Structural determinants of phosphoinositide 3-kinase inhibition by wortmannin, LY294002, quercetin, myricetin, and staurosporine.

By E. H. Walker, Michael E. Pacold, O. Perisic, L. Stephens, P. Hawkins, M. Wymann, Roger L. Williams. Molecules and Cells, 2000

1,181 citations recorded by the source corpus.

Subfields: Genetics, Molecular Biology

View Paper: https://www.semanticscholar.org/paper/9aad0cb7ae26c330d12bffa2cbff170abcaf095a

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Citations in the corpus

Protein-binding assays in biological liquids using microscale thermophoresis. (2010, result): “We found an affinity of 130±35 nM, which is in good agreement with the literature, where affinities of quercetin for various kinases are reported in the nanomolar to micromolar rang”
Targeting polo-like kinase 1 for cancer therapy (2006, background): “Previous experiments have demonstrated that wortmannin covalently modifies the Lys-833 residue of PI3K to form an irreversible adduc”
Plant Secondary Metabolite Biosynthesis and Transcriptional Regulation in Response to Biotic and Abiotic Stress Conditions (2021, background): “For example, they can alter key cellular enzymatic functions because of their anti-inflammatory, antioxidative, anticarcinogenic, and antimutagenic properties, and they are efficient inhibitors of numerous enzymes [18].”
A Pharmacological Map of the PI3-K Family Defines a Role for p110α in Insulin Signaling (2006, positive): “PIK-90 and PIK-93 both make a hydrogen bond to the backbone amide nitrogen of Val 882 (Figure 2D), an interaction conserved among all known PI3-K inhibitors (Walker et al., 2000).”
The Mechanism of Double-Strand DNA Break Repair by the Nonhomologous DNA End Joining Pathway (2010, background): “Ku is a toroidal protein because of its crystal structure (30).”
PI3K pathway alterations in cancer: variations on a theme (2008, neutral): “Like the majority of protein kinase inhibitors, all existing PI3K inhibitors bind competitively in the ATP-binding pocket of the catalytic domain.”
Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity (2008, methodology): “PI3K-inhibitors for which X-ray cocrystal structures exist (25).”