Results 41 to 50 of about 947,345 (358)

Safety, pharmacokinetics, and antitumor properties of anlotinib, an oral multi-target tyrosine kinase inhibitor, in patients with advanced refractory solid tumors

Journal of Hematology & Oncology, 2016
BackgroundAnlotinib is a novel multi-target tyrosine kinase inhibitor that is designed to primarily inhibit VEGFR2/3, FGFR1-4, PDGFR α/β, c-Kit, and Ret.
Yongkun Sun, Wei Niu, F. Du, C. Du, Shuting Li, Jinwan Wang, Li Li, Feng-qing Wang, Y. Hao, Chuan Li, Y. Chi   +10 more
semanticscholar   +1 more source

Acalabrutinib (ACP-196): A Covalent Bruton Tyrosine Kinase Inhibitor with a Differentiated Selectivity and In Vivo Potency Profile

Journal of Pharmacology and Experimental Therapeutics, 2017
Several small-molecule Bruton tyrosine kinase (BTK) inhibitors are in development for B cell malignancies and autoimmune disorders, each characterized by distinct potency and selectivity patterns.
T. Barf, T. Covey, R. Izumi, Bas van de Kar, Michael Gulrajani, B. van Lith, M. van Hoek, E. de Zwart, D. Mittag, Dennis Demont, S. Verkaik, Fanny Krantz, P. Pearson, R. Ulrich, A. Kaptein   +14 more
semanticscholar   +1 more source

Pharmacological Evidence for Involvement of Phospholipase D, Protein Kinase C, and Sodium-Calcium Exchanger in -Adrenoceptor-Mediated Negative Inotropy in Adult Mouse Ventricle

Journal of Pharmacological Sciences, 2003
The intracellular signalling pathway for a-adrenoceptor-mediated negative inotropy was studied pharmacologically in isolated adult mouse ventricle. The negative inotropy was inhibited by GF-109203X, a nonselective protein kinase C inhibitor.
Kazuhide Nishimaru, Yoshio Tanaka, Hikaru Tanaka, Koki Shigenobu   +3 more
doaj   +1 more source

Vanadate Activates Rho A Translocation in Association With Contracting Effects in Ileal Longitudinal Smooth Muscle of Guinea Pig

Journal of Pharmacological Sciences, 2004
We characterized the effects of vanadate, an inhibitor of tyrosine phosphatase, on the tension, the level of myosin light chain (MLC) phosphorylation, and Rho A activation in intact ileal longitudinal smooth muscle of the guinea pig to study the role of ...
Mayumi Mori, Hiromi Tsushima
doaj   +1 more source

Rapamycin induces transactivation of the EGFR and increases cell survival. [PDF]

, 2009
The mammalian target of rapamycin (mTOR) signaling network regulates cell growth, proliferation and cell survival. Deregulated activation of this pathway is a common event in diverse human diseases such as cancers, cardiac hypertrophy, vascular ...
Chaturvedi, D, Cohen, MS, Gao, X, Patel, TB, Taunton, J   +4 more
core   +2 more sources

Tyrosine Kinase Inhibitor Resistance in Patients with Chronic Myeloid Leukemia: A 10-Year Study of BCR-ABL Gene Mutation Profile in Russia (2006–2016) [PDF]

Клиническая онкогематология, 2018
Background. Kinase domain mutations of BCR-ABL gene is the most common cause of tyrosine kinase inhibitor resistance. Aim. To present the data on prognostic value of BCR-ABL mutation burden in Russian patients over the last 10 years.
VV Tikhonova, MA Isakov, VA Misyurin, YuP Finashutina, LA Kesaeva, NA Lyzhko, IN Soldatova, NN Kasatkina, EN Misyurina, AV Misyurin   +9 more
doaj   +1 more source

Entrectinib: an orally available, selective tyrosine kinase inhibitor for the treatment of NTRK, ROS1, and ALK fusion-positive solid tumors

Therapeutics and Clinical Risk Management, 2018
Entrectinib is a potent small-molecule tyrosine kinase inhibitor that targets oncogenic rearrangements in NTRK, ROS1, and ALK. The consolidated results of 2 Phase I trials demonstrated activity in tyrosine kinase inhibitor-naïve patients along with ...
Dazhi Liu, M. Offin, Stephen Harnicar, Bob T. Li, A. Drilon   +4 more
semanticscholar   +1 more source

Mechanisms of Resistance to Noncovalent Bruton's Tyrosine Kinase Inhibitors.

New England Journal of Medicine, 2022
BACKGROUND Covalent (irreversible) Bruton's tyrosine kinase (BTK) inhibitors have transformed the treatment of multiple B-cell cancers, especially chronic lymphocytic leukemia (CLL).
E. Wang, Xiaoli Mi, Meghan C. Thompson, S. Montoya, R. Notti, Jumana Afaghani, B. Durham, A. Penson, Matthew T. Witkowski, Sydney X Lu, J. Bourcier, Simon J. Hogg, C. Erickson, Daniel Cui, Hana Cho, Michael Singer, T. Totiger, S. Chaudhry, M. Geyer, Alvaro J Alencar, A. Linley, M. Palomba, Catherine C Coombs, Jae H. Park, A. Zelenetz, L. Roeker, M. Rosendahl, D. E. Tsai, K. Ebata, B. Brandhuber, D. Hyman, I. Aifantis, A. Mato, Justin Taylor, O. Abdel-Wahab   +34 more
semanticscholar   +1 more source

Moving on up: Second-Line Agents as Initial Treatment for Newly-Diagnosed Patients with Chronic Phase CML

Clinical Medicine Insights: Oncology, 2011
The treatment of chronic myelogenous leukemia (CML) was revolutionized by the development of imatinib mesylate, a small molecule inhibitor of several protein tyrosine kinases, including the ABL1 protein tyrosine kinase.
Marie P. Shieh, Masato Mitsuhashi, Michael Lilly   +2 more
doaj   +1 more source

Mechanisms of acquired resistance to tyrosine kinase inhibitors

Acta Pharmaceutica Sinica B, 2011
In recent years, structural and functional studies reveal that tyrosine kinases (TKs) act as the essential components of signal transduction pathways that regulate cancer cell proliferation, apoptosis and angiogenesis, and therefore become potential ...
Yi-fan Chen, Li-wu Fu
doaj   +1 more source