Category
- PI3K/Akt/mTOR
- Epigenetics
- Methylation
- Immunology & Inflammation
- Protein Tyrosine Kinase
- Angiogenesis
- Apoptosis
- Autophagy
- ER stress & UPR
- JAK/STAT
- MAPK
- Cytoskeletal Signaling
- Cell Cycle
- TGF-beta/Smad
- DNA Damage
- Stem Cells & Wnt
- Ubiquitin
- Neuronal Signaling
- NF-κB
- GPCR & G Protein
- Endocrinology & Hormones
- Transmembrane Transporters
- Metabolism
- Proteases
- Microbiology
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Archives
Endocrinology & Hormones
A novel antiandrogen, Compound 30, suppresses castration-resistant and MDV3100-resistant prostate cancer growth in vitro and in vivo
8 | Jul 15 2019
Kuruma H et al. provided a preclinical proof-of-principle that Compound 30 could be a promising next generation anti-AR agent, especially in the context of antiandrogen-resistant tumors. [Read the Full Post]
Tamoxifen a pioneering drug: An update on the therapeutic potential of tamoxifen derivatives
61 | May 21 2019
Shagufta et al. anticipated that it will assist medicinal chemists in the synthesis of novel and pharmacologically potent agents for various therapeutic targets. [Read the Full Post]
Functional and Mechanistic Interrogation of BET Bromodomain Degraders for the Treatment of Metastatic Castration Resistant Prostate Cancer
55 | Mar 30 2019
Kregel S et al. identified increases in polyunsaturated fatty acids (PUFAs) and Thioredoxin-interacting protein (TXNIP) as potential pharmacodynamics biomarkers for targeting BET proteins. [Read the Full Post]
Effects of Combination of Estradiol with Selective Progesterone Receptor Modulators (SPRMs) on Human Breast Cancer Cells In Vitro and In Vivo
50 | Mar 27 2019
Nair HB et al. hypothesized that a combination of estradiol (E2) with selective progesterone receptor modulator (SPRM) to exert a safer profile on endometrium will also reduce mammary gland proliferation and could be used to prevent breast cancer when used in MHT. [Read the Full Post]
Ultraviolet A eye irradiation ameliorates colon carcinoma induced by azoxymethane and dextran sodium sulfate through β-endorphin and methionine-enkephalin
0 | Mar 16 2019
Hiramoto K et al. suggested that UVA eye irradiation exerts major effects on AOM + DSS-induced colon carcinoma. [Read the Full Post]
ΔNp63 drives metastasis in breast cancer cells via PI3K/CD44v6 axis
77 | Feb 28 2019
Di Franco S et al. found that tumor microenvironmental cytokines significantly contribute to the establishment of breast cancer cell phenotype by positively regulating ΔNp63 and CD44v6 expression. [Read the Full Post]
Role of connexin 43 in cadmium-induced proliferation of human prostate epithelial cells
96 | Jan 26 2019
Liu Q et al. found that Cx43 might be a target for prostatic diseases associated with Cd exposure. [Read the Full Post]
Ultraviolet A eye irradiation ameliorates colon carcinoma induced by azoxymethane and dextran sodium sulfate through β-endorphin and methionine-enkephalin
189 | Jan 25 2019
Hiramoto K et al. suggested that UVA eye irradiation exerts major effects on AOM + DSS-induced colon carcinoma. [Read the Full Post]
Long-term treatment of spontaneously hypertensive rats with PD123319 and electrophysiological remodeling of left ventricular myocardium
89 | Jan 20 2019
Ying X et al. showed that long-term treatment with PD123319 worsened the development of myocyte hypertrophy and associated electrophysiological alterations in spontaneously hypertensive rat. [Read the Full Post]
Impacts of ABCB1 (G1199A) polymorphism on resistance, uptake, and efflux to steroid drugs
0 | Jan 13 2019
Peng R et al. showed the ABCB1 (G1199A) polymorphism may affect effective steroids concentration in target cells by regulating the drug transport and distribution. [Read the Full Post]
