Skip to main content

Home/ Dr. Goodyear/ Group items tagged agonist

Rss Feed Group items tagged

Filter: All | Bookmarks | Topics Simple Middle
Nathan Goodyear

The emerging role of estrogen in B cell malignancies: Leukemia & Lymphoma: Vol 58, No 3 - 0 views

www.tandfonline.com/...10428194.2016.1213828

estrogen leukemia lymphoma ER ER beta estrogen receptor cancer

shared by Nathan Goodyear on 27 Nov 17 - No Cached
  • Nathan Goodyear on 27 Nov 17
     
    Evidence that Estrogen and ER status plays role in hematological cancer.  ER-beta agonist inhibited cell growth and induced cell death. Similar to prostate cancer.
Nathan Goodyear

Cannabinoids Promote Progression of HPV-Positive Head and Neck Squamous Cell Carcinoma ... - 0 views

aacrjournals.org/...te-Progression-of-HPV-Positive

head and neck cancer THC p38 MAPK

shared by Nathan Goodyear on 15 Nov 22 - No Cached
  • Nathan Goodyear on 15 Nov 22
     
    THC stimulates p38/MAPK signaling to inhibit apoptosis via CB agonism; good thing CBD is a reverse agonist on CB receptors.
Nathan Goodyear

Update in TSH Receptor Agonists and Antagonists - 0 views

jcem.endojournals.org/...4287.abstract

receptors receptor thyroid TSHR

shared by Nathan Goodyear on 06 Dec 12 - No Cached
  • Nathan Goodyear on 06 Dec 12
     
    Just abstract is available to this just released article, but the opening sentence shows the importance of receptors: "the physiological role of the TSH receptor (TSHR) as a major regulator of thyroid functions is well understood..."
Nathan Goodyear

American College of Cardiology Foundation | Journal of the American College of Cardiolo... - 0 views

content.onlinejacc.org/article.aspx

mitochondria oxidative stress heart failure heart

shared by Nathan Goodyear on 19 Mar 13 - No Cached
  • Although currently no drugs that specifically target mitochondrial biogenesis in HF are available, acceleration of this process through adenosine monophosphate–activated kinase (AMPK), endothelial nitric oxide synthase (eNOS), and other pathways may represent a promising therapeutic approach
  • Mitochondrial biogenesis can be enhanced therapeutically with the use of adenosine monophosphate kinase (AMPK) agonists, stimulants of nitric oxide/cyclic guanosine monophosphate (NO/cGMP) pathway (including phosphodiesteraes type 5 inhibitors), or resveratrol
  • metformin, a commonly used antidiabetic drug that activates AMPK signaling
  • ...10 more annotations...
  • Recent evidence suggests that the eNOS/NO/cGMP pathway is an important activator of mitochondrial biogenesis
  • BH4 (tetrahydrobiopterin) supplementation can prevent eNOS uncoupling and was found to reduce left ventricular hypertrophy
  • folic acid is known to replenish reduced BH4 and has been shown to protect the heart through increased eNOS activity
  • Both folate deficiency and inhibition of BH4 synthesis were associated with reduced mitochondrial number and function
  • Resveratrol, a polyphenol compound responsible for the cardioprotective properties of red wine, was recently identified as a potent stimulator of mitochondrial biogenesis
  • epidemiological studies reveal a reduced risk of cardiovascular disease in premenopausal, but not post-menopausal, women compared with men
  • post-menopausal women
    • Nathan Goodyear
      Nathan Goodyear on 19 Mar 13
       
      I would hypothesis that a change in the predominance of ER expression is one of ER beta to ER alpha: creating a more pro-inflammatory signal.
  • The majority of ROS in the heart appear to come from uncoupling of mitochondrial electron transport chain at the level of complexes I and III
  • Because the majority of ROS in HF comes from mitochondria, these organelles are the primary target of oxidative damage.
  • cardioprotective therapies such as angiotensin-converting enzyme inhibitors and ATII receptor blockers were shown to possess antioxidant properties, although it is not known whether they target mitochondrial ROS directly or indirectly
  • Nathan Goodyear on 19 Mar 13
     
    great review of mitochondrial biogenesis, oxidative stress and heart failure.  
Nathan Goodyear

