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. 2023 Nov 20;120(48):e2310522120. doi: 10.1073/pnas.2310522120

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Copyright © 2023 the Author(s). Published by PNAS.

This open access article is distributed under Creative Commons Attribution License 4.0 (CC BY).

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Fig. 3. — BGC HX1012/HX1035-derived metabolites are ATP-competitive CDK inhibitors. (A) Neighbor-joining phylogenetic tree of A. uvarum RosG and human CDK enzymes with 1,000 bootstrap values. GSK3α is the outgroup. (B) Inhibition of CDK2/cyclin E1 phosphorylation of histone H1 with BGC HX1012/HX1035-derived metabolites. Data represent the average ± the SD of the mean, n = 3. ND = not determined; inhibition did not exceed 50% at the highest concentration tested (100 µM). STS, staurosporine. (C) Potency of 1 in CDK2/cyclin E1 biochemical assay with varying concentrations of adenosine 5′-triphosphate (ATP). Data represent the average ± the SD of the mean, n = 4. (D) Lineweaver-Burk plot of 1 vs. different concentrations of ATP for CDK2/cyclin E1. A zoomed-in view of the plot is displayed in the dashed box. Data represent the average ± the SD of the mean, n ≥ 2.