Cell-based assay system for high-throughput screening of anti-photo-aging agents in fibroblast transfectants
0 | Jan 03 2019
Lee S et al. indicated sclareol attenuated UVB-induced photo-aging by an increase in collagen synthesis and decrease in MMP-1 activity. [Read the Full Post]
Tracking gastrointestinal transit of solids in aged rats as pharmacological models of chronic dysmotility
0 | Dec 28 2018
Dalziel JE et al. demonstrated that loperamide slowed overall transit in aged rats, while prucalopride increased stomach emptying and accelerates colonic transit. [Read the Full Post]
Kaempferol suppresses lipid accumulation by inhibiting early adipogenesis in 3T3-L1 cells and zebrafish
339 | Sep 16 2018
Lee YJ et al. indicated that kaempferol might have an anti-obesity effect by regulating lipid metabolism. [Read the Full Post]
The Effects of Ultraviolet Eye Irradiation on Dextran Sodium Sulfate-Induced Ulcerative Colitis in Mice
479 | Sep 15 2018
Hiramoto K et al. suggested that UV eye irradiation plays an important role in DSS-induced ulcerative colitis. [Read the Full Post]
Robust and stimuli-responsive POSS hybrid PDMAEMA hydrogels for controlled drug release
225 | Aug 30 2018
Chen Y, et al. showed that the increased Oa-POSS could improve the drug loading ability, and OP-PD gels showed well controlled-release effect in simulated human stomachic condition. [Read the Full Post]
A simple, fast, label-free colorimetric method for detection of telomerase activity in urine by using hemin-graphene conjugates
387 | Aug 29 2018
Xu X, et al. found a colorimetric approach affords simplicity, sensitivity and reliability in telomerase activity detection. [Read the Full Post]
Central Agonism of GPR120 Acutely Inhibits Food Intake and Food Reward and Chronically Suppresses Anxiety-Like Behavior in Mice
246 | Aug 23 2018
Auguste S et al. suggested that GPR120 could mediate the effects of central ω-3 polyunsaturated fatty acids to inhibit appetite. The anxiolytic effect elicited by GPR120 agonist infusions favors the testing of compounds that can enter the brain to activate GPR120 for the mitigation of anxiety. [Read the Full Post]
Acquired CDK6 amplification promotes breast cancer resistance to CDK4/6 inhibitors and loss of ER signaling and dependence
0 | Aug 14 2018
Yang C et al. suggested that the clinical paradigm of sequential endocrine-based therapy may be ineffective in some settings of acquired CDK4/6 resistance. [Read the Full Post]
Inhibition of local estrogen synthesis in the hippocampus impairs hippocampal memory consolidation in ovariectomized female mice
0 | Jun 25 2018
Tuscher JJ et al. examined the role of hippocampal E2 synthesis in hippocampal memory consolidation. Using bilateral dorsal hippocampal infusions of the aromatase inhibitor letrozole, we first found that blockade of dorsal hippocampal E2 synthesis impaired hippocampal memory consolidation. We next found that elevated levels of E2 in the dorsal hippocampus observed 30min after object training were blocked by dorsal hippocampal infusion of letrozole, suggesting that behavioral experience increases acute and local E2 synthesis. Finally, aromatase inhibition did not prevent exogenous E2 from enhancing hippocampal memory consolidation, indicating that hippocampal E2 synthesis is not necessary for exogenous E2 to enhance hippocampal memory. Combined, these data are consistent with the hypothesis that hippocampally-synthesized E2 is necessary for hippocampus-dependent memory consolidation in rodents. [Read the Full Post]
Estrogen promotes the brain metastatic colonization of triple negative breast cancer cells via an astrocyte-mediated paracrine mechanism
