Sunitinib is a tyrosine kinase inhibitor approved for the treatment of multiple solid tumors. (nih.gov)
My laboratory is focused on understanding mechanisms of resistance to molecular targeting agents directed against receptor tyrosine kinases. (wisc.edu)
Monoclonal antibody therapy has been developed over the past 30 years to target receptor tyrosine kinases (RTKs), which sit on the outer membrane of cancerous cells. (wisc.edu)
BackgroundPazopanib is the only tyrosine kinase inhibitor approved for the treatment of patients with advanced soft tissue sarcoma (STS) who have received prior chemotherapy, but there have been limited real-world data on pazopanib for the treatment of advanced STS.ObjectiveWe aimed to evaluate. (sagepub.com)
Although its pyrrolidine-based structure suggests that it is derived from proline, the results from the experiments indicated that tyrosine, glycine, methionine, and acetate are the primary precursors for the biosynthesis of anisomycin. (wikipedia.org)
Phosphorylation6
On the other hand, it readily stimulated the phosphorylation of mitogen-activated protein (MAP) kinases extracellular signal-regulated kinase (ERK) and c-Jun N-terminal kinase (JNK) via a protein kinase C-dependent mechanism. (ac.rs)
We have discovered that E2F1 localizes to sites of both DNA double-strand breaks and UV-induced DNA damage and that this involves the phosphorylation of E2F1 by the ATM or ATR kinases. (mdanderson.org)
In addition, adlay bran reduced the intracellular production of reactive oxygen species, inhibited the phosphorylation of Akt and decreased the expression of protein kinase C. Furthermore, six phenolic acids and one flavone were isolated. (greenmedinfo.com)
Increases phosphorylation of protein kinases in, and migration of, human umbilical vein endothelial cells. (tocris.com)
Its activation results in the formation of inositol 1,4,5-trisphosphate, the mobilization of intracellular calcium, the phosphorylation of the MAPK3/ERK1 and MAPK1/ERK2 kinases and the inhibition of intracellular cAMP accumulation. (nih.gov)
Phosphorylation and thereby activation of the kinases p44/42 and Akt, which are involved in proliferation and survival processes, were inhibited, the mitochondrial membrane potential of the GBM cells was altered, and genes involved in dormancy-associated processes were regulated by the combined treatment strategy. (biofron.com)
Extracellular1
Woolson, H. D. , Thomson, V. S. , Rutherford, C. , Yarwood, S. J. and Palmer, T. M. (2009) Selective inhibition of cytokine-activated extracellular signal-regulated kinase by cyclic amp via Epac1-dependent induction of suppressor of cytokine signalling-3. (gla.ac.uk)
Activator phorbol2
We investigated the mechanisms and the role of autophagy in the differentiation of HL-60 human acute myeloid leukemia cells induced by protein kinase C (PKC) activator phorbol myristate acetate (PMA). (ac.rs)
Here we demonstrate that elevation of cyclic AMP (cAMP) levels in human umbilical vein endothelial cells (HUVECs) specifically attenuates ERK1,2 activation in response to either leptin or a soluble interleukin IL-6 receptor-α/IL-6 (sIL-6R-α/IL-6) trans-signalling complex but not protein kinase C activator phorbol 12-myristate 13-acetate. (gla.ac.uk)
Inhibition2
The inhibitory effect of cAMP could not be reversed by inhibition of cAMP-dependent protein kinase (PKA) but was blocked by depletion of the alternative intracellular cAMP sensor exchange protein activated by cAMP 1 (Epac1), which is also required to observe SOCS-3 accumulation in response to cAMP. (gla.ac.uk)
Morphological rescue is possible following Rho kinase inhibition in an oligodendrocyte subset. (jneurosci.org)
Mandic M, Misirkic Marjanovic M, Vucicevic L, Jovanovic M, Bosnjak M, Perovic V, Ristic B, Ciric D, Harhaji-Trajkovic L, Trajkovic V. MAP kinase-dependent autophagy controls phorbol myristate acetate-induced macrophage differentiation of HL-60 leukemia cells. (ac.rs)
Stimulation of cardiomyocytes with 4 beta-phorbol 12-myristate 13-acetate (PMA) led to a rapid increase in particulate-bound PKC activity, a response attributed to the activation of alpha-, delta- and zeta- type PKCs but not beta-type PKC. (unige.ch)
Associates with EGR1 and SP1 to mediate tetradecanoyl phorbol acetate (TPA)-induced up-regulation of CDKN2B, possibly by binding to the CDKN2B promoter region 5'-TCACA-3. (nih.gov)
Inhibitory effects1
The present study investigated the inhibitory effects of gossypol acetate on rat 5α-reductase 1, 3α-hydroxysteroid dehydrogenase, and retinol dehydrogenase 2 for androgen metabolism. (biofron.com)
Ethyl acetate1
A 40.8μg/mL concentration of the ethyl acetate fraction of the ethanolic extracts of adlay bran (ABE-EtOAc) effectively inhibited mast cell degranulation. (greenmedinfo.com)
Autophagy2
