Corticotropin-releasing factor-induced adrenocorticotropin hormone release and synthesis is blocked by incorporation of the inhibitor of cyclic AMP-dependent protein kinase into anterior pituitary tumor cells by liposomes. [PDF]
, 1985 Terry Reisine +3 more
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Molecular Oncology, EarlyView.Loss of primary cilia in endothelial cells promotes EndMT and vascular abnormalities in the ovarian tumor microenvironment through EphA2 activation. Using human samples, in vitro models, and endothelial‐specific Kif3a‐knockout mice, we show that primary cilia loss drives the acquisition of cancer‐associated fibroblast‐like phenotypes, thereby ...
Jin Gu Cho +11 more
wiley +1 more source
Pharmacology Of Protein Kinase Inhibitors
Annual Review of Pharmacology and Toxicology, 1992 Ryoji Kobayashi, Hiroyoshi Hidaka
openaire +5 more sources
Prolonged and tunable residence time using reversible covalent kinase inhibitors. [PDF]
, 2015 Drugs with prolonged on-target residence times often show superior efficacy, yet general strategies for optimizing drug-target residence time are lacking.
Angelina Bisconte +23 more
core
Inhibition of human neutrophil chemotaxis by the protein kinase inhibitor, 1-(5-isoquinolinesulfonyl) piperazine. [PDF]
, 1987 Liana Harvath +3 more
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Genomics‐led approach to drug testing in models of undifferentiated pleomorphic sarcoma
Molecular Oncology, EarlyView.GA text Genomic data from undifferentiated pleomorphic sarcoma patients and preclinical models were used to inform a targeted drug screen. Selected compounds were tested in 2D and 3D cultures of UPS cell lines. A combination of trametinib and infigratinib was synergistic in the majority of UPS cell lines tested, which was further confirmed in an ex ...
Piotr J. Manasterski +19 more
wiley +1 more source
Primary-structure requirements for inhibition by the heat-stable inhibitor of the cAMP-dependent protein kinase. [PDF]
, 1986 John D. Scott +3 more
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Molecular Oncology, EarlyView.This study identifies nuclear YB‐1 S102 phosphorylation as a marker associated with KRAS and FBXW7 mutations in colorectal cancer. Mutated KRAS correlates specifically with nuclear, not cytoplasmic, S102 YB‐1. These findings provide the first ex vivo evidence of this link in CRC and suggest future studies should assess the prognostic and therapeutic ...
Konstanze Lettau +9 more
wiley +1 more source
Systematic Analysis of Covalent and Allosteric Protein Kinase Inhibitors. [PDF]
Molecules, 2023 Xerxa E, Laufkötter O, Bajorath J.
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A nucleotide‐independent, pan‐RAS‐targeted DARPin elicits anti‐tumor activity in a multimodal manner
Molecular Oncology, EarlyView.We report a Designed Ankyrin Repeat Protein that binds and inhibits RAS proteins, which serve as central cell signaling hubs and are essential for the progression of many cancers. Its unique feature is that it does not discriminate between different RAS isoforms or mutations and is capable of binding to RAS in both its active (GTP‐bound) and inactive ...
Jonas N. Kapp +13 more
wiley +1 more source