339 | Jun 24 2018
Sartorius CA et al. provided a novel mechanism by which estrogens, acting through ER+ astrocytes in the brain microenvironment, can promote BM of TN breast cancers, and suggests existing endocrine agents may provide some clinical benefit towards reducing and managing BM. [Read the Full Post]
Letrozole-induced functional changes in carcinoma-associated fibroblasts and their influence on breast cancer cell biology
371 | Jun 24 2018
Li K et al. revealed that down-regulation of several secreted factors (CCL2, CCL5, CXCL1 etc.) in CAFs might be partially responsible for the efficacy of letrozole. [Read the Full Post]
A Novel TGR5 Activator WB403 Promotes GLP-1 Secretion and Preserves Pancreatic β-Cells in Type 2 Diabetic Mice
481 | Mar 30 2018
Zheng C et al. demonstrated that TGR5 activator WB403 effectively promoted GLP-1 release, improved hyperglycemia and preserved the mass and function of pancreatic β-cells, whereas it did not show a significant side effect on gallbladder. [Read the Full Post]
The Correlation Between PARP1 and BRCA1 in AR Positive Triple-negative Breast Cancer
327 | Feb 26 2018
Luo J et al. suggested that the combination of bicalutamide and PARP inhibitor may be a potential strategy for TNBC patients and merits further evaluation. [Read the Full Post]
The Correlation Between PARP1 and BRCA1 in AR Positive Triple-negative Breast Cancer
0 | Feb 26 2018
Luo J et al. suggested that the combination of bicalutamide and PARP inhibitor may be a potential strategy for TNBC patients and merits further evaluation. [Read the Full Post]
Role of protein S in castration-resistant prostate cancer-like cells
364 | Feb 25 2018
Ning P et al. suggested that PROS may facilitate cell proliferation and promote castration resistance in human castration-resistant PCa-like cells via its apoptosis-regulating property. Future study emphasizing on delineating how PROS regulate cellular processes controlling transformation during the development of castration resistance should open new doors for the development of novel therapeutic targets for CRPC. [Read the Full Post]
CX4945 suppresses the growth of castration-resistant prostate cancer cells by reducing AR-V7 expression
416 | Feb 25 2018
Deng C et al. presented a potential option for the treatment of prostate cancer, especially CRPC. [Read the Full Post]
Triggering of Suicidal Erythrocyte Death by Exemestane
370 | Feb 20 2018
Exemestane triggers phospholipid scrambling of the erythrocyte cell membrane, an effect paralleled by enhanced [Ca2+]i, oxidative stress, and increased ceramide abundance. [Read the Full Post]
Androgen-Sensitized Apoptosis of HPr-1AR Human Prostate Epithelial Cells
0 | Jan 31 2018
Chen C et al. proposed that the net effect of these AR-mediated expression changes shifts the balance of BCL2-family proteins, such that androgen signaling sensitizes mitochondria to apoptotic signaling, thus rendering HPr-1AR more vulnerable to cell death signals. [Read the Full Post]
Tumor suppressor SPOP mediates the proteasomal degradation of progesterone receptors (PRs) in breast cancer cells
599 | Sep 20 2017
Gao K et al. revealed novel molecular mechanisms underlying the regulation of PR protein homeostasis in breast cancer cells, and provided insights in understanding the relationship between SPOP inactivation and the development of breast cancer. [Read the Full Post]
New insights into estrogenic regulation of O6-methylguanine DNA-methyltransferase (MGMT) in human breast cancer cells: Co-degradation of ER-α and MGMT proteins by fulvestrant or O6-benzylguanine indicates fresh avenues for therapy
0 | Sep 19 2017