Natural product agonists of peroxisome proliferator-activated receptor gamma ... - 0 views

www.ncbi.nlm.nih.gov/...PMC4212005

PPAR-gamma PPAR inflammation natural

shared by Nathan Goodyear on 26 Apr 16 - No Cached
  • Nathan Goodyear on 26 Apr 16
     
    to read.
Nathan Goodyear

Genomic agonism and phenotypic antagonism between estrogen and progesterone receptors i... - 0 views

advances.sciencemag.org/...e1501924.full

progesterone PR progesterone receptors progesterone receptor cancer breast cancer hormones

shared by Nathan Goodyear on 29 Jun 16 - No Cached
  • The presence and activity of PR significantly affect the prognostic value of ER.
  • The observed loss of PR protein expression in a subset of ER+/PR+ breast cancers, because of hypermethylation or deletion of the PR gene locus, results in the loss of ER prognostic value
  • These findings emphasize the clinical value of assessing both PR and ER expression in breast cancer samples
  • ...7 more annotations...
  • PR is an essential modulator of ER-regulated genes but also that it significantly contributes to the prognostic value of ER in ER+/PR+ breast cancers
  • PR-regulated genes have independent prognostic value, and the presence of PR correlates with favorable clinicopathological outcomes
  • this study demonstrates that progestin-activated PR redirects ER chromatin binding and functions as a genomic estrogen agonist and as a phenotypic estrogen antagonist in ER+/PR+ breast cancer cells and human tumors
  • Approximately 80% of ER+ breast cancers are also positive for PR,
  • In isolation, both hormones activate or inhibit cellular processes in similar directions, although the magnitude of these effects is less for progestin alone than for estrogen alone
  • PR-mediated antagonism of estrogenic phenotypes is well documented
  • joint activation of ER and PR antagonized ER-regulated oncogenic processes
  • Nathan Goodyear on 29 Jun 16
     
    WOW!!  study finds that progesterone through PR activity antagonizes ER protein expression by the cell.  This has huge implications in breast cancer and possible prostate cancer.  But then again, women don't need progesterone; only estrogen.  The presence of PR correlates with improved clinicopathological outcomes.  The authors do seem to get confused about progesterone and progestins.  They are not one in the same.
Nathan Goodyear

ingentaconnect Adipose Tissue Macrophages, Low Grade Inflammation and Insulin Re... - 0 views

www.ingentaconnect.com/...art00009

ATMs obesity inflammation inflammatory reaction insulin resistance IR diabetes DM type II macrophages

shared by Nathan Goodyear on 10 Jan 12 - No Cached
  • “M1” or “classically activated” macrophages
  • PPAR-gamma agonists
  • “M2” or an “alternatively activated” anti-inflammatory phenotype
  • Nathan Goodyear on 10 Jan 12
     
    ATMs and obesity induced inflammation initiates insulin resistance and thus type II diabetes. The bodies reaction to a fat cell is no different than a bacterial, viral, or parasitic infection.  The body recognizes something (fat) that shouldn't be there and it attempts to destroy it and remove it.
Nathan Goodyear

Adiponectin translation is increased by the PPARγ agonists pioglitazone and ω... - 0 views

ajpendo.physiology.org/...E480.long

n-3 omega-3 DHA EPA adiponectin PPAR-gamma obesity adipocytes fatty acids

shared by Nathan Goodyear on 13 Jun 12 - No Cached
  • Nathan Goodyear on 13 Jun 12
     
    Omeg-3, DHA and EPA, increased adiponectin production.  In addition, blockade of the PPAR-gamma resulted in a reduction in adiponectin production.  Thus PPAR gamma activation results in adiponectin production by adipocytes.
Nathan Goodyear

A strong association between biologically active testosterone and leptin in non-obese m... - 0 views

www.nature.com/...0801467a.html

leptin Testosterone hormone hormones obesity

shared by Nathan Goodyear on 22 Oct 14 - No Cached
  • strongly supports an association between levels of androgens and leptin in both men and women
  • The association between androgen levels and leptin seems to be dependent of fat distribution in men
  • There is a growing bulk of evidence suggesting that testosterone may influence leptin levels. Testosterone administration reduces leptin levels in hypogonadal27,28 and eugonadal men
  • ...5 more annotations...
  • testosterone suppression by GnRH agonist treatment of central precocious puberty in boys increases leptin levels
  • Testosterone levels decreased with increasing central obesity in healthy men, while they increase with increasing obesity in healthy women, the latter irrespective of menstrual status
  • this could be due to obesity-related hyperleptinemia that inhibits testosterone secretion at the testicular level.46,47 These changes, which are proposed to be components of the insulin resistance syndrome,48 are associated with increased risk for cardiovascular disease in both men and women
  • in the more obese subjects, the higher leptin levels due to increased adiposity might reduce secretion of testosterone
  • loss of regulation of leptin by testosterone in obese men and women could be an important feature of the insulin resistance syndrome
  • Nathan Goodyear on 22 Oct 14
     
