Activity phorbol esters. Medical search. Frequent questions

May be involved in presynaptic facilitation by mediating phorbol ester-induced synaptic potentiation. (icr.ac.uk)

ProTGF-alpha cleavage is activated in response to tumor-promoting phorbol ester or to calcium ionophore. (nih.gov)
However, plant seed oils at times contain liposoluble toxic compounds, such as tumor-promoting phorbol esters found in Jatropha curcas seed oil ( 10 ), the toxic gossypol found in crude cotton ( Gossypium hirsutum ) seed oil ( 11 ) and the encephalopathy-causing Neem seed oil ( 12 ). (iiarjournals.org)

The mechanism of activation of the transient receptor potential vanilloid 4 (TRPV4) channel by 4α-phorbol esters was investigated by combining information from chemical modification of 4α-phorbol-didecanoate (4α-PDD, 2a ), site-directed mutagenesis, Ca 2+ imaging, and electrophysiology. (acs.org)
Protein kinase C (PKC) is a phorbol ester receptor. (wikipedia.org)
Down-regulation of mannose receptor activity in macrophages after treatment with lipopolysaccharide and phorbol esters. (aai.org)
The effect of these agents on receptor activity was not reversible, and activity continued to decline after the agents were removed. (aai.org)
Serine protease inhibitors did not block the reduction in receptor activity, suggesting that proteolysis is not involved in receptor down-regulation. (aai.org)
Binding of 125I-mannose-BSA to intact macrophages showed a 70% decrease in surface receptor activity after treatment with LPS/PMA. (aai.org)
When stimulated by agonists of the histamine H1 receptor (H1R), TRPC6 activity decays to the baseline despite the continuous presence of the agonist. (mdpi.com)
In this study, we examined whether H1R desensitization contributes to regulating the decay rate of TRPC6 activity upon receptor stimulation. (mdpi.com)
In the presence of phorbol myristate acetate (PMA), an activator of PKC and analog of diacylglycerol, IGF-II receptor number increased in the plasma membrane by 60% without changes in the binding affinity. (elsevierpure.com)
The effect of PMA on IGF-II receptor recycling correlated with its stimulation of PKC activity. (elsevierpure.com)
Furthermore, after down-regulation of cellular PKC levels by preincubation with PMA, PMA was unable to activate residual PKC activity in the membranous pool or increase IGF-II receptor number at the cell surface. (elsevierpure.com)

Challenge of hepatocytes with the tumour promoting phorbol ester TPA, however, elicited a marked enhancement of the phosphorylation state of alpha-Gi. (strath.ac.uk)
Activation ofPYK2 by agents that elevate intracellular calcium or by phorbol ester inducetyrosine phosphorylation of Nirs. (embl.de)
The initial serine phosphorylation corresponded to the first phase of rapid inhibition mediated by changes in intrinsic activity and/or silencing of SERT. (aspetjournals.org)
In this study, L-selectin was found to be phosphorylated in lymphoblastoid cell lines, and phosphorylation was enhanced by phorbol ester (phorbol 12-myristate 13-acetate (PMA)) treatment. (upenn.edu)
PKCd protein levels, PKCd-Thr505 phosphorylation, and PKCd kinase activity was assessed in CAP37-treated HCECs utilizing immunohistochemistry, Western blotting, as well as a kinase activity assay, respectively. (amparinhibitor.com)

Phorbol esters (PE) are analogues of DAG and potent tumour promoters that cause a variety of physiological changes when administered to both cells and tissues. (embl-heidelberg.de)
Prostratin, a non-tumour promoting phorbol ester, exhibit a potent anti-HIV activity against human immunodeficiency virus type 1 (HIV-1). (neb.com)