Paranjpe A et al. offered a clear rationale for combining alkylating agents with endocrine therapy. [Read the Full Post]
Koumine enhances spinal cord 3α-hydroxysteroid oxidoreductase expression and activity in a rat model of neuropathic pain
1302 | Sep 19 2017
Qiu HQ et al. demonstrated that 3α-HSOR is an important molecular target of koumine for alleviating neuropathic pain. Koumine may prove a promising compound for the development of novel analgesic agents effective against intractable neuropathic pain. [Read the Full Post]
Acquired CDK6 amplification promotes breast cancer resistance to CDK4/6 inhibitors and loss of ER signaling and dependence
979 | Aug 02 2017
Yang C et al. suggested that the clinical paradigm of sequential endocrine-based therapy may be ineffective in some settings of acquired CDK4/6 resistance [Read the Full Post]
Src Is a Potential Therapeutic Target in Endocrine-Resistant Breast Cancer Exhibiting Low Estrogen Receptor-Mediated Transactivation
0 | Jul 21 2017
Guest SK et al. suggested that src has differential effects in endocrine-resistant cell lines, particularly in tamoxifen resistant models, with low ER genomic activity, providing further evidence of the importance of patient selection for clinical trials testing dasatinib utility in ER+ breast cancer. [Read the Full Post]
New insights into estrogenic regulation of O6-methylguanine DNA-methyltransferase (MGMT) in human breast cancer cells: Co-degradation of ER-α and MGMT proteins by fulvestrant or O6-benzylguanine indicates fresh avenues for therapy
656 | Jun 29 2017
Paranjpe A et al. concluded that MGMT and ER-α proteins exist as a complex and are co-targeted for ubiquitin-conjugation and subsequent proteasomal degradation. The findings offer a clear rationale for combining alkylating agents with endocrine therapy. [Read the Full Post]
The gender differences in the inhibitory action of UVB-induced melanocyte activation by the administration of tranexamic acid
0 | Jun 04 2017
Hiramoto K et al. suggested that the suppression by tranexamic acid of the UVB-induced melanocyte activation (UVB sensitivity) is stronger in female mice than in male mice and that female hormones and β-endorphin play an important role in this sex difference. [Read the Full Post]
Regulated expression of the prostacyclin receptor (IP) gene by androgens within the vasculature: Combined role for androgens and serum cholesterol.
872 | May 26 2017
Eivers SB et al. found that the human IP gene is under the transcriptional regulation of DHT, where this regulation is further influenced by serum-cholesterol levels. [Read the Full Post]
Inhibition of local estrogen synthesis in the hippocampus impairs hippocampal memory consolidation in ovariectomized female mice
868 | May 20 2017
Tuscher JJ et al. found that hippocampally-synthesized E2 is necessary for hippocampus-dependent memory consolidation in rodents. [Read the Full Post]
The gender differences in the inhibitory action of UVB-induced melanocyte activation by the administration of tranexamic acid
0 | Mar 28 2017
Hiramoto K et al suggested that the suppression by tranexamic acid of the UVB-induced melanocyte activation (UVB sensitivity) is stronger in female mice than in male mice and that female hormones and β-endorphin play an important role in this sex difference. [Read the Full Post]
GRP78 confers the resistance to 5-FU by activating the c-Src/LSF/TS Axis in hepatocellular carcinoma
0 | Mar 10 2017
Gu YJ et al found that GRP78 confers the resistance to 5-FU by up-regulating the c-Src/LSF/TS axis via its ATPase domain [Read the Full Post]
The gender differences in the inhibitory action of UVB-induced melanocyte activation by the administration of tranexamic acid.
