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Nathan Goodyear

Treatment of Obesity-Related Complications with Novel Classes of Naturally Occurring PP... - 0 views

www.hindawi.com/...897894

PPAR agonist PPAR agonist

shared by Nathan Goodyear on 17 Jan 13 - No Cached
  • Nathan Goodyear on 17 Jan 13
     
    natural PPAR agonists.  Maybe provide some of the anti-inflammatory improved lipid metabolism without the side effects found in their synthetic counterpart avandia
Nathan Goodyear

LIGAND STRUCTURE-DEPENDENT ACTIVATION OF ESTROGEN RECEPTOR α/Sp BY ESTROGENS ... - 0 views

www.ncbi.nlm.nih.gov/...PMC2519242

xenoestrogens ER-alpha ER alpha ER receptor agonist agonists hormone hormones

shared by Nathan Goodyear on 23 Feb 14 - No Cached
  • Nathan Goodyear on 23 Feb 14
     
    xenoestrogens are estrogen receptor agonists.  This is a good discussion of there interaction with xenoestrogens and particularly ER alpha.
Nathan Goodyear

27-Hydroxycholesterol Links Hypercholesterolemia and Breast Cancer Pathophysiology - 0 views

www.sciencemag.org/...1094

breast cancer cholesterol ER estrogen receptor

shared by Nathan Goodyear on 04 Jan 14 - No Cached
  • Nathan Goodyear on 04 Jan 14
     
    Study finds link between cholesterol metabolite and breast cancer.  The interesting point of this article is not that statins need to be given to all women to prevent breast cancer, which of course is what many will take.  But, that the cholesterol metabolite, 27-hydroxycholesterol showed ER agonist activity.  This would have to be ER-alpha agonist activity though the authors did not clarify.  The 27-hydroxymetabolite is created from CYP27A1.
Nathan Goodyear

Targeting estrogen receptor subtypes (ERα and ERβ) with selective ER modulato... - 0 views

joe.endocrinology-journals.org/...325.abstract

ovarian cancer ER alpha ER beta ER-alpha ER-beta ovary estrogen receptor receptors ER

shared by Nathan Goodyear on 19 May 14 - No Cached
  • Nathan Goodyear on 19 May 14
     
    Studies in breast cancer and prostate cancer have revealed different effects by ER alpha vs ER beta.  It is no surprise that the same effects are found in ovarian cancer.  This study found ER alpha antagonists and ER beta agonists "significantly" suppressed growth in the ovarian cancer cell lines SKOV3 and OV2008.  Also, ER alpha agonist and ER beta antagonist "significantly" increased growth in the same cell lines.  These findings point to in increased proliferation with ER alpha and decreased with ER beta.  This is consistent with breast and prostate cancer also.
Nathan Goodyear

Thyroid Hormone Receptor Agonists Reduce Serum Cholesterol Independent of the LDL Receptor - 0 views

endo.endojournals.org/...6136.abstract

LDL cholesterol T3 thyroid hormone hormones receptor receptors

shared by Nathan Goodyear on 28 Nov 12 - No Cached
  • Nathan Goodyear on 28 Nov 12
     
    New study shows that T3 and thyroid hormone agonists reduce LDL.  This is independent that LDL receptors.  Previously, it was thought that T3 increased LDL receptor expression.  But, this study shows that T3 lowers LDL independent of the LDL receptors.  
Nathan Goodyear

The activity of bisphenol A depends on both the est... [Endocr J. 2002] - PubMed - NCBI - 0 views

www.ncbi.nlm.nih.gov/...12402979

bisphenol A ER estrogen receptor receptors hormone hormones agonist antagonist estrogen receptor BPA

shared by Nathan Goodyear on 07 Jan 13 - No Cached
  • Nathan Goodyear on 07 Jan 13
     
    bisphenol A is shown to be both an ER agonist and an ER antagonist.
Nathan Goodyear

