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Topic: Androgen antagonist

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	ACS :: Hormone (Androgen Deprivation) Therapy
		Androgens, produced mainly in the testicles, stimulate prostate cancer cells to grow.
		But unlike some of the other methods of lowering androgen levels, it is permanent, and many men have trouble accepting the removal of their testicles.
		In one form of intermittent therapy, androgen suppression is stopped once the blood PSA level drops to a very low level.
	www.cancer.org /docroot/CRI/content/CRI_2_4_4X_Androgen_Suppression_Hormone_Therapy_36.asp?sitearea= (1535 words)

	Antiandrogen - Wikipedia, the free encyclopedia
		An antiandrogen, or androgen antagonist, is any of a group of hormone antagonist compounds that are capable of preventing or inhibiting the biologic effects of androgens, male sex hormones, on normally responsive tissues in the body (see androgen insensitivity syndrome).
		Antiandrogens are often indicated to treat severe male sexual disorders, such as hypersexuality (excessive sexual desire) and sexual deviation, specifically paraphilias, as well as use as a antineoplastic agent and palliative, adjuvant or neoadjuvant hormonal therapy in prostate cancer.
		Spironolactone (Aldactone, Spiritone), a synthetic 17-spirolactone corticosteroid, which is a renal competitive aldosterone antagonist in a class of pharmaceuticals called potassium-sparing diuretics, used primarily to treat low-renin hypertension, hypokalemia, and Conn's syndrome.
	en.wikipedia.org /wiki/Antiandrogens (471 words)

	Androgen Biology Group » Laboratory of Reproductive and Developmental Toxicology » NIEHS
		Published evidence for androgen effects to shift stem cells towards a myoid pathway as opposed to an adipocytic pathway supports a role for endocrine disruptors as environmental factors affecting obesity in humans.
		The effects of androgens (testosterone and dihydrotestosterone; DHT) are chiefly meditated via androgen receptor (AR), which plays an essential role in a variety of biological processes, including energy expenditure, metabolism and control of body composition.
		Androgen receptor agonists in the environment, for example may predispose differentiation of stem cells towards muscle cell lineage, whereas AR antagonists may direct stem cells away from muscle and towards the fat cell phenotype.
	dir.niehs.nih.gov /dirlrdt/androgen.htm (1401 words)

	DIM and Prostate Health
		Although androgen ablation was found to be effective in treating androgen-dependent prostate cancer, no effective life-prolonging therapy is available for androgen-independent cancer.
		Androgen receptor (AR), cyclin D1, and cdk4, induced by R1881, are downregulated by DIM.
		Plant-derived 3,3'-Diindolylmethane is a strong androgen antagonist in human prostate cancer cells.
	www.dimfaq.com /site/prostatehealth.html (2173 words)

	Androgen Resistance, Part 2 - Prostate Cancer Research Institute
		In laboratory experiments, culture of human prostate cancer cells in the absence of androgen for prolonged time periods led to the development of cells whose growth is stimulated by the addition of Casodex®.
		When removal of androgen, lack of IGF-1, and other forces that push the cell toward suicide reach a critical point, the mitochondria release the compound cytochrome C, which initiates cell death.
		Two drugs that have been proposed to deactivate bcl-2 by phosphorylation are paclitaxel (taxol®) and docetaxel (Taxotere®); their ability to alter bcl-2 phosphorylation may explain why they can enhance the anti-tumor activity of radiation therapy and interact synergistically with a range of other agents.
	www.prostate-cancer.org /education/andeprv/Myers_AndrogenResistance2.html (3681 words)

	Interaction of Organophosphate Pesticides and Related Compounds with the Androgen Receptor
		The observation that the antagonist activity decreases as alkyl chain length increases indicates that the increase in steric bulk in the vicinity of thiophosphonyl group inhibits AR binding affinity.
		Mutations of androgen receptor gene in androgen insensitivity syndromes.
		Androgen receptor antagonist versus agonist activities of the fungicide vinclozolin relative to hydroxyflutamide.
	www.ehponline.org /members/2003/5671/5671.html (6494 words)