These domains were first discovered as the loci of phorbol ester and diacylglycerol binding to conventional protein kinase C isozymes, which contain 2 C1 domains (C1A and C1B) in their N-terminal regulatory regions. (embl-heidelberg.de)
NMR structure of a protein kinase C-gamma phorbol-binding domain and study of protein-lipid micelle interactions. (embl-heidelberg.de)
Using the human hepatoma cell line Hep G2, we have studied a possible role of protein kinase C (PKC) activity for regulation of erythropoietin (EPO) production. (ox.ac.uk)
The antioxidant activity was in the range of IC50 = 0.49 to 2.00 mg protein/mL, flavourzyme and sequential hydrolysates showed significant ABTS radical and FRAP inhibition. (bvsalud.org)
The α-amylase inhibitory activity was highest in 3 kDa permeate of flavourzyme with IC50 values of 0.34 mg protein/mL. (bvsalud.org)
These data suggest that volatile anesthetics enhance EAAT3 activity and that protein kinase C is involved in mediating these anesthetic effects. (silverchair.com)

Phorbol esters are a class of chemical compounds found in a variety of plants, particularly in the families Euphorbiaceae and Thymelaeaceae. (wikipedia.org)

Phorbol esters can stimulate PKC in a similar way to diglycerides. (wikipedia.org)
Phorbol esters can directly stimulate PKC. (embl-heidelberg.de)

Inhibitor profile of the enzyme, including inhibition by serine protease inhibitors and no inhibition by elastatinal, coincides with that previously reported for proTGF-alpha cleavage activity on CHO cells. (nih.gov)
MMP-2 and-9 activity was decreased by exposure to inhibitors. (drrathresearch.org)
A similar reduction of ↑[Ca 2+ ] e -evoked secretion was produced by inhibitors of conventional and/or novel PKCs (Gö6976, calphostin C, and pseudoA), and these compounds did not inhibit secretion at all when applied to phorbol-downregulated cells. (jneurosci.org)
Staurosporine and 1-(5-isoquinolinylsulfonyl)-2-methylpiperazine, two structurally different inhibitors of PKC activity, inhibited basal and stimulated EPO production with ED50 values of 9 nM and 50 microM, respectively. (ox.ac.uk)
Chemotaxis research revealed that therapy with pertussis toxin, PKC inhibitors, phorbol esters, and siRNAs considerably inhibited CAP37-mediated chemotaxis compared with untreated controls. (amparinhibitor.com)

Glucose-induced activation of DAG/PKC signaling in microsomes was not associated with a change in the translocation of Glut-4 transporters from microsomes to the plasma membrane, a biological response that is known to be stimulated by agonists, e.g., phorbol esters, which increase DAG/PKC signaling in plasma membranes, as well as in microsomes. (jci.org)

The enzyme was partially purified from membranes of phorbol ester-treated CHO cells. (nih.gov)
The data also suggest that half of the domain, including the phorbol site and one of the zinc sites, is capable of inserting into membranes. (embl-heidelberg.de)
Glucose rapidly increased DAG content and PKC enzyme activity in microsomes, but not in plasma membranes or other membranes, during a 30-min treatment of rat adipocytes. (jci.org)

Confluent NCI-H292 human mucoepidermoid airways epithelial cells were pretreated with AZM or MDM for 2 h and then stimulated with 200 nmol/l phorbol 12-myristate 13-acetate (PMA) for 8 h. (karger.com)
Phorbol esters and gene expression: the role of rapid changes in K+ transport in the induction of ornithine decarboxylase by 12-O-tetradecanoylphorbol-13-acetate in BALB/c 3T3 cells and a mutant cell line defective in Na+K+Cl- cotransport. (rupress.org)
Treatment of rat platelets with β-phorbol 12-myristate 13-acetate (PMA) for 5 min or less resulted in a rapid inhibition of SERT involving changes in intrinsic activity of the transporter (increased K m and decreased V max ). (aspetjournals.org)
The phorbol ester phorbol 12-myristate-13 acetate (PMA) led to a concentration-dependent inhibition of basal and stimulated EPO formation (ED50 10 nM). (ox.ac.uk)
Responses in the presence of the combination of phorbol-12-myrisate-13-acetate and volatile anesthetics (isoflurane, halothane, or sevoflurane) were not greater than those when volatile anesthetic was present alone. (silverchair.com)

