... with other roles such as cell signalling. Intriguingly, NQO2 has been identified as an off-target interactor with over 30 kinase inhibitors and other drugs and natural products. The interaction between NQO2 and kinase-targeted drugs is particularly intriguing because it suggests that NQO2 may be contributing...

... to as pseudokinases. The kinase family framework provided in that 2002 review is in widespread use today. The history of kinase inhibitor discovery parallels the timeline of new kinase revelations, as the therapeutic potential of kinase inhibition was recognized at an early stage. In this introduction, we...

... using a mouse cell line expressing an MLKL mutant that kills cells in the absence of upstream death or pathogen detector receptor activation. This screen identified the vascular endothelial growth factor receptor (VEGFR) and platelet-derived growth factor receptor (PDGFR) tyrosine kinase inhibitor, ABT...

... and MLi-2) and Type II (GZD-824, Rebastinib and Ponatinib) kinase inhibitors that bind to the closed or open conformations of the LRRK2 kinase domain, respectively. We show that Type I and Type II inhibitors suppress phosphorylation of Rab10 and Rab12, key physiological substrates of LRRK2 and also...

... of ULK1/2 dual inhibitors with improved selectivity for future exploitation of autophagy inhibition. © 2019 The Author(s). Published by Portland Press Limited on behalf of the Biochemical Society 2019 autophagy crystallography kinase inhibitor protein kinase ULK1 ULK2...

... the tyrosine sulfation of synthetic fluorescent peptides can be rapidly quantified. We exploit ligand binding and inhibitor screens to uncover a susceptibility of TPST1 and TPST2 to different classes of small molecules, including the anti-angiogenic compound suramin and the kinase inhibitor rottlerin...

... to be linked to toxicity, and thus the thrust of pharmaceutical effort has focused on developing LRRK2 kinase inhibitors. However, recent data have suggested that inhibition of LRRK2 activity results in reduced LRRK2 levels and peripheral side effects, which are similar to those observed in homozygous LRRK2...

.... kinase kinase inhibitor Parkinson's disease phosphatase ubiquitin Parkinson's disease (PD) is a progressive neurodegenerative disorder with no known cure. PD is typically of idiopathic origin; however, it has been established that environmental exposures to toxins and inheritance of dominant...

... release and chemotaxis. ITK is an attractive target for the treatment of T-cell-mediated inflammatory diseases. In the present study we describe the discovery of kinase inhibitors that preferentially bind to an allosteric pocket of ITK. The novel ITK allosteric site was characterized by NMR, surface...

... regulator of clathrin-coated vesicle trafficking and plays a central role during development. Additionally, due to the unusually high plasticity of its catalytic domain, it is a frequent ‘off-target’ of clinical kinase inhibitors associated with respiratory side effects of these drugs. In the present paper...

... (liver kinase B1) tumour suppressor kinase. Recent work suggests they play important roles in regulating key biological processes including Myc-driven tumorigenesis, senescence, cell adhesion and neuronal polarity. In the present paper we describe the first highly specific protein kinase inhibitors...

... 2013 © The Authors Journal compilation © 2013 Biochemical Society 2013 kinase activator kinase inhibitor kinase reporter phorbol ester protein kinase C (PKC) PKC (protein kinase C) isoenzymes transduce a wide range of extracellular signals that result in the generation...

... developing PI3K and TOR inhibitors. 2 To whom correspondence should be addressed (email [email protected] ). 29 11 2011 8 12 2011 14 12 2011 © The Authors Journal compilation © 2012 Biochemical Society 2012 autoimmunity cancer kinase inhibitor leukaemia lymphocyte...

... 3 2011 4 4 2011 © The Authors Journal compilation © 2011 Biochemical Society 2011 cell differentiation embryonic stem cell (ESC) kinase inhibitor leukaemia inhibitory factor (LIF) protein phosphorylation signal transducer and activator of transcription 3 (STAT3) ESCs...

... 2011 kinase inhibitor phosphoinositide 3-kinase (PI3K) ribosomal S6 kinase (RSK) p70 ribosomal S6 kinase (S6K) serum- and glucocorticoid-induced protein kinase (SGK) Given the unique position of PDK1 upstream of many protein kinases, a selective PDK1 inhibitor would be a valuable research...

.../Akt1 cancer kinase inhibitor 3-phosphoinositide-dependent protein kinase (PDK1) phosphoinositide 3-kinase (PI3K) p90 ribosomal S6 kinase (RSK) p70 ribosomal S6 kinase (S6K) serum- and glucocorticoid-induced protein kinase (SGK) PDK1 (3-phosphoinositide-dependent protein kinase 1) plays...

... (phosphoinositide-dependent kinase 1) via its PIF pocket and subsequently the T-loop (Thr 229 in S6K1) is phosphorylated [ 13 ]. Akt/protein kinase B (PKB) cancer kinase inhibitor phosphoinositide 3-kinase (PI3K) p70 ribosomal S6 kinase (S6K) serum- and glucocorticoid-induced protein kinase (SGK...

... in this issue of the Biochemical Journal , Nichols et al. have developed an extensive set of molecular tools, including an optimized peptide substrate for determining in vitro kinase activity of LRRK2, a set of kinase inhibitors that can be used to explore LRRK2 substrate specificity and biology, a much-needed...

... of the Creative Commons Attribution Non-Commercial Licence ( http://creativecommons.org/licenses/by-nc/2.5/ ) which permits unrestricted non-commercial use, distribution and reproduction in any medium, provided the original work is properly cited. Akt/protein kinase B (PKB) cancer kinase inhibitor...

... phosphorylation of the C-terminal regulatory sites Tyr-497 and Tyr-504 was obtained, nor was there any indication of in vitro regulation of FRK/RAK kinase activity. Screening a panel of known tyrosine kinase inhibitors for their ability to inhibit FRK/RAK revealed several compounds that inhibited FRK/RAK...