2156 | Feb 01 2017
Hiramoto K et al. suggested that the suppression by tranexamic acid of the UVB-induced melanocyte activation (UVB sensitivity) is stronger in female mice than in male mice and that female hormones and β-endorphin play an important role in this sex difference. [Read the Full Post]
Src Is a Potential Therapeutic Target in Endocrine-Resistant Breast Cancer Exhibiting Low Estrogen Receptor-Mediated Transactivation
1897 | Dec 16 2016
Guest SK, et al. suggested that src has differential effects in endocrine-resistant cell lines, particularly in tamoxifen resistant models, with low ER genomic activity, providing further evidence of the importance of patient selection for clinical trials testing dasatinib utility in ER+ breast cancer. [Read the Full Post]
Androgen-Sensitized Apoptosis of HPr-1AR Human Prostate Epithelial Cells
1258 | Nov 13 2016
The study of Chen C et al. offers insight into AR-mediated regulation of prostate epithelial cell death signaling. [Read the Full Post]
Inhibition of local estrogen synthesis in the hippocampus impairs hippocampal memory consolidation in ovariectomized female mice
1281 | Oct 18 2016
Tuscher JJ et al. found that hippocampally-synthesized E2 is necessary for hippocampus-dependent memory consolidation in rodents. [Read the Full Post]
TAK 875 was dissolved in dimethyl sulfoxide
2343 | Feb 12 2014
AK-875 is a selective GPR40 agonist with EC50 of 14 nM, 400-fold more potent than oleic acid. [Read the Full Post]
EPZ005687 is the catalytic subunit of the polycomb repressive complex 2
2347 | Dec 06 2013
EPZ005687 is a potent and selective inhibitor of EZH2 with Ki of 24 nM, 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases. [Read the Full Post]
MS275 is a benzamide histone deacetylase inhibitor
2446 | Aug 08 2013
MS-275 shows inhibitory to HDACs by 2'-amino group. MS-275 induces accumulation of p21WAF1/CIP1 and gelsolin in K562 cell. MS-275 could reduce S-phase cells and induce G1-phase cells in A2780 cell. [Read the Full Post]
TOK001 is an experimental drug being developed by Tokai Pharmaceuticals
2310 | Jul 16 2013
Galeterone is effective at preventing binding of [3H]-R1881 to the mutant LNCaP AR (T877A) with IC50 of 845 nM. [Read the Full Post]
RG108 is a cell permeable specific DNA methyltransferase inhibitor
2618 | Jul 05 2013
RG108 effectively blocks DNA methyltransferases in vitro and does not cause covalent enzyme trapping in human cell lines. Incubation of cells with low micromolar concentrations of RG108 results in significant demethylation of genomic DNA without any detectable toxicity. [Read the Full Post]
MDV3100- AN ANTI PROSTATE CANCER AGENT
2200 | Apr 09 2012
ROLE OF ANDROGEN RECEPTORS Androgen receptors (ARs), a type of nuclear receptors that are involved in the regulation of expression of different types of genes that play role in the development and progress of male sexual characteristics. ARs can also be called as receptor subfamily number 3, C group, and member number 4 (NR3C4nuclear). Dihydrotestosterone or testosterone and androgenic hormones function as ligands for these receptors and are in turn translocated into the nucleus, where they directly or indirectly regulate the respective gene expression. Higher quantities of progestin inhibit these receptors. These receptors are known to effect many different types of genes and their expression e.g., AKT1, Cyclin D1, HDAC1, BRCA1, STAT3, SRC kinases and EGFR etc. they all are mostly cell cycle regulating proteins or oncoproteins which are malfunctioning in many different types of cancers. [Read the Full Post]
OSTARINE
3614 | Apr 05 2012
MODULATORS OF ANDROGEN RECEPTORS: Androgenic compounds are famous for their uses in banned drugs for sportsmen but very few people have knowledge to link these compounds for therapeutic purposes. Although androgen receptor modulators have restricted legitimate uses compared to anabolic steroids, many of these are undergoing clinical trials, these Selective androgen receptor modulators (SARMs) proved to be far more specific in their activities as well. The increases in knowledge about these modulators lead to the assessment in preclinical and clinical studies against different diseases. The structural diversity has been increased dramatically due to more application of SARMs for various modifying levels of androgen. The ability of SARMs as therapeutics is reported to enhance by anabolic dissociation and androgenic activities. In elder age the muscle wasting is being cured by using SARMs therefore their uses at a larger scale lead to the better drug design. Receptors of androgen are altered in a pleiotropic way in order to produce promising drugs against ageing, andropause, hypogonadism, muscle wasting, sarcopenia and osteoporosis. Keeping in mind this potential, these SARMs are becoming famous as potent and novel therapeutics. [Read the Full Post]