Structural and mechanistic insights into bisphenols action provide guidelines for risk ... - 0 views

www.pnas.org/...1203574109.abstract

BPA bisphenol A ER estrogen receptor agonist hormone hormones

shared by Nathan Goodyear on 07 Jan 13 - No Cached
  • Nathan Goodyear on 07 Jan 13
     
    bisphenol A is a estrogen receptor agonist, though partial.
Nathan Goodyear

Inflammatory Mechanisms in Alzheimer's Disease: Inhibition of β-Amyloid-Stimu... - 0 views

www.jneurosci.org/...558.full

microglia microglial cells inflammation Alzheimer's disease neurodegenerative

shared by Nathan Goodyear on 06 Jan 12 - No Cached
  • The activated microglia mount a complex local proinflammatory response
  • PPARγ plays a critical role in regulating the inflammatory responses of microglia and monocytes to β-amyloid
  • Nathan Goodyear on 06 Jan 12
     
    microglial and inflammatory response in Alzheimer's disease.  Agonists of PPAR-gamma inhibit this action.  This has important implications in reducing the local inflammatory response found in the brains of those with Alzheimers and other neuordegenerative disease.
Nathan Goodyear

PPARs, Obesity, and Inflammation - 0 views

www.ncbi.nlm.nih.gov/...PMC1783744

obesity inflammation PPARs perioxisome proliferator-activated receptor

shared by Nathan Goodyear on 16 Jan 12 - No Cached
  • increase of 61% within 10 years
  • Many of the inflammatory markers found in plasma of obese individuals appear to originate from adipose tissue
  • obesity is a state of chronic low-grade inflammation that is initiated by morphological changes in the adipose tissue.
  • ...19 more annotations...
  • secretion of MCP-1, resistin, and other proinflammatory cytokines is increased by obesity, the adipose secretion of the anti-inflammatory protein adiponectin is decreased
  • the peroxisome proliferators- activated receptor (PPAR) family are involved in the regulation of inflammation and energy homestasis
  • natural agonists, including unsaturated fatty acids and eicosanoids
  • PPARα also regulates inflammatory processes, mainly by inhibiting inflammatory gene expression
  • upregulation of COX-2 is seen in alcoholic steatohepatitis and nonalcoholic steatohepatitis and has been directly linked to the progression of steatosis to steatohepatitis, the inhibitory effect of PPARα on COX-2 may reduce steatohepatitis
  • PPARα agonists have a clear anorexic effect resulting in decreased food intake, evidence is accumulating that PPARα may also directly influence adipose tissue function, including its inflammatory status.
  • PPARα may govern adipose tissue inflammation in three different ways: (1) by decreasing adipocyte hypertrophy, which is known to be connected with a higher inflammatory status of the tissue [3, 11, 59], (2) by direct regulation of inflammatory gene expression via locally expressed PPARα, or (3) by systemic events likely originating from liver
  • PPARγ is considered the master regulator of adipogenesis
  • Unsaturated fatty acids and several eicosanoids serve as endogenous agonists of PPARγ
  • PPARγ2, which is adipose-tissue specific
  • two different molecular mechanisms have been proposed by which anti-inflammatory actions of PPARγ are effectuated: (1) via interference with proinflammatory transcription factors including STAT, NF-κB, and AP-1
  • and (2) by preventing removal of corepressor complexes from gene promoter regions resulting in suppression of inflammatory gene transcription
  • diet-induced obesity is associated with increased inflammatory gene expression in adipose tissue via adipocyte hypertrophy and macrophage infiltration
  • PPARγ is able to reverse macrophage infiltration, and subsequently reduces inflammatory gene expression
  • Inflammatory adipokines mainly originate from macrophages which are part of the stromal vascular fraction of adipose tissue [18, 19], and accordingly, the downregulation of inflammatory adipokines in WAT by PPARγ probably occurs via effects on macrophages
  • By interfering with NF-κB signaling pathways, PPARγ is known to decrease inflammation in activated macrophages
  • Recent data suggest that activation of PPARγ in fatty liver may protect against inflammation
  • PPARs may influence the inflammatory response either by direct transcriptional downregulation of proinflammatory genes
  • anti-inflammatory properties of PPARs in human obesity
  • Nathan Goodyear on 16 Jan 12
     
