Targeting kinases with anilinopyrimidines: Discovery of N-phenyl-N'-[4-(pyrimidin-4-ylamino)phenyl]urea derivatives as selective inhibitors of class III receptor tyrosine kinase subfamily [PDF]
, 2015 Kinase inhibitors are attractive drugs/drug candidates for the treatment of cancer. The most recent literature has highlighted the importance of multi target kinase inhibitors, although a correct balance between specificity and non-specificity is ...
Chilin, Adriana +5 more
core +2 more sources
Evidence of the presence of calcium/calmodulin-dependent protein kinase IV in human sperm and its involvement in motility regulation [PDF]
, 2005 The mechanisms involved in the regulation of mammalian sperm motility are not well understood. Calcium ions (Ca(2+)) have been suggested to play a key role in the maintenance of motility; nevertheless, how Ca(2+) modulates this process has not yet been ...
Buffone, Mariano Gabriel +6 more
core +1 more source
Activation of tyrosine kinases by mutation of the gatekeeper threonine. [PDF]
, 2008 Protein kinases targeted by small-molecule inhibitors develop resistance through mutation of the gatekeeper threonine residue of the active site. Here we show that the gatekeeper mutation in the cellular forms of c-ABL, c-SRC, platelet-derived growth ...
Azam, Mohammad +4 more
core +1 more source
Tyrosine Kinase Inhibitors as Antiangiogenic Drugs in Multiple Myeloma
Pharmaceuticals, 2010 Tyrosine kinase inhibitors are a new class of anticancer drugs, that are capable of directly interacting with the catalytic site of the target enzyme and thereby inhibiting catalysis. Therapeutically useful tyrosine kinase inhibitors are not specific for
Domenico Ribatti
doaj +1 more source
Tyrosine kinase inhibitors for the therapy of anaplastic thyroid cancer [PDF]
, 2015 Anaplastic thyroid cancer (ATC) is often incurable so new therapeutic approaches are needed. Tyrosine kinases inhibitors (such as imanitib, sunitinib or sorafenib) are under evaluation for the treatment of ATC.
Bond JA +11 more
core +1 more source
Tumor Biology, 2017 The finding of epidermal growth factor receptor tyrosine kinase inhibitors, which reflects a classical process of translational research, is a critical milestone for non-small-cell lung cancer treatment.
Shaohua Cui, Liyan Jiang
doaj +1 more source
Haematologica, 2013 Response to tyrosine kinase inhibitors at three months is a predictor for long-term outcome in chronic myeloid leukemia patients treated with tyrosine kinase inhibitors.
Aziz Nazha +12 more
doaj +1 more source
Targeting Btk/Etk of prostate cancer cells by a novel dual inhibitor. [PDF]
, 2014 Btk and Etk/BMX are Tec-family non-receptor tyrosine kinases. Btk has previously been reported to be expressed primarily in B cells and has an important role in immune responses and B-cell malignancies.
Bhardwaj, G +16 more
core +2 more sources
Systemic Mastocytosis: Following the Tyrosine Kinase Inhibition Roadmap
Frontiers in Pharmacology, 2020 Systemic mastocytosis is a rare and heterogeneous disease characterized by mast cell proliferation and activation. KIT is a transmembrane tyrosine kinase which plays a key role in mast cell growth, differentiation and survival. After interaction with its
Miguel Piris-Villaespesa +1 more
doaj +1 more source
Kinase profiling of liposarcomas using RNAi and drug screening assays identified druggable targets. [PDF]
, 2017 BackgroundLiposarcoma, the most common soft tissue tumor, is understudied cancer, and limited progress has been made in the treatment of metastatic disease.
Doan, Ngan B +9 more
core +2 more sources