The NanoBRET TE platform combines the sensitivity of NanoLuc technology with quantitative capabilities of energy transfer, and allows for quantitative measurements of drug affinity and kinase
selectivity inside live cells at target levels similar to that of endogenous kinases
Summary: The PIM kinases
are a family of serine/threonine kinases
that catalyze the ATP dependent phosphorylation.
are enzymes that regulate essential cellular processes.
These include kinase
inhibitors with activity against serine/threonine kinases
, dual specificity kinases
or both tyrosine and serine/threonine kinases
being developed for oncological indications.
Summary: TEHRAN (FNA)- Some cancers can be effectively treated with drugs inhibiting proteins known as receptor tyrosine kinases
, but not those cancers caused by mutations in the KRAS gene.
are a large group of related enzymes that activate many kinds of proteins, thus mediating signal transduction in cell growth and differentiation.
Since their identification in the 1980s as having an important role in oncogenesis and tumor progression, protein kinases
have received increasing attention as targets for anticancer drugs.
regulate a variety of cellular functions, such as cell growth, proliferation, differentiation, motility, survival and intracellular trafficking.
Louis, Missouri, urban particles (UPs; Standard Reference Material 1648) on the constriction of isolated rat pulmonary artery tings and the activation of extracellular signal-regulated kinases
1 and 2 (ERK1/2) and p38 mitogen-activated protein kinases
(MAPKs) in human pulmonary artery endothelial cells with or without losartan, an antagonist of A[T.
Since receptor-binding Fn peptides decrease focal contacts, disturb cytoskeletal elements such as actin and decrease Fn receptor aggregation in fibroblasts, we have proposed that Fn-fs have similar effects in chondrocytes and that these changes in receptor and cytoskeletal elements alter the location of upstream kinases
near receptors which leads to altered signal transduction and emergence of inflammatory MAP kinase
Defects in specific protein kinases
have been linked to over 400 diseases including cancer, diabetes and Alzheimers, and about 25% of all pharmaceutical industry research and development is now focused on the discovery and evaluation of protein kinase
inhibitors for therapeutic applications.
P38 MAP kinases
are ubiquitously expressed not only in inflammatory cells, but in the liver, lungs, kidneys, heart, intestines, and other tissues.