Sentences with phrase «targeting kinases»

These lipid - targeting kinases are under tight regulation, with disruption occurring in many diseases such as cancer, viral infections and inflammation.

Miniaturizing each individual experiment allows us to print whole libraries on a single plate, for instance gRNA / siRNA targeting all kinases in the human genome are printed on approximately 2.06 cm2 (0.32 sq. in.).

Oncodesign searched its library of 4,000 compounds that targeted kinases, and after exhaustive study, narrowed the selection down to 13.

If drug makers incorporated this technique into their early drug discovery process, he said, it would help identify which version of an atropisomeric compound actually targets the kinase they want to target, cutting the potential for side effects and helping to usher drugs past strict regulatory hurdles and into the hands of waiting patients.

When the researchers screened both the modified and unmodified versions against their target kinases, they found major differences in which kinases the different versions inhibited.

Not exact matches

The researchers observed that two drugs each killed a large fraction of the cells that had begun transitioning: dasatinib, a drug that targets the Src Family Kinase (SFK) and RK20449, a new drug in pre-clinical testing that specifically targets one of the SFK proteins called Hck.

Both tasocitinib and Incyte's drug, INCB028050, target Janus kinases, which mediate signaling by immune - system proteins called cytokines.

And several attempts to carve a new target from a family of enzymes called p38 kinases have also failed, despite favorable results in animal models.

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

These results not only show promise on a new targeted therapy to treat this malignancy, as PI3K inhibitors are already used in the clinical practice, but also unravel a new function of the PI3K kinase in cancer biology through its role in promoting metastasis.

Óscar Llorca and his team have used this technique to learn about the structure and functioning of a complex system called R2TP, which is involved in various key processes for cell survival such as the activation of the kinases mTOR, ATR and ATM, proteins that are the target of various cancer drugs currently being developed.

The researchers targeted mTOR with an experimental drug based on a prototype first designed by Shokat, a chemist and an expert in designing molecules to target this type of protein, called a kinase.

How lithium stabilises mood is poorly understood but when the scientists investigated how it prolongs the lives of flies, they discovered a new drug target that could slow aging — a molecule called glycogen synthase kinase - 3 (GSK - 3).

Often such trials include genetic markers for drugs that target particular pathways, such as a kinase inhibitor for cancer treatment.

The target for ibrutinib, an enzyme called Bruton's tyrosine kinase (BTK), is a key component of B - cell receptor signaling.

These receptors, called receptor tyrosine kinases (RTKs), transmit instructions through the cell wall and down through a cascade of reactions to a target gene in the nucleus.

They also say that the research shows that phosphatases, like kinases, could be general targets for drug development.

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.

Based on the current study results, the team believes a particular enzyme, «dual specificity tyrosine - regulated kinase - 1a (DYRK1A),» is the likely target of harmine.

Originally designed to block a kinase called MET, it was later discovered to target ALK as well.

These are used to identify protein - protein interactions, to identify the substrates of protein kinases, or to identify the targets of biologically active small molecules.

Understanding the molecular mechanisms underlying Aurora kinase - overexpressing tumours will help in the design of targeted and personalised cancer therapy,» said Dr Linda Chuang, Senior Research Scientist at CSI Singapore, who is the first author of the study.

Of the 10 already known, KnIT accounted for them in reasoning as well as ranking the likelihood that the other 64 kinases targeted p53.

There are over 500 known human kinases and 10s of thousands of possible proteins they can target.

Zeroing in on this kinase was encouraging, Goga said, because other researchers have shown that genetic - knockout mice that lack the entire family of PIM kinases are slightly smaller than normal mice, but «basically fine,» indicating that a drug targeting just PIM1 may have manageable levels of toxicity in breast cancer patients.

Approximately 10 - 15 % of Caucasian and 30 - 35 % of Asian patients with NSCLC have a mutation in the epidermal growth factor receptor (EGFR), which can be successfully targeted with EGFR inhibitors called tyrosine kinase inhibitors (TKI), such as erlotinib, gefitinib and afatinib.