	Anti-androgens as hair loss medication
		Antiandrogen or Androgen Antagonist factors are a group of hormone antagonist compounds that are capable of preventing or inhibiting the biologic effects of androgens; the male sex hormones.
		Androgen antagonists do not stop the production or conversion of androgens but they counteract the actions of androgens.
		The anti-androgens and androgen atagonists which are used to prevent or reverse premature hair loss are: progesterone, spironolactone (Aldactone®), flutamide (Eulexin®), finasteride (Proscar®), cimetidine (Tagamet®), Serenoa repens (Permixon®) and cyproterone acetate (Androcur/Diane®).
	www.hairlossinformation.com /hair-loss-in-men/anti-androgens.shtml (780 words)

	Reduction in Penis Size and Plasma Testosterone Concentrations in Juvenile Alligators Living in a Contaminated ... (Site not responding. Last check: 2007-10-23)
		We have hypothesized that the reduced plasma androgen levels in hatchling and juvenile alligators from Lake Apopka (Guillette et al., 1994) are due to modifications in liver degradation of androgens or modifications in the synthesis of plasma proteins responsible for binding steroids.
		Although mean plasma androgen concentrations are different between the males caught on the two lakes, it is very obvious that the major differences in plasma testosterone exist in the larger size classes.
		In mammals, the lack of androgen receptors-testicular feminization or androgen insensitivity syndrome-produces a condition where the male phenotype does not develop and XY individuals develop the external genitalia normal of females (Wilson and Foster, 1985).
	www.mindfully.org /Pesticide/Alligator-Penis-Apopka-Guillette.htm (5949 words)

	eMedicine - Prostate Cancer: Neoadjuvant Androgen Deprivation : Article by Vipul Patel, MD
		Antagonistic effect suppresses LH and FSH hormones, causing serum testosterone level to decrease, which in turn slows prostate cancer growth.
		While the evidence suggests that 3 months of androgen deprivation therapy is not sufficient, current evidence indicates that increasing the duration of therapy to 6 or 8 months further reduces tumor volume and PSA nadir levels and decreases the proportion of men with positive margins.
		The combination of androgen deprivation with cytotoxic chemotherapy in patients with adverse prognostic factors who elect to undergo RP may improve the future of neoadjuvant therapy.
	www.emedicine.com /med/topic3396.htm (6404 words)

	Selection for Androgen Receptor Mutations in Prostate Cancers Treated with Androgen Antagonist -- Taplin et al. 59 ...
		The role of androgen receptor (AR) mutations in androgen-independent
		Culig Z., Hobisch A., Cronauer M. V., Cato A. C., Hittmair A., Radmayr C., Eberle J., Bartsch G., Klocker H. Mutant androgen receptor detected in an advanced-stage prostatic carcinoma is activated by adrenal androgens and progesterone.
		Mutation of the androgen receptor causes oncogenic transformation of the prostate
	cancerres.aacrjournals.org /cgi/content/full/59/11/2511 (4366 words)

	Myc confers androgen-independent prostate cancer cell growth -- Bernard et al. 112 (11): 1724 -- Journal of Clinical ... (Site not responding. Last check: 2007-10-23)
		pathways by pharmacological inhibitors of the androgen receptor
		Amplification of the androgen receptor gene in bone metastases from hormone-refractory prostate cancer.
		Methylation and inactivation of estrogen, progesterone, and androgen receptors in prostate cancer.
	www.jci.org /cgi/content/full/112/11/1724 (4641 words)

	Effects of castration and androgen treatment on androgen-receptor levels in rat skeletal muscles -- Antonio et al. 87 ...
		Regulation of immunoreactive androgen receptor in the adrenal gland of the adult rat.
		Quantification of androgen binding, androgen tissue levels, and sex hormone-binding globulin in prostate, muscle and plasma of patients with benign prostatic hypertrophy.
		Androgen use by athletes: a reevaluation of the health risks.
	jap.physiology.org /cgi/content/full/87/6/2016 (2575 words)

	Androgen-dependent regulation of human angiotensinogen expression in KAP-hAGT transgenic mice -- Ding and Sigmund 280 ...
		Regulation of gene expression by androgens in murine kidney.
		Androgen regulation of rat renal angiotensinogen messenger RNA expression.
		Androgen regulated expression of kidney androgen-regulated protein mRNA is localized in the epithelial cells of the murine renal proximal convoluted tubules.
	ajprenal.physiology.org /cgi/content/full/280/1/F54 (4439 words)

