MTOR cross-talk in cancer and potential for combination therapy [PDF]
The mammalian Target of Rapamycin (mTOR) pathway plays an essential role in sensing and integrating a variety of exogenous cues to regulate cellular growth and metabolism, in both physiological and pathological conditions.
Bazzichetto, C.+7 more
core +3 more sources
Pharmacology and pharmacovigilance of protein kinase inhibitors
Protein kinase inhibitors experienced their advent in the 2000s. Their market introduction made it possible to constitute a class of targeted therapies administered orally. This name was chosen to mark a break with conventional chemotherapy drugs, but it is important to stress that these are multi-target drugs with complex affinity profiles.
Khouri, Charles+4 more
openaire +5 more sources
Therapeutic resistance to kinase inhibitors constitutes a major unresolved clinical challenge in cancer and especially in glioblastoma. Multi-kinase inhibitors may be used for simultaneous targeting of multiple target kinases and thereby potentially ...
Oxana V. Denisova+10 more
doaj +1 more source
Dynamic telomerase gene suppression via network effects of GSK3 inhibition [PDF]
<b>Background</b>: Telomerase controls telomere homeostasis and cell immortality and is a promising anti-cancer target, but few small molecule telomerase inhibitors have been developed. Reactivated transcription of the catalytic subunit hTERT
Bilsland, Alan E.+10 more
core +12 more sources
Cytoprotective effect of the elongation factor-2 kinase-mediated autophagy in breast cancer cells subjected to growth factor inhibition. [PDF]
Autophagy is a highly conserved and regulated cellular process employed by living cells to degrade proteins and organelles as a response to metabolic stress. We have previously reported that eukaryotic elongation factor-2 kinase (eEF-2 kinase, also known
Yan Cheng+5 more
doaj +1 more source
JNK signalling in cancer: In need of new, smarter therapeutic targets [PDF]
Copyright © 2013 The British Pharmacological Society. This is the accepted version of the following article: Bubici, C. and Papa, S. (2014), JNK signalling in cancer: in need of new, smarter therapeutic targets.
Adams+137 more
core +2 more sources
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
semanticscholar +1 more source
Requirement for the eIF4E binding proteins for the synergistic down-regulation of protein synthesis by hypertonic conditions and mTOR inhibition. [PDF]
The protein kinase mammalian target of rapamycin (mTOR) regulates the phosphorylation and activity of several proteins that have the potential to control translation, including p70S6 kinase and the eIF4E binding proteins 4E-BP1 and 4E-BP2.
Michael J Clemens+2 more
doaj +1 more source
Analysis of the phosphoproteome of CK2α(–/–)/Δα′ C2C12 myoblasts compared to the wild-type cells
CK2 is a Ser/Thr protein kinase composed of two catalytic (α/α′) subunits and a non-catalytic β-subunit dimer, whose activity is often abnormally high in cancer cells.
Christian Borgo+8 more
doaj +1 more source
The p110 delta structure: mechanisms for selectivity and potency of new PI(3)K inhibitors. [PDF]
Deregulation of the phosphoinositide-3-OH kinase (PI(3)K) pathway has been implicated in numerous pathologies including cancer, diabetes, thrombosis, rheumatoid arthritis and asthma.
Alex Berndt+16 more
core +2 more sources