Results 1 to 10 of about 1,477,881 (298)
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
Mechanistic target of rapamycin signaling in human nervous system development and disease
Mechanistic target of rapamycin (mTOR) is a highly conserved serine/threonine kinase that regulates fundamental cellular processes including growth control, autophagy and metabolism. mTOR has key functions in nervous system development and mis-regulation
Marie Girodengo +3 more
doaj +1 more source
Developmental and epileptic encephalopathies (DEEs) are a group of rare childhood disorders characterized by severe epilepsy and cognitive deficits. Numerous DEE genes have been discovered thanks to advances in genomic diagnosis, yet putative molecular ...
Marisol Sampedro-Castañeda +9 more
doaj +1 more source
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
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
ERK5 Inhibition Induces Autophagy-Mediated Cancer Cell Death by Activating ER Stress
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
A new series of piperine-carboximidamide hybrids VIa-k was developed as a new cytotoxic agent targeting EGFR, BRAF, and CDK2. The antiproliferative effect against four cancer cells was investigated against erlotinib.
Lamya H. Al-Wahaibi +4 more
doaj +1 more source
Cellular Tolerance Induced by Chronic Opioids in the Central Nervous System
Opioids are powerful analgesics that elicit acute antinociceptive effects through their action the mu opioid receptor (MOR). However opioids are ineffective for chronic pain management, in part because continuous activation of MORs induces adaptive ...
Sweta Adhikary, John T. Williams
doaj +1 more source
Although 15–20% of COVID‐19 patients experience hyper‐inflammation induced by massive cytokine production, cellular triggers of this process and strategies to target them remain poorly understood.
Marina Chan +5 more
doaj +1 more source
Identification of Potential Kinase Inhibitors within the PI3K/AKT Pathway of Leishmania Species
Leishmaniasis is a public health disease that requires the development of more effective treatments and the identification of novel molecular targets. Since blocking the PI3K/AKT pathway has been successfully studied as an effective anticancer strategy ...
Rodrigo Ochoa +7 more
doaj +1 more source

