Oncogenic RET Kinase domain mutations perturb the autophosphorylation trajectory by enhancing substrate presentation in trans [PDF]
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. +8 more
core +1 more source
C27H22BrClN2O5, triclinic, P1̄, a = 6.8549(4) Å, b = 13.2863(12) Å, c = 14.3690(13) Å, α = 85.944(7)°, β = 84.882(6)°, γ = 89.932(6)°, V = 1300.18(18) Å3, Z = 2, Rgt(F) = 0.0655, wRref(F2) = 0.1841, T = 293(2) K.
Meng Jiang Ping, Lei Jie
doaj +1 more source
Downfalls of Chemical Probes Acting at the Kinase ATP-Site: CK2 as a Case Study
Protein kinases are a large class of enzymes with numerous biological roles and many have been implicated in a vast array of diseases, including cancer and the novel coronavirus infection COVID-19.
Eleanor L. Atkinson +5 more
doaj +1 more source
The global burden of cancer necessitates rapid and ongoing development of effective cancer therapies. One promising approach in this context is the repurposing of existing non-cancer drugs for cancer indications.
Saiful Islam +6 more
doaj +1 more source
Inhibition of Rho-kinase improves response to deep inspiration in ovalbumin-sensitized guinea pigs [PDF]
Objective(s): The modulatory effect of deep inspiration (DI) on airway constriction is impaired in asthma. However, mechanisms underlying this impairment are not clear.
Saeed Pazhoohan +6 more
doaj +1 more source
Xenopus 45-kDa mitogen-activated protein (MAP) kinase kinase (MAPKK) is a serine/threonine/tyrosine kinase, which activates MAP kinase (MAPK) by phosphorylating its threonine and tyrosine residues. MAPKK is active only when its threonine and/or serine residues are phosphorylated.
S, Matsuda, Y, Gotoh, E, Nishida
openaire +2 more sources
Conserved Docking Site Is Essential for Activation of Mammalian MAP Kinase Kinases by Specific MAP Kinase Kinase Kinases [PDF]
Mammalian mitogen-activated protein kinase (MAPK) cascades control various cellular events, ranging from cell growth to apoptosis, in response to external stimuli. A conserved docking site, termed DVD, is found in the mammalian MAP kinase kinases (MAPKKs) belonging to the three major subfamilies, namely MEK1, MKK4/7, and MKK3/6.
Takekawa, Mutsuhiro +2 more
openaire +2 more sources
Flavopiridol Protects Against Inflammation by Attenuating Leukocyte-Endothelial Interaction via Inhibition of Cyclin-Dependent Kinase 9 [PDF]
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. +23 more
core +1 more source
The Ca2+/Calmodulin-dependent Protein Kinase Kinases Are AMP-activated Protein Kinase Kinases [PDF]
The AMP-activated protein kinase (AMPK) is an important regulator of cellular metabolism in response to metabolic stress and to other regulatory signals. AMPK activity is absolutely dependent upon phosphorylation of AMPKalphaThr-172 in its activation loop by one or more AMPK kinases (AMPKKs).
Rebecca L, Hurley +5 more
openaire +2 more sources
Loss of the Conserved Alveolate Kinase MAPK2 Decouples
Mitogen-activated protein kinases (MAPKs) are a conserved family of protein kinases that regulate signal transduction, proliferation, and development throughout eukaryotes. The apicomplexan parasite Toxoplasma gondii expresses three MAPKs.
Xiaoyu Hu +3 more
doaj +1 more source

