Sentences with phrase «kinase activity at»

Not exact matches

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.

Axitinib, a drug used to treat renal cell carcinoma, has been shown to be effective at inhibiting the Abl kinase activity in patients with BCR - ABL1 (T315I).

«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.

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.

He received his MSc and his PhD in Molecular Pharmacology and Oncology at the Institute for Higher Studies of the University of Ferrara exploring the role of LRRK2 kinase activity in mouse model of model of familial Parkinson's disease and performing studies focused on the phenomena underlying neurodegeneration.

Flavopiridol inhibits several cellular kinases and has demonstrated cytostatic and cytotoxic activity in vitro and in vivo in numerous human tumor cell lines and xenograft models (including human breast, prostate, and lung carcinoma) at clinically achievable concentrations.

In 2005, the identification of an activating mutation in JAK2 (the V617F mutation) as a STAT5 - activating and disease - causing genetic alteration in a significant proportion of patients with myeloproliferative neoplasms (MPNs) has emphasized the oncogenic role of the JAK tyrosine kinases in hematologic malignancies.2 — 5 JAK2 is a member of the Janus tyrosine kinase family comprising three other mammalian non-receptor tyrosine kinases (JAK1, JAK3 and TYK2) that associate with cytokine receptors lacking intrinsic kinase activity to mediate cytokine - induced signal transduction and activation of STAT transcription factors.6 All JAKs share a similar protein structure and contain a tyrosine kinase domain at the C - terminus flanked by a catalytically inactive pseudokinase domain with kinase - regulatory activity, by an atypical SH2 domain and by a FERM domain that mediates association to the membrane - proximal region of the cytokine receptors.7, 8 Soon after the discovery of JAK2 V617F, we and others described that activating JAK1 mutations are relatively common in adult patients with T - cell acute lymphoblastic leukemia (ALL) and participate in ALL development allowing for constitutive activation of STAT5.9 — 11 Several STAT5 - activating JAK1 mutations were also reported in AML and breast cancer patients.10

In addition, at least some Eph receptors can also signal through non-canonical mechanisms that are independent of ligand binding and kinase activity, for example through interplay with other receptor tyrosine kinase families and with serine / threonine kinases.

Furthermore, we determined that RIPK2 inhibitor 1 effectively inhibited KHM2 cells at an approximate IC50 of 5 — 10 nM, and kinase activity was somewhat sensitive to detergent conditions (Fig. 4, B and C).

We further demonstrate that the cAMP - responsive enhancement of Oct4 activity is at least partially regulated through the p38 MAP kinase pathway.

It has been shown to interrupt glucose metabolism at a fundamental level and inhibit the expression of various kinases, which stimulate cancerous activity in the cells.