The enzyme activity was about 5-6-fold increased by exposure of the cells with phorbol ester or with calcium ionophore. (nih.gov)
This investigation evaluates the effects of mechanical deformation on in vitro osteoblasts by assessing changes in MMP gene expression and enzyme activity. (allenpress.com)

Involved in nerve growth factor (NFG)-induced neurite outgrowth and neuron morphological change independently of its kinase activity, by inhibition of RHOA pathway, activation of CDC42 and cytoskeletal rearrangement. (icr.ac.uk)
Direct activation of PKCd by CAP37 was demonstrated making use of a kinase activity assay. (amparinhibitor.com)
Insulin-stimulated glucose transport in isolated skeletal muscle was reduced 47% in obese versus lean rats, with a parallel 42% reduction in tyrosine-associated PI 3-kinase activity. (diabetesjournals.org)

We demonstrate that Nirs arecalcium-binding proteins that exhibit PI transfer activity in vivo. (embl.de)
Many C1 domains and C1 domain-containing proteins bind phorbol esters, but many others do not. (embl-heidelberg.de)

These findings suggest that the enzyme is a processing protease involved in the cleavage of proTGF-alpha and that induction of proTGF-alpha conversion by phorbol ester or by calcium ionophore can be attributed to activation of the processing protease. (nih.gov)
Is able to form a complex with PDLIM5 and N-type calcium channel, and may enhance channel activities and potentiates fast synaptic transmission by phosphorylating the pore-forming alpha subunit CACNA1B (CaV2.2). (icr.ac.uk)

PMA and TNF-α, with increased concentration, increased MMP-9 secretion, while IL-1ß and LPS did not significantly modify MMP-9 activity. (drrathresearch.org)
Only PKCγ was found to have been translocated to the membrane fraction when secretion of 5-HT was evoked by ↑[Ca 2+ ] e or phorbol esters. (jneurosci.org)
Although phorbol downregulation caused PKCγ to disappear, secretion was only partially inhibited. (jneurosci.org)
In contrast, the phorbol downregulation-resistant component of secretion was abolished by pseudoZ, which inhibits the atypical PKCζ. (jneurosci.org)

Exposure of epithelial type II cells to halothane reduced the activity of sodium, potassium-adenosine triphosphatase, and amiloride-sensitive Na channels, whereas Na cotransporters were unchanged. (asahq.org)
The decrease in sodium, potassium-adenosine triphosphatase activity was maximal for 30 min of exposure and reached 50, 42, and 56% for halothane concentrations of 1, 2, and 4%, respectively, and did not change for longer exposure times. (asahq.org)

A BALB/c 3T3 preadipose cell line defective in Na+K+Cl- cotransport (3T3-E12a cells) has been used to study the relationship between phorbol ester-induced rapid changes in cation fluxes and changes in expression of a gene known to be modulated by this agent. (rupress.org)
These results suggest that rapid changes in ion fluxes mediated by the Na+K+Cl- cotransport system are necessary for at least one of the phorbol ester-induced changes in gene expression in responsive cells. (rupress.org)
The compound K-mediated inhibition of MMP-9 gene expression appears to occur via AP-1 because its DNA-binding and transcriptional activities were suppressed by the agent. (korea.ac.kr)
During pilocarpine-induced SE, in vivo disruption of STEP activity allowed activation of the MAPK pathway, leading to immediate-early gene expression and significant rescue from cell death. (jneurosci.org)

Whereas inhibition of SERT activity was detected from 1 to 45 min after phorbol ester addition, the decrease in surface SERT required at least 30 min of phorbol ester incubation. (aspetjournals.org)
Furthermore, inhibition of ChoK shows a strong in vivo antitumor activity against human breast cancer xenografts. (aacrjournals.org)

