Sentences with phrase «kinase activity of»

It is likely that our RIPK2 inhibitor 1 may interfere with the kinase activity of these off targets indirectly by resolving the inflammation.

The Ser / Thr kinase activity of the Yersinia protein kinase A (YpkA) is necessary for full virulence in the mouse, mollifying phagocytes, and disrupting the eukaryotic cytoskeleton.

The kinase activity of RIPK1 mediates hypothermia and lethality in a mouse model of TNF - induced shock, reflecting the hyperinflammatory state of systemic inflammatory response syndrome (SIRS), where the proinflammatory «cytokine storm» has long been viewed as detrimental.

Rapamycin forms an inhibitory complex with the FRB domain of mTOR and inhibits the kinase activities of mTOR protein (18, 19).

The basal and B - RAF - stimulated kinase activities of a third variant are unaltered but its activation by RAS is significantly reduced, suggesting that it may act in a dominant - negative manner to modulate pathway signaling.

Not exact matches

In the melanoma cell to its right, red indicates activity of a signaling molecule called PI3 - kinase.

«If we understand this assembly pathway — explains the researcher — we will be able to identify new ways of targeting the activity of these kinases.»

Using the nanodiscs, the team elucidated the activation mechanism of receptor kinase AgrC and discovered a key regulatory hotspot in the kinase that could greatly affect its activity.

But major pharmaceutical laboratories are investigating highly selective inhibitors of this molecular linchpin, many of them targeted at the enzymes (such as I - kB kinase) that regulate NF - kB activity.

Chronic activation of these autoreceptors revs up the activity of protein kinase A (PKA).

Our results suggest that frequent overexpression of Aurora Kinase in cancer may reduce RUNX3 transcription activity, leading to cell division and formation of tumours.

Transmission of signals in a cell is controlled by the coordinated activity of two families of enzymes: protein tyrosine kinases, which add a phosphate group to proteins, and protein tyrosine phosphatases, which remove them.

And it turns out that bosutinib may inhibit the activity of exactly the kinases that EGFR - dependent lung cancers need to mutate around the challenge of EGFR inhibitors.

Images taken with a fluorescent microscope show the activity of a kinase (green) in tumor cells (bottom) compared to normal cells (top).

The protein phosphatases were too long thought to just be the negative counterpart of protein kinases, with promiscuous activity and low intrinsic substrate specificity.

Some of its members have similar structures, which has led some researchers to propose that the activity of these kinases is probably regulated in a similar manner and, therefore, may be targeted with similar medications.

As the name suggests, kinase inhibitors interrupt the function of kinases — a particular type of enzyme — and effectively shut down the activity of proteins that contribute to cancer.

They were then able to use a compound recently discovered by Harvard University investigator Professor Nathanael Gray to block the activity of one of the kinases important in HCV replication, MAP4K2.

RET is a type of receptor tyrosine kinase, and mutations that kick its activity into overdrive are linked to certain kinds of cancer.

The activity of tyrosine kinases is typically regulated in an auto - inhibitory fashion, but the BCR - Abl fusion gene codes for a protein that is «always on» or continuously activated leading to unregulated cell division (i.e. cancer).

A role for casein kinase II phosphorylation in the regulation of IRF - 1 transcriptional activity.

Disruption of Ca2 + - dependent cell - matrix adhesion enhances c - Src kinase activity, but causes dissociation of the c - Src / FAK complex and dephosphorylation of tyrosine - 577 of FAK in carcinoma cells.

Moreover; it has been observed that elevated calcium levels and interaction of the membrane bound DAG with protein kinase C (PKC), activates PKC's kinase activity, which is known to regulate the cellular activity of MAPK [41].

Regulation of phospholipid scramblase activity during apoptosis and cell activation by protein kinase C$ ẹlta $.

In addition to being integral to cell biology, tyrosine kinases also present targets for new anticancer therapies: One of the most highly touted, rationally designed anticancer compounds, Gleevec, inhibits an oncogenic tyrosine kinase whose aberrant activity fuels the rampant growth of cells in patients with chronic myeloid leukemia.

It has been observed that mutated BRAF not only upregulates its own kinase activity, but also that of MEK and ERK, which in turn promotes cell proliferation [34].

Hydrophobic motif phosphorylation coordinates activity and polar localization of the Neurospora crassa nuclear Dbf2 - related kinase COT1.

LKB1, originally identified as a tumor suppressor protein, is currently thought as a critical regulator of cellular metabolism and growth by controlling the activity of AMP - activated protein kinase (AMPK) and also 12 other kinases that are closely related to AMPK.

