Results 1 to 10 of about 864,418 (362)

Structural and dynamic determinants for highly selective RET kinase inhibition reveal cryptic druggability

open access: yesJournal of Advanced Research, 2023
Introduction: The structural and dynamic determinants that confer highly selective RET kinase inhibition are poorly understood. Objectives: To explore the druggability landscape of the RET active site in order to uncover structural and dynamic ...
Moustafa A. Shehata   +6 more
doaj   +1 more source

ERK5 Inhibition Induces Autophagy-Mediated Cancer Cell Death by Activating ER Stress

open access: yesFrontiers in Cell and Developmental Biology, 2021
Autophagy is a highly conserved intracellular process that preserves cellular homeostasis by mediating the lysosomal degradation of virtually any component of the cytoplasm.
Andrés Gámez-García   +12 more
doaj   +1 more source

Targeting mTOR to overcome resistance to hormone and CDK4/6 inhibitors in ER-positive breast cancer models

open access: yesScientific Reports, 2023
Resistance to therapy remains a major obstacle in cancer management. Although treatment with hormone and CDK4/6 inhibitors is successful in luminal breast cancer, resistance to these treatments is frequent, highlighting the need for novel therapeutic ...
María Jimena Rodriguez   +12 more
doaj   +1 more source

An allosteric switch between the activation loop and a c-terminal palindromic phospho-motif controls c-Src function

open access: yesNature Communications, 2023
Autophosphorylation controls the transition between discrete functional and conformational states in protein kinases, yet the structural and molecular determinants underlying this fundamental process remain unclear.
Hipólito Nicolás Cuesta-Hernández   +10 more
doaj   +1 more source

Protein Kinase Mitogen-activated Protein Kinase Kinase Kinase Kinase 4 (MAP4K4) Promotes Obesity-induced Hyperinsulinemia [PDF]

open access: yesJournal of Biological Chemistry, 2016
Previous studies revealed a paradox whereby mitogen-activated protein kinase kinase kinase kinase 4 (Map4k4) acted as a negative regulator of insulin sensitivity in chronically obese mice, yet systemic deletion of Map4k4 did not improve glucose tolerance.
Roth Flach, Rachel J.   +12 more
openaire   +3 more sources

Protein kinases in cardiovascular diseases

open access: yesChinese Medical Journal, 2022
. Cardiovascular disease (CVD) remains the leading cause of death worldwide. Therefore, exploring the mechanism of CVDs and critical regulatory factors is of great significance for promoting heart repair, reversing cardiac remodeling, and reducing ...
Jiawen Chen   +6 more
doaj   +1 more source

The Ca2+/Calmodulin-dependent Protein Kinase Kinases Are AMP-activated Protein Kinase Kinases [PDF]

open access: yesJournal of Biological Chemistry, 2005
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

A framework for classification of prokaryotic protein kinases. [PDF]

open access: yesPLoS ONE, 2010
BACKGROUND: Overwhelming majority of the Serine/Threonine protein kinases identified by gleaning archaeal and eubacterial genomes could not be classified into any of the well known Hanks and Hunter subfamilies of protein kinases.
Nidhi Tyagi   +2 more
doaj   +1 more source

Secreted protein kinases [PDF]

open access: yesTrends in Biochemical Sciences, 2013
Protein kinases constitute one of the largest gene families and control many aspects of cellular life. In retrospect, the first indication for their existence was reported 130 years ago when the secreted protein, casein, was shown to contain phosphate.
Vincent S. Tagliabracci   +2 more
openaire   +3 more sources

Author Correction: YAP1/TAZ drives ependymoma-like tumour formation in mice

open access: yesNature Communications, 2020
An amendment to this paper has been published and can be accessed via a link at the top of the paper.
Noreen Eder   +14 more
doaj   +1 more source

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