PMA failed to activate autophagy inducer AMP-activated protein kinase (AMPK) and inhibit autophagy suppressor mechanistic target of rapamycin complex 1 (mTORC1). (ac.rs)
Therefore, MAP kinases ERK and JNK control PMA-induced macrophage differentiation of HL-60 leukemia cells through AMPK/mTORC1-independent, TFEB/FOXO-mediated transcriptional and beclin-1-dependent post-translational activation of autophagy. (ac.rs)
Phosphate3
In enzymology, an acetate kinase (diphosphate) (EC 2.7.2.12) is an enzyme that catalyzes the chemical reaction diphosphate + acetate ⇌ {\displaystyle \rightleftharpoons } phosphate + acetyl phosphate Thus, the two substrates of this enzyme are diphosphate and acetate, whereas its two products are phosphate and acetyl phosphate. (wikipedia.org)
Comment: Glycine can be reduced to acetyl phosphate by glycine reductase (EC 1.21.4.2 ), and then converted to acetate (by ackA in reverse) or acetyl-CoA (by pta) Or glycine can cleaved to ammonia, CO2, and 5,10-methylene-tetrahydrofolate by the glycine cleavage system, gcvPTH/lpd. (lbl.gov)
Comment: Acetaldehyde can be oxidized to acetyl-CoA, or oxidized to acetate and activated to acetyl-CoA by either acetyl-CoA synthetase (acs) or by acetate kinase (ackA) and phosphate acetyltransferase (pta). (lbl.gov)
Glycine1
Glycine or acetate account for C-4 and C-5 on the pyrrolidine ring. (wikipedia.org)
Genome1
CSL is an download Your Brain on Latino Comics: From Gus Arriola to Los Bros Hernandez of a possible DNA-binding histone cause that releases kinase of invalid genome interests in one decision, but hormone of the Canadian developments in another endocytosis. (evakoch.com)
Inhibitors1
Comert Onder F, Siyah P, Durdagi S, Ay M, Ozpolat B . Novel etodolac derivatives as eukaryotic elongation factor 2 kinase (eEF2K) inhibitors for targeted cancer therapy. (viictr.org)
Intracellular1
Stimulation of acid secretion typically involves an initial elevation of intracellular calcium and cAMP, followed by activation of protein kinase cascades, which trigger the translocation of the proton pump, H+,K+-ATPase, from cytoplasmic tubulovesicles to the apical plasma membrane and thereby H+ secretion into the stomach lumen. (genome.jp)
Receptor1
Ozyurt R, Ozpolat B . Therapeutic Landscape of AXL Receptor Kinase in Triple-Negative Breast Cancer. (viictr.org)
Peripheral1
In order to examine the role of NFkappabeta in the pathophysiology of CFS, this study examines the production of NFkappabeta p50 in unstimulated, 10 ng/mL TNF-alpha (tumor necrosis factor alpha) and 50 ng/mL PMA (phorbolmyristate acetate) stimulated peripheral blood lymphocy tes of 18 unmedicated patients with CFS and 18 age-sex matched controls. (nel.edu)
Preparations1
The potency and mode of action of gossypol acetate to inhibit these enzymes in both enzyme-expressed preparations and immature Leydig cells were examined. (biofron.com)
Activate1
[2] Anisomycin can activate stress-activated protein kinases , MAP kinase and other signal transduction pathways. (wikipedia.org)
Structural1
Integrin-linked kinase (ILK) is a major structural adaptor protein governing signaling complex formation and cytoskeletal dynamics. (jneurosci.org)
Effects1
The expression of protein kinase C (PKC) isoenzymes and the effects of PKC activation on myocardial phospholipase A2 (PLA2) activity, platelet-activating factor (PAF) generation and eicosanoid release were studied in spontaneously beating cultured rat cardiomyocytes. (unige.ch)
Primarily1
In omnivorous mammals, the short chain fatty acids acetate, propionate and butyrate are produced primarily by the gut microbiome that metabolizes dietary fibers. (nih.gov)
Cells1
Gossypol acetate inhibited 5α-reductase 1 and 3α-hydroxysteroid dehydrogenase with IC50 values of 3.33 ± 0.07 and 0.52 ± 0.06 × 10-6 M in the expressed enzymes as well as 8.512 ± 0.079 and 1.032 ± 0.068 × 10-6 M in intact rat immature Leydig cells, respectively. (biofron.com)
Activity2
http://www.thefreedictionary.com/ "Multiple_Dictionaries", PMID:22654893] [Term] id: XCO:0000001 name: activity def: "The state of being involved in some action, either physical or mental. (mcw.edu)
GlcDEF from E. coli (EC 1.1.99.14 ) is usually described as glycolate dehydrogenase or glycolate oxidase, but it has similar activity on D-lactate ( PMID:4557653 ), and homologs from various Proteobacteria are important for D-lactate utilization. (lbl.gov)
Treatment1
11C]Acetate-PET showed decreased myocardial perfusion following treatment. (nih.gov)
Article1
Total count of NCBI Gene Reference Into Function hits for target listed in parenthesis, and summary table with links to publications per PMID with the specific text in article that includes the reported target. (nih.gov)
Forms1
Or, after L-lactate oxidase (lctO) forms acetate, the acetate is activated to acetyl-CoA. (lbl.gov)