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. 2020 Apr 8;12(4):913. doi: 10.3390/cancers12040913

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© 2020 by the authors.

Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).

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Phosphoglycerate kinase 1 (PGK1) is a potential cellular target for the antiglycolytic effect of gracillin. (A) The effect of gracillin on glucose uptake was determined by flow cytometric analysis of 2-deoxy-D-glucose (2-NBDG)-treated cells in the presence or absence of gracillin. (B) Schematic diagram illustrating the glycolysis pathway. (C) The effect of gracillin on the mRNA expression of GAPDH and PGK1 was determined by real-time PCR. (D) Docking analysis of the interaction between gracillin and three glycolysis-associated enzymes (GAPDH and PGK1) using SwissDock. (E) The inhibitory effect of gracillin on PGK1 activity with minimal modulation of GAPDH activity was determined as described in Materials and Methods. The bars represent the mean ± SD; * p < 0.05, ** p < 0.01, and *** p < 0.001, as determined by a two-tailed Student’s t-test by comparison with the vehicle-treated control group. Con: control; GRA: gracillin.