Sentences with phrase «kinase inhibition»

Rb and E2F remain bound together as a result of cyclin dependent kinase inhibition.

Thus, Rho - kinase inhibition at low oxygen tension can be regarded as a potential way to enhance extracellular matrix production and maintain a chondrocyte phenotype in cell - based tissue engineering applications.

Interestingly, Rho kinase inhibition under hypoxic conditions produced a more effective increase in chondrocyte - specific gene expression and synthesis of extracellular matrix components by HCS - 2 / 8 cells.

Special focus is placed on Rho - kinase inhibition, relating to its potential to promote and support extracellular matrix production in cultured chondrocytes and its role in fibroblast cells as a part of direct chemical cellular differentiation.

«Kinase inhibition has been a watershed for cancer treatment,» said Gustafson, who attended SDSU as an undergraduate before earning his Ph.D. in organic chemistry from Yale University, then working there as a National Institutes of Health poctdoctoral fellow in chemical biology.

The Rho - kinase inhibition stimuli under low oxygen conditions (of 5 percent oxygen atmosphere), which is a condition corresponding to conditions in the body's cartilage, produced a more effective increase in chondrocyte - specific gene expression and synthesis of extracellular matrix components by HCS - 2 / 8 cells.

In his research, Juha Piltti has focused on a small molecule, which causes Rho - kinase inhibition and regulation of specific down - stream protein pathways involved in many physiological processes.

The research has also investigated the role of Rho - kinase inhibition on cellular - scale protein expression and stimulation of cellular differentiation of fibroblast cells.

According to the researcher, further studies are warranted to confirm responses in primary cells and to reveal whether Rho - kinase inhibition stimuli can be used to manufacture a better cartilage - type of tissue in laboratory.

Not exact matches

The results showed that, when applied, a long - term inhibition of Rho - kinase signaling increased the expressions of chondrocyte - specific genes and differentiation markers in human chondrosarcoma 2/8 cells.

In this pathway, dopamine - and an adenosine 3 ′, 5 ′ - monophosphate (cAMP)-- regulated phospho - protein of 32 kilodaltons (DARPP - 32) is phosphorylated or dephosphorylated at three sites, in a pattern predicted to cause a synergistic inhibition of protein phosphatase — 1 and concomitant regulation of its downstream effector proteins glycogen synthesis kinase — 3 (GSK - 3), cAMP response element — binding protein (CREB), and c - Fos.

DDRs inhibition with a tyrosine kinase inhibitor appears to insulate the brain via blood - brain barrier repair, which prevents harmful immune cells that circulate in the body from getting into the brain where they can indiscriminately attack and kill healthy and sick neurons, like those that have been unable to perform autophagy to «take out their trash,» says Moussa.

They found that inhibition of one component of DNA damage response machinery, a protein called DNAPK - kinase, increased the occurrence of translocations almost 10-fold.

They will know that compound X inhibits kinases A, B and C, but compound Z inhibits kinases D and E. With such a big data set people can easily find compounds of particular interest to them and know that the compounds are annotated with near full - kinome inhibition data.»

A short - term inhibition of Rho - kinase failed to induce extracellular matrix production in fibroblasts or in HCS - 2 / 8 cells, while its long - term exposure increased the expressions of chondrocyte - specific genes and differentiation markers, and also promoted the synthesis of sulfated glycosaminoglycans by chondrocytic cells.

The protein encoded by the PIK3C2G gene belongs to the phosphatidylinositol -4,5-bisphosphonate 3 - kinase (PI3K) family, which plays a critical role in cancer.28 Experimental evidence suggests that activation of PI3K signaling enhances production of COX - 2 and PGE2, which results in inhibition of apoptosis in colon cancer cell lines that can be restored with NSAID - mediated blockade of PI3K.29

A randoMized phAse II trIal of fulvestraNt wiTh or without Ribociclib After progression on AntI-estrogeN therapy plus cyclin - dependent kinase 4/6 inhibition in patients with unresectable or metastatic hormone receptor positive, HER2 negative breast cancer (MAINTAIN Trial)

Growth inhibition induced by antiprogestins RU - 38486, ORG - 31710, and CDB - 2914 in ovarian cancer cells involves inhibition of cyclin dependent kinase 2.

Neuronal apoptosis induced by selective inhibition of Rac GTPase versus global suppression of Rho family GTPases is mediated by alterations in distinct mitogen - activated protein kinase signaling cascades.

Glennie et al 134 have shown that T cells stimulated in co-cultures with MSC exhibit an extensive inhibition of cyclin D2 and upregulation of the cyclin dependent kinase inhibitor p27kip1.

Another focus was the differential sensitivity of different mutations towards inhibition with specific tyrosine kinase inhibitors (5).

Cellular entry of human papillomavirus type 16 involves activation of the phosphatidylinositol 3 - kinase / Akt / mTOR pathway and inhibition of autophagy.

Reciptrocal regulation of beta - adrenergic receptor mRNA stability by mitogen activated protein kinase activation and inhibition.

Inhibition of Myosin Light - Chain Kinase Attenuates Cerebral Edema after Traumatic Brain Injury in Postnatal Mice.

Rho family GTPase inhibition reveals opposing effects of mitogen - activated protein kinase kinase / extracellular signal - regulated kinase and Janus kinase / signal transducer and activator of transcription signaling cascades on neuronal survival.

T cells deficient in diacylglycerol kinase zeta are resistant to PD - 1 inhibition and help create persistent host immunity to leukemia.

Inhibition of c - Abl with STI571 attenuates stress - activated protein kinase activation and apoptosis in the cellular response to 1 - β - d - arabinofuranosylcytosine.

