Results 61 to 70 of about 2,078,396 (299)

Transcriptomic profiling of human cardiac cells predicts protein kinase inhibitor-associated cardiotoxicity

Nature Communications, 2020
Cardiotoxic adverse events associated with kinase inhibitors are a growing concern in clinical oncology. Here the authors use cellular transcriptomic responses of human cardiomyocytes treated with protein kinase inhibitors and the associated drug ...
J. G. Coen van Hasselt, Rayees Rahman, Jens Hansen, Alan Stern, Jaehee V. Shim, Yuguang Xiong, Amanda Pickard, Gomathi Jayaraman, Bin Hu, Milind Mahajan, James M. Gallo, Joseph Goldfarb, Eric A. Sobie, Marc R. Birtwistle, Avner Schlessinger, Evren U. Azeloglu, Ravi Iyengar   +16 more
doaj   +1 more source

Structure-based design and activity modeling of novel epidermal growth factor receptor kinase inhibitors; an in silico approach

Scientific African, 2020
The development of EGFR kinase inhibitors to treat non-small cell lung cancers is an important medical necessity due to persistent development of resistance by the mutations.
Muhammad Tukur Ibrahim, Adamu Uzairu, Gideon Adamu Shallangwa, Sani Uba   +3 more
doaj   +1 more source

Statistical and Clustering Analysis of Safety Profiles of FDA-Approved Protein Kinase Inhibitors

Applied Sciences
Protein kinases are vital regulators in cell biology, modifying protein functions through phosphorylation. Protein kinase inhibitors (PKIs), which impede these kinases’ activities, have broadened their therapeutic scope from cancer treatment to ...
Ioana Lavinia Radulian, Georgiana Nitulescu, Anca Zanfirescu, George Mihai Nitulescu   +3 more
doaj   +1 more source

An isoform of 14‐3‐3 protein regulates transbilayer lipid movement at the plasma membrane

FEBS Letters, EarlyView.
Loss of 14‐3‐3ζ in CHO cells confers resistance to exogenous phosphatidylserine (PS) and impairs endocytosis‐independent inward flip‐flop of fluorescent PS at the plasma membrane. RNAi‐mediated knockdown reproduces this defect, while no additive effect is seen in ATP11C‐deficient cells.
Akiko Yamaji‐Hasegawa, Akira Hattori, Masafumi Tsujimoto, Toshihide Kobayashi   +3 more
wiley   +1 more source

Selective inhibition of the kinase DYRK1A by targeting its folding process

Nature Communications, 2016
Kinase inhibitors are important drugs and usually target the ATP binding pocket of kinases. Here, Kii et al.report a completely new type of kinase inhibitor that specifically targets the protein folding intermediate state, but not the mature form, of the
Isao Kii, Yuto Sumida, Toshiyasu Goto, Rie Sonamoto, Yukiko Okuno, Suguru Yoshida, Tomoe Kato-Sumida, Yuka Koike, Minako Abe, Yosuke Nonaka, Teikichi Ikura, Nobutoshi Ito, Hiroshi Shibuya, Takamitsu Hosoya, Masatoshi Hagiwara   +14 more
doaj   +1 more source

Identification of a Novel Inhibitor of Mitogen-activated Protein Kinase Kinase*

Journal of Biological Chemistry, 1998
The compound U0126 (1,4-diamino-2,3-dicyano-1,4-bis[2-aminophenylthio]butadiene) was identified as an inhibitor of AP-1 transactivation in a cell-based reporter assay. U0126 was also shown to inhibit endogenous promoters containing AP-1 response elements
M. Favata, K. Horiuchi, E. Manos, A. J. Daulerio, Deborah A. Stradley, W. Feeser, D. E. Van Dyk, W. Pitts, R. Earl, F. Hobbs, R. Copeland, R. Magolda, P. Scherle, J. Trzăskos   +13 more
semanticscholar   +1 more source

Organizing the interface—Plasma membrane architecture and receptor dynamics in virus‐cell interactions

FEBS Letters, EarlyView.
Plasma membranes contain dynamic nanoscale domains that organize lipids and receptors. Because viruses operate at similar scales, this architecture shapes early infection steps, including attachment, receptor engagement, and entry. Using influenza A virus and HIV‐1 as examples, we highlight how receptor nanoclusters, multivalent glycan interactions ...
Jan Schlegel, Christian Sieben
wiley   +1 more source

The Role of Protein Kinases in Antigen-activation of Peripheral Blood Mononuclear Cells of Schistosoma mansoni Infected Individuals

Memorias do Instituto Oswaldo Cruz, 1997
T cell recognition of antigens displayed on the surface of antigen presenting cell results in rapid activation of protein tyrosine kinases and kinase C.
Almeida Célia A, Goes Alfredo M
doaj  

cGMP-Dependent Protein Kinase Inhibitors in Health and Disease

Pharmaceuticals, 2013
cGMP-dependent protein kinases (PKG) exhibit diverse physiological functions in the mammalian system e.g., in vascular and gastrointestinal smooth muscles, in platelets, in kidney, in bone growth, nociception and in the central nervous system ...
Jens Schlossmann, Johannes P. Huettner, Stefanie Wolfertstetter   +2 more
doaj   +1 more source

Potential and limitations of PKA/ PKG inhibitors for platelet studies

Platelets, 2022
Cyclic nucleotides (cAMP and cGMP) and corresponding protein kinases, protein kinase A (PKA) and protein kinase G (PKG), are the main intracellular mediators of endothelium-derived platelet inhibitors. Pharmacological PKA/PKG inhibitors are often used to
Valentina Shpakova, Natalia Rukoyatkina, Ulrich Walter, Stepan Gambaryan   +3 more
doaj   +1 more source