    Leptin and Testosterone.  Interesting relationship that differs between the sexes.
Nathan Goodyear

Modulation of NF-[kappa]B-dependent transcription and cell survival by the SIRT1 deacet... - 0 views

www.nature.com/...7600244a.html

resveratrol inflammation

shared by Nathan Goodyear on 18 Mar 11 - No Cached
  • Treatment of cells with resveratrol, a small-molecule agonist of Sirtuin activity, potentiates chromatin-associated SIRT1 protein on the cIAP-2 promoter region, an effect that correlates with a loss of NF-B-regulated gene expression
  • Nathan Goodyear on 18 Mar 11
     
    resveratrol decreases NF-kappa Beta expression and thus reduces inflammation
Nathan Goodyear

Plant-derived 3,3′-Diindolylmethane Is a Strong Androgen Antagonist in Human ... - 0 views

www.jbc.org/...21136.full

DIM I3C PSA AR androgen receptor prostate cancer men male hormone hormones androgen

shared by Nathan Goodyear on 05 Nov 14 - No Cached
  • Inhibition of Endogenous PSA Expression by DIM
  • DIM strongly inhibited DHT induction of androgen-responsive genes by more than 50%
  • antiandrogenic activity of DIM
  • ...8 more annotations...
  • DIM suppresses DHT-induced cell growth and PSA expression and exhibits no AR agonist activity
  • DIM has a strong affinity for both the mutant AR inLNCaP cells and for recombinant wild-type human AR
  • nuclear translocation and foci formation of DHT-bound AR are inhibited by DIM
  • Our investigation, leads to the conclusion that DIM is a strong, pure androgen antagonist.
  • The down-regulation of PSA by DIM
  • PSA has been reported to promote the proliferation, migration, and metastasis of prostate cancer cells through several mechanisms, including cleavage of insulin-like growth factor-binding protein-3 and degradation of extracellular matrix proteins fibronectin and laminin
  • PSA expression is regulated by the AR and is thought to function as a growth factor in LNCaP cells
  • down-regulation of PSA expression may be important in the antiproliferative effects of DIM in LNCaP cells
  • Nathan Goodyear on 05 Nov 14
     
    DIM, from cruciferous veggies often used to aid estrogen metabolism, is found to decrease PSA transcription and function as an androgen receptor antagonist in prostate cancer cell lines.
Nathan Goodyear

Differential Effects of Dehydroepiandrosterone and Testosterone in Prostate and Colon C... - 0 views

press.endocrine.org/...en.2012-2249

testosterone prostate colon colon cancer cancer NGF nerve growth factor dhea dehydroepiandrosterone

shared by Nathan Goodyear on 19 Nov 14 - No Cached
  • Several studies indicate that DHEA may enhance cancer-promoting activities in several prostate cancer cell lines acting as agonist or antagonist for the intracellular AR
  • the estrogenic metabolites of DHEA, 5a-androstane-3b, 17b-diol (3b-Adiol) and E2 bind to estrogen receptors but not to AR
  • no specific receptor has been identified for DHEA
  • ...16 more annotations...
  • Different members of neurotrophins are expressed during cancer progression, suggesting their involvement in cell proliferation, anoikis protection, and malignancy
  • Regulation of the apoptotic machinery in prostate and colon cancer cells by testosterone occurs rapidly and is initiated at the plasma membrane level through specific membrane-binding sites not involving the classical cytoplasmic AR
  • testosterone exerts potent regulatory effects on prostate and colon cancer cell apoptosis
  • Testosterone increased cell death in a dose-dependent manner
  • testosterone antagonizes the prosurvival effects of DHEA in neuronal cells, blocking its binding to NGF receptors
  • treatment of cells with DHEA exerted a strong antiapoptotic effect,
  • Androgens hold a central role in prostate and colon cancer biology
  • elevated levels of DHEA or its sulfate ester DHEA-sulfate in young adults are associated to low incidence of androgen-dependent tumors
  • DHEA may play a protective role in young prostate
  • The decline of DHEA with aging may contribute to prostate cancer progression associated with advanced age
  • DHEA is an effective antiapoptotic factor, reversing the serum deprivation-induced apoptosis in prostate cancer cells (DU145 and LNCaP cell lines) as well as in colon cancer cells
  • NGF appears to exert similar antiapoptotic actions in both prostate and color cancer cells
  • exposure of prostate DU145 and colon Caco2 cancer cells to testosterone totally blocked the protective effects of both DHEA and NGF. These findings suggest that testosterone acts as an antagonist of DHEA and NGF
  • These findings support the hypothesis that testosterone may inhibit cancer cell growth by antagonizing the proliferative, antiapoptotic effects of endogenous factors, such as DHEA or NGF, in the case of prostate and colon cancer cells
  • intratumor hormonal microenvironment may play a critical role in tumor progression.
  • The paracrine interactions of androgens with locally produced NGF may define tumor cell fate
  • Nathan Goodyear on 19 Nov 14
     