    PPARs play pivotal in obesity.  PPARs appear to reduce the inflammatory cascade associated with obesity.  Downregulation of PPARs are associated with increased inflammation.  Natural PPARs include unsaturated fats and eicosanoids.
Nathan Goodyear

Inflammatory Mechanisms in Alzheimer's Disease: Inhibition of β-Amyloid-Stimu... - 0 views

www.jneurosci.org/...558.long

inflammation AD alzheimer's neurodegenerative disease PPAR-gamma PPAR microglial alzheimer

shared by Nathan Goodyear on 11 Jun 12 - No Cached
  • PPARγ agonists were shown to inhibit the β-amyloid-stimulated expression of the cytokine genes interleukin-6 and tumor necrosis factor α. Furthermore, PPARγ agonists inhibited the expression of cyclooxygenase-2.
  • Nathan Goodyear on 11 Jun 12
     
    Not that we are recommending NSAIDS to reduce inflammation: but the learned biochemical pathways of inflammation involved with AD, allows a natural approach to reduce microglial associated inflammation through PPAR-gamma activation.
Nathan Goodyear

AroER Tri-Screen™ is a Biologically Relevant Assay for Endocrine Disrupting C... - 0 views

toxsci.oxfordjournals.org/...toxsci.kfu023.abstract

Paxil paroxetine estrogen receptor agonist cancer breast prostate hormone hormones

shared by Nathan Goodyear on 19 Feb 14 - No Cached
  • Nathan Goodyear on 19 Feb 14
     
    Paxil is estrogen receptor agonist.  What is interesting about this is that the FDA just approved this as a non-hormonal way to reduce hot flashes--but it is paxil under a different name.  It is non-hormonal--yeah right.  The organization making the approval doesn't know what they are doing at worse, or like the IOM stated are not up with the latest scientific knowledge.
Nathan Goodyear

The Incretins: GLP-1 Agonists and DPP-4 Inhibitors | Diabetesnet.com - 0 views

www.diabetesnet.com/...incretins

GLP-1 incretins insulin glucose diabetes obesity overweight

shared by Nathan Goodyear on 06 Apr 11 - No Cached
  • Nathan Goodyear on 06 Apr 11
     
    GLP-1 agonists improve insulin/glucose control
Nathan Goodyear

Transrepression of Inflammation -- Foley 4 (173): ec141 -- Science Signaling - 0 views

stke.sciencemag.org/...ec141

ER-beta inflammation microglia astrocyte MS multiple sclerosis autoimmune disease

shared by Nathan Goodyear on 06 Oct 12 - No Cached
  • Nathan Goodyear on 06 Oct 12
     
    ER-beta agonist activity/agnoists inhibit inflammatory gene expression in microglia and astrocyte cells.
Nathan Goodyear

Essential Role for Estrogen Receptor β in Stromal-Epithelial Regulation of Pr... - 0 views

endo.endojournals.org/...566.abstract

ER-alpha ER-beta BPH aromatase activity prostate men male T testosterone low estrogen

shared by Nathan Goodyear on 19 Sep 12 - No Cached
  • Nathan Goodyear on 19 Sep 12
     
    ER beta agonists shown to be anti-proliferative in the prostate and "ablated preexisting prostatic epithelial hyperplasia".  This has important implications: low T conditions increase ER alpha expression, which increases ER alpha production.  Low T is a pro inflammatory state in men, which increases aromatase activity.  Thus increase conversion of T to E2 in the stroma of the prostate results in growth.  ER beta is not activated.
Nathan Goodyear

Mechanisms of Estrogen Action - 0 views

physrev.physiology.org/...1535.full

estrogen receptor receptors ER alpha ER-alpha ER beta ER-beta

shared by Nathan Goodyear on 27 Jan 14 - No Cached
  • Nathan Goodyear on 27 Jan 14
     
    good discussion of estrogen receptors and their role of estrogen signaling transmission.This article goes deep into coregulators, corepressors, cofactors, agonists, antagonists...
Nathan Goodyear

