Results 1 to 10 of about 854,863 (214)

Crosstalks between Raf-kinase inhibitor protein and cancer stem cell transcription factors (Oct4, KLF4, Sox2, Nanog)

Tumor Biology, 2017
Raf-kinase inhibitor protein has been reported to inhibit both the Raf/mitogen extracellular signal–regulated kinase/extracellular signal–regulated kinase and nuclear factor kappa-light-chain of activated B cells pathways.
Benjamin Bonavida, Sohyun Lee
exaly   +2 more sources

Is asciminib an effective tyrosine kinase inhibitor for chronic myeloid leukemia patients with tyrosine kinase inhibitor resistance? [PDF]

Hematol Transfus Cell Ther
Asciminib represents a significant advancement in the treatment of chronic myeloid leukemia, establishing a novel therapeutic paradigm by specifically targeting the ABL1 myristoyl pocket, a mechanism distinct from that of conventional adenosine ...
Omar MM, Alanazi MA, Jackson DE.
europepmc   +2 more sources

Structure Activity Relationship Studies around DB18, a Potent and Selective Inhibitor of CLK Kinases

Molecules, 2022
Three series of our lead CLK1 inhibitor DB18 have been designed, synthetized and tested against CLKs and DYRK1A kinases. Their cytotoxicity was subsequently measured on seven representative cancer cell lines.
Dabbugoddu Brahmaiah, Anagani Kanaka Durga Bhavani, Pasula Aparna, Nangunoori Sampath Kumar, Hélène Solhi, Rémy Le Guevel, Blandine Baratte, Thomas Robert, Sandrine Ruchaud, Stéphane Bach, Surender Singh Jadav, Chada Raji Reddy, Paul Mosset, Nicolas Gouault, Nicolas Levoin, René Grée   +15 more
doaj   +1 more source

The Kinase Specificity of Protein Kinase Inhibitor Peptide

Frontiers in Pharmacology, 2021
G-protein-coupled-receptor (GPCR) signaling is exquisitely controlled to achieve spatial and temporal specificity. The endogenous protein kinase inhibitor peptide (PKI) confines the spatial and temporal spread of the activity of protein kinase A (PKA ...
Yao Chen, Yao Chen, Bernardo L. Sabatini
doaj   +1 more source

Development of a CDK10/CycM in vitro Kinase Screening Assay and Identification of First Small-Molecule Inhibitors

Frontiers in Chemistry, 2020
Cyclin-dependent kinases (CDKs) constitute a family of 20 serine/threonine protein kinases that play pivotal roles in the regulation of numerous important molecular and cellular processes. CDKs have long been considered promising therapeutic targets in a
Thomas Robert, Thomas Robert, Jared L. Johnson, Roxane Guichaoua, Tomer M. Yaron, Stéphane Bach, Stéphane Bach, Lewis C. Cantley, Pierre Colas   +8 more
doaj   +1 more source

Synthesis and Kinase Inhibitory Potencies of Pyrazolo[3,4-g]isoquinolines

Molecules, 2022
A new series of pyrazolo[3,4-g]isoquinoline derivatives, diversely substituted at the 4- or 8-position, were synthesized. The results of the kinase inhibitory potency study demonstrated that the introduction of a bromine atom at the 8-position was ...
Mathilde Defois, Chloé Rémondin, Béatrice Josselin, Lionel Nauton, Vincent Théry, Fabrice Anizon, Sandrine Ruchaud, Francis Giraud, Pascale Moreau   +8 more
doaj   +1 more source

Inhibitory effects of regorafenib, a multiple tyrosine kinase inhibitor, on corneal neovascularization [PDF]

International Journal of Ophthalmology, 2014
AIM:To evaluate the inhibitory effects of regorafenib (BAY 73-4506), a multikinase inhibitor, on corneal neovascularization (NV).METHODS:Thirty adult male Sprague-Dawley rats weighing 250-300 g, were used.
Halil Ibrahim Onder, Mesut Erdurmus, Yasin Yücel Bucak, Hüseyin Simavli, Murat Oktay, Ahmet Sahap Kukner   +5 more
doaj   +1 more source

The Anti-Candida albicans Agent 4-AN Inhibits Multiple Protein Kinases

Molecules, 2019
Small molecules containing quinone and/or oxime moieties have been found as promising anti-fungal agents. One of them is 4-AN, a recently reported potent anti-Candida compound, which inhibits the formation of hyphae, decreases the level of cellular ...
Maciej Masłyk, Monika Janeczko, Aleksandra Martyna, Sławomir Czernik, Małgorzata Tokarska-Rodak, Marta Chwedczuk, Béatrice Foll-Josselin, Sandrine Ruchaud, Stéphane Bach, Oleg M. Demchuk, Konrad Kubiński   +10 more
doaj   +1 more source

Death by a thousand cuts through kinase inhibitor combinations that maximize selectivity and enable rational multitargeting

eLife, 2023
Kinase inhibitors are successful therapeutics in the treatment of cancers and autoimmune diseases and are useful tools in biomedical research. However, the high sequence and structural conservation of the catalytic kinase domain complicate the ...
Ian R Outhwaite, Sukrit Singh, Benedict-Tilman Berger, Stefan Knapp, John D Chodera, Markus A Seeliger   +5 more
doaj   +1 more source

Second‐line therapy with first‐ or second‐generation tyrosine kinase inhibitors in EGFR‐mutated non‐small cell lung cancer patients with T790M‐negative or unidentified mutation

Thoracic Cancer, 2021
Background T790M mutation causes resistance to tyrosine kinase inhibitors (TKIs) in approximately 49% of patients with epidermal growth receptor‐mutant non‐small cell lung cancer (NSCLC).
Tadashi Nishimura, Tomohito Okano, Masahiro Naito, Soichi Iwanaka, Ayaka Ohiwa, Yasumasa Sakakura, Taro Yasuma, Hajime Fujimoto, Corina N. D'Alessandro‐Gabazza, Yasuhiro Oomoto, Tetsu Kobayashi, Esteban C. Gabazza, Hidenori Ibata   +12 more
doaj   +1 more source