The drug is a multi - kinase inhibitor (MKI)-- meaning it targets the specific enzymes that are required for growth in DTC.

Hund's team identified a phosphorylation site (Serine 571) on the voltage-gated sodium channel targeted by CaM kinase II that serves as a switch for inappropriate «late» sodium influx.

There are about 500 kinases in the human genome, each of which represents a potentially important drug target.

Specifically, these agents targeted the MAP / ERK kinase, which contributes to tumor growth, and the VEGFR protein, which controls blood vessel development.

Enter AICAR, which targets a protein called adenosine monophosphate - activated protein kinase (AMPK).

PAK kinases thus represent a new therapeutic target, which is independent of previous treatment methods.

Zelboraf targets patients who test positive for a variant of the BRAF gene, another kinase that can go haywire and cause cells to grow out of control.

«If we find a kinase that regulates filopodial bridge formation or a kinase that facilitates virus surfing along a filopodium,» he says, these enzymes can be targeted to thwart infection.

Our study reveals a new activation mechanism for protein kinases, which should be considered in the design of drugs that target PKG I,» said Kim.

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.

During the early years of my PhD studies, I was very fascinated by the exciting discoveries in the field of signal transduction, in particular how receptor tyrosine kinases are activated to transmit their signals and how protein complexes are formed through defined protein folds (domains) interacting with specific cellular targets.

In 2009, Stegmaier's laboratory discovered that SYK, a kinase that had attracted attention for its role in other malignancies, could be a potential drug target in AML.

The pathway Kean and her team studied is Aurora Kinase A, a well - known genetic target for cancer researchers.

The researchers, including scientists from pharmaceutical company AstraZeneca, report in an advanced online publication in Nature Medicine on May 4, that their findings indicate «an underappreciated genomic heterogeneity» in mechanisms of resistance to tyrosine kinase inhibitor (TKI) drugs that target the Epidermal Growth Factor Receptor (EGFR) mutation that drive some cases of non-small cell lung cancer (NSCLC).

«The LINK - A dependent HIF1 signalizing cascade and the consequent effects on cancer cells implicate LINK - A and LINK - A interacting kinases and receptors as promising therapeutic targets for TNBC.»

Protein kinases are targets for treatment of a number of diseases.

These therapies, the first an antibody and the second of a class called tyrosine kinase inhibitors (TKIs), reduce the ability of a target gene to manufacture the protein it encodes.

Among the serine - threonine kinases, p38, Rho - kinase, cyclin - dependent kinases, and Chk1 have been targeted with productive results for inflammation and cancer.

TKM - 080301 targets a specific gene called polo - like kinase 1 (PLK1), which codes for a protein involved in tumor cell growth.

Kinases are also druggable targets, as seen by the success of kinase - inhibitors in earning FDA approval (including, for example, crizotinib against ALK - fusion and erlotinib against EGFR).

D'Oro, U., Vacchio, M.S., Weissman, A.M. & Ashwell, J.D. Activation of the Lck tyrosine kinase targets cell surface T cell antigen receptors for lysosomal degradation.

MicroRNA - 93 inhibits inflammatory responses and cell apoptosis after cerebral ischemia reperfusion by targeting interleukin - 1 receptor - associated kinase 4.

Similarly, Bernaudin et al. [43] found increased expression of 18 genes in the neonatal rat brain following hypoxia (8 % O2 for 3 h) including several known hypoxia inducible genes such as MAP kinase phosphatase - 1 (MKP - 1), several HIF - 1 target genes including VEGF and GLUT - 1, genes implicated in apoptosis, signal transduction molecules, and transcription factors.

MicroRNA -7-5p regulates the proliferation and migration of intestinal epithelial cells by targeting trefoil factor 3 via inhibiting the phosphoinositide 3 - kinase / Akt signalling pathway.