Effects of Peroxisome Proliferator-Activated Receptor-α and -γ Agonists on 11... - 0 views

jcem.endojournals.org/...1848.long

11-betaHSD1 PPAR agonist PPAR-alpha PPAR-gamma PPARs cortisol

shared by Nathan Goodyear on 08 Oct 13 - No Cached
  • Nathan Goodyear on 08 Oct 13
     
    PPAR alpha and/or PPAR gamma does not down regulate 11Beta-HSD1.
Nathan Goodyear

The Androgen 5α-Dihydrotestosterone and Its Metabolite 5α-Androstan-3β, 17β-D... - 0 views

www.jneurosci.org/...1448.full

DHT 3 beta androstanediol androgens Hypothalamus HPA hormones stress

shared by Nathan Goodyear on 15 Jul 15 - No Cached
  • Sex steroid hormones are primarily responsible for sex difference in adult HPA function; androgens inhibit whereas estrogens enhance HPA axis activation after a stressor
  • the PVN contains relatively high levels of AR (Bingaman et al., 1994; Zhou et al., 1994) and ERβ (Alves et al., 1998; Hrabovszky et al., 1998; Somponpun and Sladek, 2003) but is essentially devoid of ERα
  • the nonaromatizable androgen DHT and the nonselective ER ligand E2 influence HPA reactivity by acting on neurons within or surrounding the PVN
  • ...9 more annotations...
  • inhibitory action of DHT is detectable at both the level of hormone secretion as well as PVN c-fos mRNA expression
  • the inhibition can be mimicked by the DHT metabolite 3β-diol and by the subtype selective ERβ agonist DPN
  • E2 acts to enhance HPA reactivity
  • the ability of the ER antagonist tamoxifen, but not the AR antagonist flutamide, to block the inhibitory actions of DHT, speaks to the intracellular mechanism by which this inhibitory signal might be transduced.
    • Nathan Goodyear
      Nathan Goodyear on 15 Jul 15
       
      that is because the interaction with the DHT metabolite is not with the AR, but with the ER-beta.
  • the DHT metabolite 3β-diol and the ERβ-subtype-selective agonist DPN suppressed ACTH, corticosterone, and c-fos mRNA responses to restraint stress in a manner similar to DHT
  • metabolism of DHT to 3β-diol and subsequent binding to ERβ can be inhibitory to HPA reactivity, and this is one possible mechanism for the action of DHT.
  • Our data also suggest that E2 enhances the reactivity of the HPA axis to stress by acting on or near neurons of the PVN
  • the actions of E2 appear to be through an ERα-dependent mechanism
  • these studies suggest that ERβ, within the male hypothalamus, acts to inhibit the HPA axis and that the inhibitory effects of DHT may be, at least in part, via its intracellular conversion to 3β-diol and subsequent binding to ERβ
  • Nathan Goodyear on 15 Jul 15
     
    DHT metabolites: particularly 3beta-androstanediol inhibit HPA axis through ER-beta.
Nathan Goodyear

Cannabinoids reduce ErbB2-driven breast cancer progression through Akt inhibition | Mol... - 0 views

molecular-cancer.biomedcentral.com/...1476-4598-9-196

Cancer "breast cancer" THC CBD "medical medical marijuana

shared by Nathan Goodyear on 12 Nov 18 - No Cached
  • Nathan Goodyear on 12 Nov 18
     
    Mouse study finds THC and CBD agonist reduce tumor growth, inhibit angiogenesis, induce apoptosis, and reduce metastasis. In addition, 91% of breast cancers in animal study expressed CB2 receptors.
Nathan Goodyear

