Results 31 to 40 of about 88,066 (234)
Structural insights into characterizing binding sites in EGFR kinase mutants [PDF]
Journal of Chemical Information and Modeling, 2018, 2018 Over the last two decades epidermal growth factor receptor (EGFR) kinase has become an important target to treat non-small cell lung cancer (NSCLC). Currently, three generations of EGFR kinase-targeted small molecule drugs have been FDA approved. They nominally produce a response at the start of treatment and lead to a substantial survival benefit for ...
arxiv +1 more source
Cyclin-dependent kinases: a family portrait [PDF]
Nature Cell Biology, 2009 To the Editor, Cyclin-dependent kinases (CDKs) are protein kinases involved in critical cellular processes, such as cell cycle or transcription, whose activity requires association with specific cyclin subunits. Based on sequence similarity, the human genome contains 21 genes encoding CDKs and five additional genes encoding a more distant group of ...
Tony Hunter +8 more
openaire +3 more sources
Palbociclib-mediated cell cycle arrest can occur in the absence of the CDK inhibitors p21 and p27
Open Biology, 2021 The use of CDK4/6 inhibitors in the treatment of a wide range of cancers is an area of ongoing investigation. Despite their increasing clinical use, there is limited understanding of the determinants of sensitivity and resistance to these drugs.
Betheney R. Pennycook, Alexis R. Barr
doaj +1 more source
Inferring the Sign of Kinase-Substrate Interactions by Combining Quantitative Phosphoproteomics with a Literature-Based Mammalian Kinome Network [PDF]
, 2010 Protein phosphorylation is a reversible post-translational modification commonly used by cell signaling networks to transmit information about the extracellular environment into intracellular organelles for the regulation of the activity and sorting of proteins within the cell.
arxiv +1 more source
Advance in Reversible Covalent Kinase Inhibitors [PDF]
arXiv, 2021 Reversible covalent kinase inhibitors (RCKIs) are a class of novel kinase inhibitors attracting increasing attention because they simultaneously show the selectivity of covalent kinase inhibitors, yet avoid permanent protein-modification-induced adverse effects.
arxiv
Targeting Cyclin-Dependent Kinases for Treatment of Gynecologic Cancers
Frontiers in Oncology, 2018 Ovarian, uterine/endometrial, and cervical cancers are major gynecologic malignancies estimated to cause nearly 30,000 deaths in 2018 in US. Defective cell cycle regulation is the hallmark of cancers underpinning the development and progression of the ...
Z. Ping Lin +2 more
doaj +1 more source
Using the structural kinome to systematize kinase drug discovery [PDF]
arXiv, 2021 Kinase-targeted drug design is challenging. It requires designing inhibitors that can bind to specific kinases when all kinase catalytic domains share a common folding scaffold that binds ATP. Thus, obtaining the desired selectivity, given the whole human kinome, is a fundamental task during early-stage drug discovery.
arxiv
A knowledge graph representation learning approach to predict novel kinase-substrate interactions [PDF]
arXiv, 2022 The human proteome contains a vast network of interacting kinases and substrates. Even though some kinases have proven to be immensely useful as therapeutic targets, a majority are still understudied. In this work, we present a novel knowledge graph representation learning approach to predict novel interaction partners for understudied kinases.
arxiv
CDK12: A Potent Target and Biomarker for Human Cancer Therapy
Cells, 2020 Cyclin-dependent kinases (CDKs) are a group of serine/threonine protein kinases and play crucial roles in various cellular processes by regulating cell cycle and gene transcription.
Shujing Liang +6 more
doaj +1 more source
Frontiers in Pharmacology, 2021 Phenazopyridine is a widely used drug against urinary tract pain. The compound has also been shown to enhance neural differentiation of pluripotent stem cells. However, its mechanism of action is not understood.
Olivier Preynat-Seauve +11 more
doaj +1 more source