Some bind phorbol esters and diacylglycerol. (embl-heidelberg.de)
The natural agonist, diacylglycerol (DAG), and the natural product superagonist, phorbol dibutyrate (PDB), activate the enzyme to produce wide-ranging physiological effects. (embl-heidelberg.de)

The inhibitory activity of the water-solublefraction was greatest, followed by that of the n-hexane-soluble and acetone-soluble fractions in all bioassays.Significant reductions in the germination and growth of the roots and hypocotyls were observed as the extractconcentration increased. (researchgate.net)

Like RA, these synthetic retinoids allow all three RAR types to repress AP1 (c-Jun/c-Fos) activity, demonstrating that the transactivation and transrepression functions of RARs can be dissociated by properly designed ligands. (nih.gov)
Using AP1 reporter cells, we also show that glucocorticoids or vitamin D3, together with either RA or these 'dissociating' synthetic retinoids, can synergistically repress phorbol ester-induced AP1 activity. (nih.gov)

Proteolytic activity and collagenolytic degradation of extracellular matrix at the bone-implant interface have been reported in conjunction with increased mRNA expression of metalloproteinases (MMPs) in otherwise healthy tissues. (allenpress.com)

The purpose of this study was to examine the effects of halothane on Na transport activities. (asahq.org)
Sodium, potassium-adenosine triphosphatase, and amiloride-sensitive Na channel activities are impaired by halothane in alveolar type II cells in vitro. (asahq.org)

hence, the activity probably locates on the outer surface of the cell membrane. (nih.gov)
In the cell-free reconstitution system, the membrane-bound Suc-Ala-Ala-Ala-MCA-hydrolyzing enzyme from CHO cells was also activated by phorbol ester in the presence of the soluble fraction, ATP, and vanadate. (nih.gov)
In prostate cancer cells, interacts with and phosphorylates STAT3, which increases DNA-binding and transcriptional activity of STAT3 and seems to be essential for prostate cancer cell invasion. (icr.ac.uk)

In the present study, we report that prostratin exhibits potent antiviral activity against different strains of HIV-1 (subtypes B and D), a clinical HIV isolate (L1), HIV-2 (ROD and EHO) and SIV (MAC251) with EC50-values ranging from 0.02-0.09 microg/ml. (neb.com)

Steel HC, Theron AJ, Cockeran R, Anderson R, Feldman C: Pathogen- and host-directed anti-inflammatory activities of macrolide antibiotics. (karger.com)

Induction of tyrosine hydroxylase in the locus coeruleus of transgenic mice in response to stress or nicotine treatment: lack of activation of tyrosine hydroxylase promoter activity. (rochester.edu)
The inhibitory effect of compound K on MMP-9 expression correlated with decreased MMP-9 mRNA levels and suppression of MMP-9 promoter activity. (korea.ac.kr)

however, a decrease in pH and TPC and an increase in acidity and antioxidant activity were observed (p (bvsalud.org)
In conclusion, the synbiotic supplementation of inulin in soymilk enhanced the viability of Lactobacillus paracasei CD4 and antioxidant activity during storage under refrigeration conditions. (bvsalud.org)
The release of polyphenols, their antioxidant activity and impact on microbial diversity was evaluated under long term fermentation for 21â ¯days. (bvsalud.org)
At each stage, the Total polyphenolic content (TPC), Total antioxidant activity (TAA) and polyphenolic profile was determined. (bvsalud.org)

The phorbol binding site was identified by titrating this domain with phorbol-12,13-dibutyrate (PDB) in the presence of organic cosolvents. (embl-heidelberg.de)
Titrations of this domain with lipid micelles, in the absence and presence of phorbols, indicate selective broadening of some resonances. (embl-heidelberg.de)

Taken together, our results show that 4α-phorbol is a useful template to investigate the molecular details of TRPV4 activation by small molecules and obtain information for the rational design of structurally simpler ligands for this ion channel. (acs.org)