Anticancer mechanisms of cannabinoids - 0 views

www.ncbi.nlm.nih.gov/...PMC4791144

THC cannabinoids cancer

shared by Nathan Goodyear on 18 Sep 18 - No Cached
  • modulating key cell signalling pathways involved in the control of cancer cell proliferation and survival
  • cannabinoids inhibit angiogenesis and decrease metastasis in various tumour types in laboratory animals
  • Cannabis sativa L. (marijuana)
  • ...41 more annotations...
  • of the approximately 108 cannabinoids produced by C. sativa, Δ9-tetrahydrocannabinol (thc) is the most relevant because of its high potency and abundance in plant preparations
  • Tetrahydrocannabinol exerts a wide variety of biologic effects by mimicking endogenous substances—the endocannabinoids anandamide3 and 2-arachidonoylglycerol4,5—that engage specific cell-surface cannabinoid receptors
  • the cb2 receptor was initially described to be present in the immune system6, but was more recently shown to also be expressed in cells from other origins
  • transient receptor potential cation channel subfamily V, member 1
  • orphan G protein–coupled receptor 55
  • Most of the effects produced by cannabinoids in the nervous system and in non-neural tissues rely on cb1 receptor activation
  • two major cannabinoid-specific receptors—cb1 and cb2
  • cardiovascular tone, energy metabolism, immunity, and reproduction
  • cannabinoids are well known to exert palliative effects in cancer patients
  • best-established use is the inhibition of chemotherapy-induced nausea and vomiting
  • thc and other cannabinoids exhibit antitumour effects in a wide array of animal models of cancer
  • cannabinoid receptors and their endogenous ligands are both generally upregulated in tumour tissue compared with non-tumour tissue
  • cb2 promotes her2 (human epidermal growth factor receptor 2) pro-oncogenic signalling in breast cancer
  • pharmacologic activation of cannabinoid receptors decreases tumour growth
  • endocannabinoid signalling can also have a tumour-suppressive role
  • pharmacologic stimulation of cb receptors is, in most cases, antitumourigenic. Nonetheless, a few reports have proposed a tumour-promoting effect of cannabinoids
  • most prevalent effect is the induction of cancer cell death by apoptosis and the inhibition of cancer cell proliferation
  • impair tumour angiogenesis and block invasion and metastasis
  • thc and other cannabinoids induce the apoptotic death of glioma cells by cb1- and cb2-dependent stimulation
  • Autophagy is primarily a cytoprotective mechanism, although its activation can also lead to cell death
  • autophagy is important for cannabinoid antineoplastic activity
  • autophagy is upstream of apoptosis in the mechanism of cannabinoid-induced cell death
  • the effect of cannabinoids in hormone- dependent tumours might rely, at least in part, on the ability to interfere with the activation of growth factor receptors
  • glioma cells), pharmacologic blockade of either cb1 or cb2 prevents cannabinoid-induced cell death with similar efficacy
  • other types of cancer cells (pancreatic48, breast24, or hepatic43 carcinoma cells, for example), antagonists of cb2 but not of cb1 inhibit cannabinoid antitumour actions
  • thc promotes cancer cell death in a cb1- or cb2-dependent manner (or both) at lower concentrations
  • cannabidiol (cbd), a phytocannabinoid with a low affinity for cannabinoid receptors15, and other marijuana-derived cannabinoids57 have also been proposed to promote the apoptotic death of cancer cells acting independently of the cb1 and cb2 receptors
  • In cancer cells, cannabinoids block the activation of the vascular endothelial growth factor (vegf) pathway, an inducer of angiogenesi
  • In vascular endothelial cells, cannabinoid receptor activation inhibits proliferation and migration, and induces apoptosis
  • cb1 or cb2 receptor agonists (or both) reduce the formation of distant tumour masses in animal models of both induced and spontaneous metastasis, and inhibit adhesion, migration, and invasiveness of glioma64, breast65,66, lung67,68, and cervical68 cancer cells in culture
  • the ceramide/p8–regulated pathway plays a general role in the antitumour activity of cannabinoids targeting cb1 and cb2
  • cbd, by acting independently of the cb1 and cb2 receptors, produces a remarkable anti-tumour effect—including reduction of invasiveness and metastasis
  • cannabinoids can also enhance immune system–mediated tumour surveillance in some contexts
  • ability of thc to reduce inflammation75,76, an effect that might prevent certain types of cancer
  • recent observations suggest that the combined administration of cannabinoids with other anticancer drugs acts synergistically to reduce tumour growth
  • combined administration of gemcitabine (the benchmark agent for the treatment of pancreatic cancer) and various cannabinoid agonists synergistically reduced the viability of pancreatic cancer cells
  • Other reports indicated that anandamide and HU-210 might also enhance the anticancer activity of paclitaxel89 and 5-fluorouracil90 respectively
  • Combined administration of thc and cbd enhances the anticancer activity of thc and reduces the dose of thc needed to induce its tumour growth-inhibiting activity
  • Preclinical animal models have yielded data indicating that systemic (oral or intraperitoneal) administration of cannabinoids effectively decreases tumour growth
  • Combinations of cannabinoids with classical chemotherapeutic drugs such as the alkylating agent temozolomide (the benchmark agent for the management of glioblastoma80,84) have been shown to produce a strong anticancer action in animal models
  • pharmacologic inhibition of egfr, erk83, or akt enhances the cell-death-promoting action of thc in glioma cultures (unpublished observations by the authors), which suggests that targeting egfr and the akt and erk pathways could enhance the antitumour effect of cannabinoids
  • Nathan Goodyear on 18 Sep 18
     
