A comprehensive review of protein kinase inhibitors for cancer therapy
Introduction: Protein kinases are involved in various cellular functions. About 2% of the human genome encodes for protein kinases. Dysregulation of protein kinases is implicated in various processes of carcinogenesis.
Radhamani Kannaiyan, D. Mahadevan
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Seminal plasma and prostaglandin E2 up-regulate fibroblast growth factor 2 expression in endometrial adenocarcinoma cells via E-series prostanoid-2 receptor-mediated transactivation of the epidermal growth factor receptor and extracellular signal-regulated kinase pathway [PDF]
We report a multiwavelength (X-ray, ultraviolet/optical/infrared, radio) analysis of the relativistic tidal disruption event candidate Sw J2058+05 from 3 months to 3 yr post-discovery in order to study its properties and compare its behavior with that of
Bower, Geoffrey C. +15 more
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Depletion of Ca2+ from the sarcoplasmic reticulum of cardiac muscle prompts phosphorylation of phospholamban to stimulate store refilling [PDF]
Nonmuscle cells have almost ubiquitously evolved a mechanism to detect and prevent Ca(2+) store depletionstore operated calcium entry. No such mechanism has, as yet, been reported in cardiac myocytes.
Bhogal, M.S., Colyer, J.
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Insights into the binding mode of MEK type-III inhibitors. A step towards discovering and designing allosteric kinase inhibitors across the human kinome. [PDF]
Protein kinases are critical drug targets for treating a large variety of human diseases. Type-III kinase inhibitors have attracted increasing attention as highly selective therapeutics.
Zheng Zhao, Lei Xie, Philip E Bourne
doaj +1 more source
Salt-inducible kinases (SIKs) regulate TGFβ-mediated transcriptional and apoptotic responses [PDF]
The signalling pathways initiated by members of the transforming growth factor-β (TGFβ) family of cytokines control many metazoan cellular processes, including proliferation and differentiation, epithelial-mesenchymal transition (EMT) and apoptosis. TGFβ
A Rojas-Fernandez +63 more
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The pathophysiology of pulmonary arterial hypertension (PAH) induced by protein kinase inhibitors (PKIs) remains unclear. To gain knowledge into this rare and severe pathology we performed a study combining a pharmacovigilance approach and the ...
Lucie Cornet +9 more
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Many clinically approved protein kinase inhibitors stabilize an inactive conformation of their kinase target. Such inhibitors are generally highly selective compared to active conformation inhibitors, and consequently, general methods to identify ...
Yoshiji Hantani +8 more
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Mutations in the leucine-rich repeat kinase 2 (LRRK2) gene are a common cause of familial Parkinson's disease (PD). Variation around the LRRK2 locus also contributes to the risk of sporadic PD.
Rudenko Iakov N +2 more
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Investigating the effect of target of rapamycin kinase inhibition on the Chlamydomonas reinhardtii phosphoproteome: from known homologs to new targets [PDF]
Recuperado de: https://www.biorxiv.org/content/10.1101/310102v1Target of rapamycin (TOR) kinase is a conserved regulator of cell growth whose activity is modulated in response to nutrients, energy and stress.
Couso Liáñez, Inmaculada Concepción +6 more
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Targeting mTOR for cancer therapy
Mechanistic target of rapamycin (mTOR) is a protein kinase regulating cell growth, survival, metabolism, and immunity. mTOR is usually assembled into several complexes such as mTOR complex 1/2 (mTORC1/2).
Hui Hua +5 more
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