-and-or-the-alternative-backdoor-pathway
#19
Nesa Marti, Jana Malikova, José A Galván, Maude Aebischer, Marco Janner, Zdenek Sumnik, Barbora Obermannova, Genevieve Escher, Aurel Perren, Christa E Flück
Children with adrenocortical tumors (ACTs) often present with virilization due to high tumoral androgen production, with dihydrotestosterone (DHT) as most potent androgen. Recent work revealed two pathways for DHT biosynthesis, the classic and the backdoor pathway. Usage of alternate routes for DHT production has been reported in castration-resistant prostate cancer, CAH and PCOS. To assess whether the backdoor pathway may contribute to the virilization of pediatric ACTs, we investigated seven children suffering from androgen producing tumors using steroid profiling and immunohistochemical expression studies...
May 10, 2017: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/28488586/uridine-diphosphate-glucuronosyltransferase-2b15-d85y-gene-polymorphism-is-associated-with-lower-prostate-cancer-risk-a-systematic-review-and-meta-analysis
#20
Xiao Zhong, Jiayu Feng, Ya Xiao, Pingxian Wang, Qiming Fan, Ronghua Wu, Wengang Hu, Chibing Huang
UGT2B15 (uridine diphosphate-glucuronosyltransferase 2B15) catalyzes the conversion of lipophilic C19 steroid androgens such as dihydrotestosterone (DHT) into water-soluble metabolites that can be excreted. Studies of the association between the UGT2B15 gene D85Y polymorphism and prostate cancer have yielded contradictory results. We therefore systematically searched in the PubMed, EMBASE, Science Direct/Elsevier, CNKI, and Cochrane Library databases, and identified six relevant studies with which to perform a meta-analysis of the relation between UGT2B15 D85Y polymorphism and prostate cancer risk...
April 24, 2017: Oncotarget
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