    Good review of the anticancer effects of cananbinoids.
Nathan Goodyear

The current state and future perspectives of cannabinoids in cancer biology - 0 views

www.ncbi.nlm.nih.gov/...PMC5852356

Cancer CBD THC cannabinoids

shared by Nathan Goodyear on 19 Sep 18 - No Cached
hoangkimchi liked it
  • The activation of each of them leads to an inhibition of adenylyl cyclase via G proteins (Gi/o), which in turn activates many metabolic pathways such as mitogen‐activated protein kinase pathway (MAPK), phosphoinositide 3‐kinase pathway (PI3K), cyclooxygenase‐2 pathway (COX‐2), accumulation of ceramide, modulation of protein kinase B (Akt), and ion channels
  • phytocannabinoids, endocannabinoids, and synthetic cannabinoids
  • Action of THC in human organism relies on mimicking endogenous agonists of CB receptors—endocannabinoids
  • ...8 more annotations...
  • The upregulated expression of CB receptors and the elevated levels of endocannabinoids have been observed in a variety of cancer cells (skin, prostate, and colon cancer, hepatocellular carcinoma, endometrial sarcoma, glioblastoma multiforme, meningioma and pituitary adenoma, Hodgkin lymphoma, chemically induced hepatocarcinoma, mantel cell lymphoma)
  • concentration of endocannabinoids, expression level of their receptors, and the enzymes involved in their metabolism frequently are associated with an aggressiveness of cancer
  • CB2 receptor contributes to human epidermal growth factor receptor (HER2) pro‐oncogenic signaling and an overexpression of CB2 increases susceptibility for leukemia development after leukemia viral infection
  • endocannabinoid‐degrading enzymes are upregulated in cancer cell lines and in human tumors
  • Many cannabinoids, ranging from phytocannabinoids (THC, CBD), endocannabinoids (2‐arachidonoylglycerol, anandamide), to synthetic cannabinoids (JWH‐133, WIN‐55,212‐2), have shown ability to inhibit proliferation, metastasis, and angiogenesis in a variety of models of cancer
  • Despite some inconsistent data, the main effect of cannabinoids in a tumor is the inhibition of cancer cells’ proliferation and induction of cancer cell death by apoptosis
  • CB1 and CB2 receptor agonists stimulate apoptotic cell death in glioma cells by induction of de novo synthesis of ceramide, sphingolipid with proapoptotic activity
  • process of autophagy is upstream of apoptosis in mechanism of cell death induced by cannabinoids
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