	CancerNetwork:
		Thus, the first therapeutic intervention in patients who progress during therapy with an androgen antagonist to which they previously responded should be discontinuation of the antiandrogen with a period of observation and documentation of progression, particularly prior to enrollment in any study.
		Mutation of the androgen receptor gene in metastatic androgen-independent prostate cancer.
		In concert with this stage migration, androgen deprivation therapy is being applied to the treatment of patients with T3 and even earlier stages of the disease, although the value of this approach is not altogether certain.
	www.cancernetwork.com /journals/oncology/o9710e.htm (9001 words)

	Plant-derived 3,3'-Diindolylmethane Is a Strong Androgen Antagonist in Human Prostate Cancer Cells -- Le et al. 278 ...
		Plant-derived 3,3'-Diindolylmethane Is a Strong Androgen Antagonist in Human Prostate Cancer Cells -- Le et al.
		B, recombinant androgen receptor (PanVera) at 6 pmol/reaction was used in the competitive binding assay.
		Down-regulation of Androgen Receptor by 3,3'-Diindolylmethane Contributes to Inhibition of Cell Proliferation and Induction of Apoptosis in Both Hormone-Sensitive LNCaP and Insensitive C4-2B Prostate Cancer Cells.
	www.jbc.org /cgi/content/full/278/23/21136 (5332 words)

	A Glucocorticoid-Responsive Mutant Androgen Receptor Exhibits Unique Ligand Specificity: Therapeutic Implications for ...
		the GR/PR antagonist RU486, and the MR/AR antagonist spironolactone.
		Culig Z, Hobisch A, Cronauer MV, Cato AC, Hittmair A, Radmayr C, Eberle J, Bartsch G, Klocker H 1993 Mutant androgen receptor detected in an advanced-stage prostatic carcinoma is activated by adrenal androgens and progesterone.
		Tilley WD, Buchanan G, Hickey TE, Bentel JM 1996 Mutations in the androgen receptor gene are associated with progression of human prostate cancer to androgen independence.
	endo.endojournals.org /cgi/content/full/143/5/1889 (6380 words)

	Hairloss-reversible.com: "Free" testosterone (Site not responding. Last check: 2007-10-23)
		The amount of free testosterone available for this conversion is determined by two factors: (1) how much testosterone is produced, and (2) the amount of androgen antagonists.
		If the ratio of androgen antagonists to testosterone is high, then there will be less free testosterone to be converted into DHT.
		Supposedly a diet high in amimal fat reduces the amount of this androgen antagonist thereby "freeing" testosterone to be converted into DHT.
	www.hairloss-reversible.com /discus/messages/4/26.html?1062156102 (376 words)

	Distinguishing Androgen Receptor Agonists and Antagonists: Distinct Mechanisms of Activation by Medroxyprogesterone ...
		and is inhibited by coincubation with the antagonist hydroxyflutamide
		H]19-nortestosterone for the estimation of androgen receptor in rat liver cytosol.
		-dimethyl-19-nortestosterone (mibolerone) in the assay of androgen receptors.
	mend.endojournals.org /cgi/content/full/13/3/440 (6760 words)

	Effects of Androgen on Androgen Receptor Expression in Rat Testicular and Epididymal Cells: A Quantitative ...
		Regulation of androgen receptor protein and mRNA concentrations by androgens in rat ventral prostate and seminal vesicles and in human hepatoma cells.
		Androgen receptor distribution in rat testis: new implantations for androgen regulation of spermatogenesis.
		Androgen transport and receptor mechanisms in testis and epididymis.
	www.biolreprod.org /cgi/content/full/63/2/368 (5345 words)

	Persistent DDT metabolite p,p'–DDE is a potent androgen receptor antagonist
		Persistent DDT metabolite p,p'–DDE is a potent androgen receptor antagonist
		THE increase in the number of reports of abnormalities in male sex development in wildlife and humans coincided with the introduction of 'oestrogenic' chemicals such as DDT (1,1,1-trichloro-2,2-bis(p-chlorophenyl)ethane) into the environment.
		Although these phenotypic alterations are thought to be mediated by the oestrogen receptor, they are also consistent with inhibition of androgen receptor-mediated events.
	www.nature.com /cgi-taf/DynaPage.taf?file=/nature/journal/v375/n6532/abs/375581a0.html (397 words)