    Full article of previously posted abstract.  Cancers are unique.  Not all cancers are alike.  Whether they are tissue specific or not, cancers are unique.  This article describes the uniqueness of DHEA and Testosterone cancer, with particular attention to colon.
Nathan Goodyear

Original Articles: Comparison of Insulin Action on Glucose versus Potassium Uptake in H... - 0 views

www.ncbi.nlm.nih.gov/...PMC3133473

diabetes insulin resistance potassium hyperkalemia glucose insulin

shared by Nathan Goodyear on 31 Oct 17 - No Cached
  • When treating hyperkalemia, insulin remains efficacious in diabetics and nondiabetics and one does not need to resort to b-agonists, and diabetics do not require different doses of insulin to shift potassium
  • the commonly encountered “insulin-resistant” patients actually have preserved insulin-induced potassium disposal, one wonders why their high insulin levels are not causing hypokalemia
  • insulin independently regulates glucose and potassium uptake into cells and this independence explains why in noninsulin-dependent diabetic insulin resistance leads to impaired insulin uptake into cells but has no effect on the cell's potassium disposal
  • ...9 more annotations...
  • insulin suppresses glycogenolysis, gluconeogenesis, lipolysis and fatty acid release, and protein catabolism and is the principal hormone that stimulates glucose uptake into mainly skeletal muscle and to a certain extent adipocytes
  • Plasma [K+] is a major determinant of the resting potential of all cells
  • Hyperkalemia and hypokalemia are silent yet fatal disturbances because of their arrhythmogenic potentials
  • Basal insulin maintains fasting plasma [K+] within the normal range
  • When insulin levels are suppressed, plasma [K+] rises and pronounced hyperkalemia develops after a potassium load
  • Potassium is a well proven insulin secretagogue
  • Insulin is a key defender against exogenous potassium load by using intracellular buffering to minimize hyperkalemia before renal excretion
  • Hyperkalemia is often encountered in patients with diabetes
  • The insulin-deficient state in type 1 diabetes predisposes to hyperkalemia because of an impaired ability of potassium to enter cells. During hyperglycemic hypertonic states in type 1 and type 2 diabetics, potassium is carried out of cells by convective flux as the most abundant intracellular cation
  • Nathan Goodyear on 31 Oct 17
     
    good review of the potassium, glucose, insulin relationship mostly in diabetes.  In diabetes, hyperkalemia is present due to the hyperglycemia and the associated exchange.  Inuslin independantly regulates potassium and glucose intake into the cell.  INterestingly, in IR found in diabetes, the hyperkalemia is the norm, which should cause hypokalemia--the authors were perplexed by this finding.
Nathan Goodyear

Premetastatic milieu explained by TLR4 agonist-mediated homeostatic inflammation - 0 views

www.ncbi.nlm.nih.gov/...PMC4001895

metastasis TLRs cancer TLR toll-like receptors TLR4

shared by Nathan Goodyear on 22 Aug 20 - No Cached
  • Nathan Goodyear on 22 Aug 20
     
    To be read
Nathan Goodyear

Enhanced dendritic cell maturation by the B-chain of Korean mistletoe lectin (KML-B), a... - 0 views

pubmed.ncbi.nlm.nih.gov/24859056

dendritic cell Mistletoe dendritic cells

shared by Nathan Goodyear on 14 Sep 23 - No Cached
  • Nathan Goodyear on 14 Sep 23
     
    Mistletoe increases dendritic cell activation.
‹ Previous 21 - 40 of 41 Next ›
Showing 20▼ items per page