Title: Inhibition of glycogen synthase kinase - 3 alleviates Tcf3 repression of the pluripotency network and increases embryonic stem cell resistance to differentiation Authors: Wray J, Kalkan T, Gomez - Lopez S, Eckardt D, Cook A, Kemler R & Smith A Date: 19th June 2011 Publication Details: Nature Cell Biology 13,838 — 845 (2011) doi: 10.1038 / ncb2267

Inhibition of Pulmonary and Skeletal Metastasis by a Transforming Growth Factor - β Type I Receptor Kinase Inhibitor

Glycogen synthase kinase - 3 inhibition reduces ischemic cerebral damage, restores impaired mitochondrial biogenesis and prevents ROS production..

Using NPCs, Silva et al. delineated two phases in the reprogramming process (pre-pluripotency and ground state pluripotency) and demonstrated that dual inhibition (2i) of mitogen - activated protein kinase (MAKP) signaling and glycogen synthase kinase - 3 (GSK3) signaling combined with the self - renewal cytokine leukemia inhibitory factor (LIF) promotes pre-pluripotent cells to ground state pluripotency [19].

Thioredoxin - 1 (Trx1) is an endogenous antioxidant protein important for redox regulation and participates in the regulation of apoptosis through the inhibition of apoptosis signal - regulating kinase - 1 (Ask - 1).

Our data raise the possibility that inhibition of ABL kinases can increase apoptosis of breast cancer cells and block osteoclast activation, which is required for osteolytic metastasis.

We found that allosteric inhibition of the ABL kinases effectively impaired breast cancer bone metastasis and blocked tumor - induced osteolysis in mouse models.

These results demonstrate that ABL kinase activity is required for osteolytic metastasis in breast cancer and suggest that pharmacological inhibition of the ABL kinases may be an effective treatment for bone metastasis.

This concentration was used due to robust inhibition of NFκB and RIPK2 kinase assay in assays outlined in Figs. 2 — 6.

University of Wisconsin A chemical - genetic library of human cell lines for evaluating pharmacologic inhibition of protein kinases

(D) RIPK2 in vitro kinase assay was carried out as in Fig. 3B in KMH2 and HCT116 cells in the presence of ponatinib or RIPK2 inhibitor 1 to carry out a comparison of RIPK2 inhibition.

Different inhibition of Gβγ - stimulated class IB phosphoinositide 3 - kinase (PI3K) variants by a monoclonal antibody.

We decided to investigate whether the acquisition of a secondary JAK inhibitor resistant mutation in the kinase domain would make JAK1 V658F insensitive to JAK inhibition.

We found that canonical signaling by the EphB4 receptor is low in breast cancer cells and that ephrin - induced stimulation of EphB4 kinase activity inhibits breast cancer cell malignancy in culture and tumor growth in vivo (Figure 1A) through inhibition of the CRK proto - oncogene.

More recently, we elucidated an additional mechanism of tumor suppression mediated by canonical ephrin - induced EphA2 signaling (Figure 1A), which leads to inhibition of the AKT - mTORC1 oncogenic pathway through interplay of EphA2 with a phosphatase that dephosphorylates the AKT serine / threonine kinase.

We can clearly observe RIPK2 inhibitor 1 and 2 inhibition of MDP - dependent activation of RIPK2 autophosphorylation (on tyrosine 474) using an in vitro kinase assay in HCT116 cells (Fig. 3B).

Jha, B.K., Polyakova, I., Kessler, P., Dong, B., Dickerman, B., Sen, G.C., and Silverman, R.H. Inhibition of RNase L and RNA - dependent protein kinase (PKR) by sunitinib impairs antiviral innate immunity.

Specifically, my research proposal addresses the mechanisms by which the kinase 3 - phosphoinoside dependent protein kinase - 1 (PDK1) mediates resistance to cell cycle related CDK4 / 6 inhibition in ER + breast cancer and explores the in vivo effects of inhibiting PDK1 in combination with CDK4 / 6 inhibitors toward ER + breast cancer growth.

Concordantly, inhibition of the cGMP - dependent protein kinase G (PKG) blocks egress induced by PKAc1 inactivation or environmental acidification, while a cGMP - phosphodiesterase inhibitor circumvents egress repression by PKAc1 or pH neutralisation.

Au - Yeung G, Lang F, Azar WJ, Mitchell C, Jarman KE, Lackovic K, Aziz D, Cullinane C, Pearson RB, Mileshkin L, Rischin D, Karst AM, Drapkin R, Etemadmoghadam D, Bowtell DD.: Selective targeting of Cyclin E1 amplified high grade serous ovarian cancer by cyclin - dependent kinase 2 and AKT inhibition.

In contrast, loss of adhesion induced the phosphatases Dusp4 and -5 (Map - kinase phosphatases), which are inhibitors of the MAP - kinase signaling pathway, whereas contact inhibition induced the quiescent cell - specific transcription inhibitor E2F4.

Activation of the insulin receptor leads to sequential activation of a number of protein and lipid kinases, including the serine / threonine kinases Akt1 and Akt2, which not only stimulate mTOR and thus downregulate autophagic protein catabolism (and thus cysteine supplies), but elicit phosphorylation (inhibition) of FOXO1, a transcription factor that induces expression of proteins involved in both of the proteolysis recycling pathways: the autophagic / lysosomal pathway and the ubiquitin - proteasomal pathway.

Screened the analogues for the inhibition of protein kinase C using 32P - radioactive assay and found some interesting analogues with outstanding inhibition activity.