Dynamic and multi-pharmacophore modeling for designing polo-box domain inhibitors. [PDF]
, 2014 The polo-like kinase 1 (Plk1) is a critical regulator of cell division that is overexpressed in many types of tumors. Thus, a strategy in the treatment of cancer has been to target the kinase activity (ATPase domain) or substrate-binding domain (Polo-box
Lee, Keun Woo +4 more
core +3 more sources
Mediators of Inflammation, 2000 The effect of various phospholipase A2 and protein kinase inhibitors on the arachidonic acid liberation in bovine platelets induced by the protein kinase activator 12-O-tetradecanoylphorbol–13-acetate (TPA) was studied.
M. Lehr, K. Griessbach
doaj +1 more source
Kinase-targeted cancer therapies: progress, challenges and future directions
Molecular Cancer, 2018 The human genome encodes 538 protein kinases that transfer a γ-phosphate group from ATP to serine, threonine, or tyrosine residues. Many of these kinases are associated with human cancer initiation and progression.
Khushwant S. Bhullar +6 more
doaj +1 more source
Ubiquitylation in immune disorders and cancer: from molecular mechanisms to therapeutic implications [PDF]
, 2012 Conjugation of ubiquitin to proteins (ubiquitylation) has emerged to be one of the most crucial post-translational modifications controlling virtually all cellular processes.
Fulda, Simone +2 more
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Biological aspects of mTOR in leukemia [PDF]
, 2018 The mammalian target of rapamycin (mTOR) is a central processor of intra-and extracellular signals, regulating many fundamental cellular processes such as metabolism, growth, proliferation, and survival.
Bianchi, Mp +5 more
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GSK3-mediated raptor phosphorylation supports amino acid-dependent Q2 mTORC1-directed signalling [PDF]
, 2015 The mammalian or mechanistic target of rapamycin (mTOR) complex 1 (mTORC1) is a ubiquitously expressed multimeric protein kinase complex that integrates nutrient and growth factor signals for the co-ordinated regulation of cellular metabolism and cell ...
Alan Prescott +60 more
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1,2,6-thiadiazinones as novel narrow spectrum calcium/calmodulin-dependent protein kinase kinase 2 (CaMKK2) inhibitors [PDF]
, 1983 We demonstrate for the first time that 4H-1,2,6-thiadiazin-4-one (TDZ) can function as a chemotype for the design of ATP-competitive kinase inhibitors. Using insights from a co-crystal structure of a 3,5-bis(arylamino)-4H-1,2,6-thiadiazin-4-one bound to ...
Asquith, Christopher R.M. +11 more
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Rapid evolution of protein kinase PKR alters sensitivity to viral inhibitors. [PDF]
, 2009 Protein kinase PKR (also known as EIF2AK2) is activated during viral infection and phosphorylates the alpha subunit of eukaryotic translation initiation factor 2 (eIF2), leading to inhibition of translation and viral replication. We report fast evolution
Dever, Thomas E +4 more
core
DNA dependent protein kinase (DNA-PK) enhances HIV transcription by promoting RNA polymerase II activity and recruitment of transcription machinery at HIV LTR. [PDF]
, 2020 Despite reductions in mortality from the use of highly active antiretroviral therapy (HAART), the presence of latent or transcriptionally silent proviruses prevents HIV cure/eradication.
Bukrinsky, Michael +10 more
core +2 more sources
Specific inhibition of AGC protein kinases by antibodies against C-terminal epitopes [PDF]
, 2004 The sequences contributing to the catalytic site of protein kinases are not all comprised within the highly conserved catalytic core. Thus, in mammalian cAMP-dependent protein kinase (PKA), the C-terminal sequence participates in substrate binding. Using
Giacomoni, Véronique +2 more
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