	Nongenomic Effects of Androstenedione on Human Granulosa Luteinizing Cells -- Machelon et al. 83 (1): 263 -- Journal of ...
		1990 Immunohistochemical localization of androgen receptors with mono- and polyclonal antibodies to androgen receptors with mono- and polyclonal antibodies to androgen receptor.
		1994 Immunohistochemical distribution of progesterone, androgen and estrogen receptors in the human ovary during the mentrual cycle: relationship to expression of steroidogenic enzymes.
		Biochemical Characterization of a Membrane Androgen Receptor in the Ovary of the Atlantic Croaker (Micropogonias undulatus)
	jcem.endojournals.org /cgi/content/full/83/1/263 (4042 words)

	Neonatal Coadministration of Testosterone With Diethylstilbestrol Prevents Diethylstilbestrol Induction of Most ...
		Preserved male fertility despite decreased androgen sensitivity caused by a mutation in the ligand-binding domain of the androgen receptor gene.
		Suppression of androgen action and the induction of gross abnormalities of the reproductive tract in male rats treated neonatally with diethylstilbestrol.
		Prins GS, Birch L. The developmental pattern of androgen receptor expression in rat prostate lobes is altered after neonatal exposure to estrogen.
	www.andrologyjournal.org /cgi/content/full/24/4/557 (5423 words)

	Gender Differences in Hypertension in Spontaneously Hypertensive Rats : Role of Androgens and Androgen Receptor -- ...
		androgen receptors and therefore lack secondary androgen characteristics.
		Androgen receptor and the testes influence hypertension in a hybrid rat model.
		Androgens augment renal vascular responses to ANG II in New Zealand genetically hypertensive rats
	hyper.ahajournals.org /cgi/content/full/34/4/920 (3204 words)

	Androgen Antagonist Activity by the Antioxidant Moiety of Vitamin E, 2,2,5,7,8-Pentamethyl-6-chromanol in Human ...
		Androgen Antagonist Activity by the Antioxidant Moiety of Vitamin E, 2,2,5,7,8-Pentamethyl-6-chromanol in Human Prostate Carcinoma Cells -- Thompson and Wilding 2 (8): 797 -- Molecular Cancer Therapeutics
		Androgen Antagonist Activity by the Antioxidant Moiety of Vitamin E, 2,2,5,7,8-Pentamethyl-6-chromanol in Human Prostate Carcinoma Cells
		LNCaP cells were grown in medium containing 5% serum to provide endogenous serum androgens, thus allowing antiandrogenic modulation of AR protein levels.
	mct.aacrjournals.org /cgi/content/full/2/8/797 (4120 words)

	Inhibition of Recovery of Spermatogenesis in Irradiated Rats by Different Androgens -- Shetty et al. 143 (9): 3385 -- ...
		androgenic potencies toward a variety of tissues (25).
		GnRH antagonist and androgen treatments were started at wk 3 after irradiation and maintained until the rats were killed at wk 5 (n = 4 per group).
		Comparative effects of the different androgens tested on weights of the seminal vesicle (A), ventral prostate (B), bulbocavernosus muscle (C), and testis (D), in relation to their respective inhibition of GnRH-antagonist-stimulated tubule differentiation.
	endo.endojournals.org /cgi/content/full/143/9/3385 (6970 words)

	Future Directions in the Study and Management of Congenital Adrenal Hyperplasia due to 21-Hydroxylase Deficiency -- ...
		An antiandrogen agent is administered to block the effect of the elevated androgen levels, and an inhibitor of androgen-to-estrogen conversion is given to block conversion of the increased amount of androgen to estrogen.
		In vivo and in vitro characterization of antalarmin, a nonpeptide corticotropin-releasing hormone (CRH) receptor antagonist: suppression of pituitary ACTH release and peripheral inflammation Endocrinology.
		The impact of the nonpeptide corticotropin-releasing hormone antagonist antalarmin on behavioral and endocrine responses to stress Endocrinology.
	www.annals.org /cgi/content/full/136/4/320 (7306 words)

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