Results 21 to 30 of about 1,888,598 (318)

Oncogenic RET Kinase domain mutations perturb the autophosphorylation trajectory by enhancing substrate presentation in trans [PDF]

, 2014
To decipher the molecular basis for RET kinase activation and oncogenic deregulation, we defined the temporal sequence of RET autophosphorylation by label-free quantitative mass spectrometry.
Martínez-Torres, R.J., Goodman, K., Plaza-Menacho, I., Barnouin, K., Mouilleron, S., Borg, A., Knowles, P.P., Murray-Rust, J., McDonald, Neil Q.   +8 more
core   +1 more source

Microwave-assisted efficient and facile synthesis of tetramic acid derivatives via a one-pot post-Ugi cascade reaction

Beilstein Journal of Organic Chemistry, 2020
A facile microwave-assisted method for the synthesis of tetramic acid derivatives has been developed through an Ugi/Dieckmann cyclization strategy with DBU.
Yong Li, Zheng Huang, Jia Xu, Yong Ding, Dian-Yong Tang, Jie Lei, Hong-yu Li, Zhong-Zhu Chen, Zhi-Gang Xu   +8 more
doaj   +1 more source

Structural instability in an autophosphorylating kinase switch [PDF]

, 2009
We analyse a simple kinase model that exhibits bistability when there is no protein turnover, and show analytically that the property of being bistable is not necessarily conserved when degradation and synthesis of the kinase are taken into ...
Grinfeld, M., Webb, S.D.
core   +1 more source

Flavopiridol Protects Against Inflammation by Attenuating Leukocyte-Endothelial Interaction via Inhibition of Cyclin-Dependent Kinase 9 [PDF]

, 2011
Objective: The cyclin-dependent kinase (CDK) inhibitor flavopiridol is currently being tested in clinical trials as anticancer drug. Beyond its cell death–inducing action, we hypothesized that flavopiridol affects inflammatory processes.
Mayer, Bettina A., Nina Berberich, Stefan Zahler, Sass, Gabriele, Fritz Krombach, Vollmar, Angelika M., Tiegs, Gisa, Krombach, Fritz, Fürst, Robert, Robert Fürst, Totzke, Frank, Angelika M. Vollmar, Jos Joore, Gisa Tiegs, Berberich, Nina, Alexander G. Khandoga, Bettina A. Mayer, Joore, Jos, Ulrike K. Schmerwitz, Gabriele Sass, Zahler, Stefan, Frank Totzke, Schmerwitz, Ulrike K., Khandoga, Alexander G.   +23 more
core   +1 more source

Kinases on Double Duty: A Review of UniProtKB Annotated Bifunctionality within the Kinome

Biomolecules, 2022
Phosphorylation facilitates the regulation of all fundamental biological processes, which has triggered extensive research of protein kinases and their roles in human health and disease.
Aziz M. Rangwala, Victoria R. Mingione, George Georghiou, Markus A. Seeliger   +3 more
doaj   +1 more source

Benzimidazoisoquinoline derivatives inhibit glioblastoma cell proliferation through down-regulating Raf/MEK/ERK and PI3K/AKT pathways

Cancer Cell International, 2018
Background Recent studies showed that benzimidazoleisoquinolinone derivatives exhibit anticancer activity against human cancer cell lines. The aim of this study is to evaluate the anti-tumor effects and mechanisms of benzimidazoleisoquinolinones in ...
Ya-Jun Zhang, Zhi-Gang Xu, Shi-Qiang Li, Liu-Jun He, Yan Tang, Zhong-Zhu Chen, Dong-Lin Yang   +6 more
doaj   +1 more source

Identification of Quinazolinone Analogs Targeting CDK5 Kinase Activity and Glioblastoma Cell Proliferation

Frontiers in Chemistry, 2020
CDK5/p25 kinase plays a major role in neuronal functions, and is hyperactivated in several human cancers including glioblastoma and neurodegenerative pathologies such as Alzheimer's and Parkinson's.
Marion Peyressatre, Dominique Patomo Arama, Arthur Laure, Juan A. González-Vera, Morgan Pellerano, Nicolas Masurier, Vincent Lisowski, May C. Morris   +7 more
doaj   +1 more source

Design, Synthesis, and Biochemical Evaluation of New Triazole Derivatives as Aurora-A Kinase Inhibitors

Molecules, 2021
Aurora-A kinase, a key mitosis regulator, is expressed in a cell cycle-dependent manner and has an essential role in maintaining chromosomal stability and the normal progression of the cell through mitosis.
Omeima Abdullah
doaj   +1 more source

Selective anticancer activity of a hexapeptide with sequence homology to a non-kinase domain of Cyclin Dependent Kinase 4 [PDF]

, 2011
Background: cyclin-dependent kinases 2, 4 and 6 (Cdk2, Cdk4, Cdk6) are closely structurally homologous proteins which are classically understood to control the transition from the G1 to the S-phases of the cell cycle by combining with their appropriate ...
Maurer, RI, Jon W Essex, Warenius Hilmar M, Kilburn, Jeremy D., Richard I Maurer, Seabra, LA, Usha Agarwala, Laurence A Seabra, Warenius, Hilmar M., Warenius, HM, Blaydes, JP, Seabra Laurence A, Jeremy D Kilburn, Essex, JW, Agarwala, U, Essex Jon W, Agarwala, Usha, Blaydes Jeremy P, Essex, Jon W., Jeremy P Blaydes, Maurer, Richard I., Agarwala Usha, Seabra, Laurence A., Kilburn Jeremy D, Hilmar M Warenius, Blaydes, Jeremy P., Maurer Richard I, Kilburn, Jeremy D, Kilburn, JD   +28 more
core   +1 more source

Regulation of Cardiac PKA Signaling by cAMP and Oxidants

Antioxidants, 2021
Pathologies, such as cancer, inflammatory and cardiac diseases are commonly associated with long-term increased production and release of reactive oxygen species referred to as oxidative stress.
Friederike Cuello, Friedrich W. Herberg, Konstantina Stathopoulou, Philipp Henning, Simon Diering   +4 more
doaj   +1 more source