To cite a few instances, polymerase chain reaction (PCR), a molecular method developed over three decades ago, has been widely applied in disease diagnosis, disease mechanism deciphering, and prognosis prediction; the elucidation of tyrosine kinase activity in cancer cells has led to the development of novel drugs for cancer treatment; and the identification of proteins and genetic molecules by molecular methods as biomarkers for disease diagnosis and prognosis has been drawing great interest.

Since November 2013, as part of SGC, Clara mainly investigates different subfamilies of kinases involved in alternative splicing through phosphorylation - mediated regulation of SR proteins activity.

Ablation of MEKK4 kinase activity causes neurulation and skeletal patterning defects in the mouse embryo.

Quizartinib inhibits FLT3 kinase activity and induced about a 50 % composite response rate among patients with FLT3 - ITD mutations in phase I and II studies, said lead author Mahesh Swaminathan, MD of the University of Texas MD Anderson Cancer Center in Houston.

Recently, interest has developed regarding the possibility of targeting intracellular inhibitory proteins to improve T cell activity against cancer, including diacylglycerol kinase ζ (DGKζ)(9, 10) and Casitas b - lineage proto - oncogene b (Cbl - b)(11), which attenuate signal transduction events downstream of the TCR and CD28.

ATM and ATR protein kinase activity confers cellular resistance to the cytotoxic effects of the anthelminthic drug niclosamide.

Invasion of eukaryotic cells by Borrelia burgdorferi requires β1 integrins and Src kinase activity.

«Two groups had reported a kinase activity associated with the viral Src protein,» recalls Hunter: Marc Collett and Ray Erikson, then at the University of Colorado Medical Center, and Mike Bishop and Harold Varmus, then at the University of California, San Francisco.

The mutation is acquired, is present in a variable proportion of granulocytes, alters a highly conserved valine present in the negative regulatory JH2 domain, and is predicted to dysregulate kinase activity.

Larotrectinib, a highly selective inhibitor of all three tropomyosin receptor kinase (TRK) proteins, was recently shown to have marked and sustained antitumor activity in patients with TRK fusion — positive cancers, according to an analysis of three phase I and II cohorts.

Kapoor P, Bao Y, Xiao J, Luo J, Shen J, Persinger J, Peng G, Ranish J, Bartholomew B, Shen X. (2015) Regulation of Mec1 kinase activity by the SWI / SNF chromatin remodeling complex.

AKT is a downstream effector of phosphatidylinositol 3 - kinase (PI3K) and a critical mediator of mammalian target of rapamycin (mTOR) activity (6).

Kapoor P, Bao Y, Xiao J, Espejo A, Yang L, Bedford MT, Peng G, Shen X. (2015) Phosphorylation - Dependent Enhancement of Rad53 Kinase Activity through the INO80 Chromatin Remodeling Complex.

Disruption of Autophagy at the Maturation Step by the Carcinogen Lindane Is Associated with the Sustained Mitogen - Activated Protein Kinase / Extracellular Signal — Regulated Kinase Activity

«As a result, researchers have used the presence of IBs and heightened kinase activity as a proxy for measuring LRRK2's harmful effects, rather than measuring LRRK2 levels directly,» explained Dr. Finkbeiner, who is the associate director of neurological research at Gladstone as well as a professor at the University of California, San Francisco, with which Gladstone is affiliated.

However, PI 3 - kinase activity, a well - known driver of prostate cancer, was notably absent from the metastasized tumors.

Additionally, we identified p21waf1 / cip1, a cyclin - dependent kinase inhibitor, as a target gene of DDX3, and the up - regulation of p21waf1 / cip1 expression accounted for the colony - suppressing activity of DDX3.

To evaluate whether loss of ABL kinases affected TAZ activity, we performed chromatin immunoprecipitation (ChIP) analysis using primers for TAZ targets identified by ChIP sequencing analysis (42).

Regardless, our data support a role for ABL kinases in the regulation of TAZ protein abundance and activity in breast cancer cells.

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.

Kinase domain mutants of Bcr - Abl exhibit altered transformation potency, kinase activity, and substrate utilization, irrespective of sensitivity to imKinase domain mutants of Bcr - Abl exhibit altered transformation potency, kinase activity, and substrate utilization, irrespective of sensitivity to imkinase activity, and substrate utilization, irrespective of sensitivity to imatinib

Studies by ours and other groups have shown that a number of EphA2 and EphA3 mutations inactivate Eph receptor canonical signaling by disrupting ephrin binding or kinase activity, consistent with a role of canonical signaling in tumor suppression.