Tyrosine Kinase Inhibitors in Cancer: Breakthrough and Challenges of Targeted Therapy
Receptor tyrosine kinases (RTKs) are key regulatory signaling proteins governing cancer cell growth and metastasis. During the last two decades, several molecules targeting RTKs were used in oncology as a first or second line therapy in different types ...
C. Pottier+5 more
semanticscholar +1 more source
Background: The efficacy of next-generation epidermal growth factor receptor-tyrosine kinase inhibitors in patients with advanced non-small cell lung cancer who have failed first-generation epidermal growth factor receptor-tyrosine kinase inhibitors ...
Yi-Tian Qi MM+2 more
doaj +1 more source
Managing toxicities of Bruton tyrosine kinase inhibitors.
Inhibition of Bruton's tyrosine kinase (BTK) has revolutionized the treatment landscape for patients with chronic lymphocytic leukemia (CLL). By targeting this critical kinase in proximal B-cell receptor signaling, BTK inhibitors (BTKis) impair cell ...
A. Lipsky, N. Lamanna
semanticscholar +1 more source
Tyrosine kinase inhibitors and immunotherapy combinations in renal cell carcinoma
The treatment landscape of metastatic renal cell carcinoma (mRCC) has been transformed with the advent of antiangiogenics, notably tyrosine kinase inhibitors (TKIs) targeting vascular endothelial growth factor receptor (VEGFR), and immune checkpoint ...
E. Rassy, R. Flippot, L. Albiges
semanticscholar +1 more source
Diarrhoea is one of the most burdensome and common adverse events of chemotherapeutics, and has no standardised therapy to date. Increasing evidence suggests that the gut microbiome can influence the development of chemotherapy-induced diarrhoea. Here we
G. Ianiro+17 more
semanticscholar +1 more source
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]
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 +1 more source
EGF regulates tyrosine phosphorylation and membrane-translocation of the scaffold protein Tks5 [PDF]
Background: Tks5/FISH is a scaffold protein comprising of five SH3 domains and one PX domain. Tks5 is a substrate of the tyrosine kinase Src and is required for the organization of podosomes/invadopodia implicated in invasion of tumor cells.
Buday, László+5 more
core +1 more source
Identification of tyrosine kinase inhibitors that halt Plasmodium falciparum parasitemia.
Although current malaria therapies inhibit pathways encoded in the parasite's genome, we have looked for anti-malaria drugs that can target an erythrocyte component because development of drug resistance might be suppressed if the parasite cannot mutate ...
Kristina Kesely+7 more
doaj +1 more source
Emerging Agents for the Treatment of Advanced, Imatinib-Resistant Gastrointestinal Stromal Tumors : Current Status and Future Directions [PDF]
Imatinib is strongly positioned as the recommended first-line agent for most patients with advanced gastrointestinal stromal tumor (GIST) due to its good efficacy and tolerability.
Bauer, Sebastian, Joensuu, Heikki
core +1 more source
Effects of tyrosine kinase inhibitors on protein kinase-independent systems [PDF]
Tyrosine kinase inhibitors have been widely used to probe the role of tyrosine phosphorylation in cellular signalling. These inhibitors exhibit an apparent specificity for tyrosine kinases over the serine/threonine kinases but little is known about their
Denton, Richard M.+5 more
core +1 more source