1999. Transactivation activity of human, zebrafish, and rainbow trout aryl hydrocarbon receptors expressed in COS-7 cells: Greater insight into species differences in toxic potency of polychlorinated dibenzo- p -dioxin, dibenzofuran, and biphenyl congeners. (cdc.gov)

Thus, we propose a model where Rab40c/CRL5 regulates ANKRD28 ubiquitylation and degradation, leading to a decrease in PP6 activity, which ultimately affects FAK and Hippo pathway signaling to alter focal adhesion dynamics. (life-science-alliance.org)

Stimulation of PF cells with ↑[Ca 2+ ] e increased the activity of immunoprecipitated PKCζ (but not PKCι/λ), and the activity of this PKCζ was inhibited by pseudoZ. (jneurosci.org)

The expression and activity of mRNA for several MMPs (2, 3, 9, and 10) was assessed. (allenpress.com)

The present study aimed to screen the indigenous probiotic cultures for their effect on total phenolic contents (TPC) and associated antioxidant activities in synbiotic fermented soymilk during storage. (bvsalud.org)

As shown by time-of-addition experiments, prostratin needs to be present at the time of viral adsorption to exert its antiviral activity. (neb.com)

However, TPA failed to cause an increase in ODC activity in mutant cells, although a substantial induction of the enzyme was seen in parental cells. (rupress.org)
Although chelerythrine did not change the anesthetic effects on the activity of EAAT3, staurosporine or calphostin C abolished the anesthetic-induced increase of EAAT3 activity. (silverchair.com)

The enzyme is involved in wound healing, and studies in mice suggest that it regulates the activity of defensins in intestinal mucosa. (cancerindex.org)

The lipophilic ester groups on ring C serve mainly as a steering element, affecting the orientation of the diterpenoid core into the ligand binding pocket, while the nature of the A,B ring junction plays an essential role in the Ca 2+ -dependence of the TRPV4 response. (acs.org)
Isoform-specific AMPK activity was measured in skeletal muscle in response to insulin, contraction, or hypoxia. (diabetesjournals.org)

Binding of 4α-phorbol esters occurs in a loop in the TM3−TM4 domain of TRPV4 that is analogous to the capsaicin binding site of TRPV1, and the ester decoration of ring C and the A,B ring junction are critical for activity. (acs.org)
Twenty-eight other domains fit the profile for the overall C1 domain fold but do not fit the profile for phorbol ester binding, and are termed "atypical. (embl-heidelberg.de)
Interacts (via phorbol-ester/DAG-type 2 domain) with PRPH and VIM (PubMed:18408015). (icr.ac.uk)

Twenty-six C1 domains fit the profile for phorbol-ester binding and are termed "typical. (embl-heidelberg.de)

The sequential hydrolysis demonstrated antimicrobial activity against all pathogens used with 3 kDa permeate showed significantly higher (p (bvsalud.org)

Anatomy30

Organisms6

Diseases4

Chemicals and Drugs158

Analytical, Diagnostic and Therapeutic Techniques and Equipment12

Phenomena and Processes43

Information Science3

Mediating phorbol ester-induced1

Tumor-promoti2

Receptor11

Phosphorylation5

Tumour2

Protein6

Chemical compounds1

Stimulate2

Inhibitors5

Agonists1

Membranes3

Acetate5

Enzyme activity2

Kinase activity3

Proteins2

Calcium2

Secretion4

Exposure2

Gene4

Inhibition2

Diacylglycerol2

Inhibitory activity1

Synthetic2

Extracellular matrix1

Halothane2

Cell3

Potent1

Anti-inflammatory1

Promoter activity2

Antioxidant activity4

Presence2

Molecular1

Transactivation1

Decrease1

Stimulation1

MMPs1

Study1

Antiviral1

Increase2

Regulates1

Response2

Domain3

Profile1

Significantly1