PXD017819-2

PXD017819 is an original dataset announced via ProteomeXchange.

Title	Esculetin inhibits cancer cell glycolysis by binding tumor PGK2, GPD2, and GPI
Description	Glycolysis can improve the tolerance of tissue cells to hypoxia, and its intermediates provide raw materials for the synthesis and metabolism of the tumor cells. If it can inhibit the activity of glycolysis-related enzymes and control the energy metabolism of tumor, it can be targeted for the treatment of malignant tumor. The target proteins phosphoglycerate kinase 2 (PGK2), glycerol-3-phosphate dehydrogenase (GPD2) and glucose-6-phosphate isomerase (GPI) were screened by combining transcriptome, proteomics and reverse docking. We detected the binding constant of the active compound using microscale thermophoresis (MST). It was found that esculetin bound well with three potential target proteins. Esculetin significantly inhibited the rate of glycolysis, manifested by differences of cellular lactate production and glucose consumption in HepG2 cells with or without esculetin. It was found that GPD2 bound strongly to GPI, revealing the direct interaction between the two glycolysis-related proteins. Animal tests have further demonstrated that esculetin may have anticancer effects by affecting the activity of PGK2, GPD2 and GPI. The results of this study demonstrated that esculetin can affect the glucose metabolism by binding to glycolytic proteins, thus playing an anti-tumor role, and these proteins which have direct interactions are potential novel targets for tumor treatment by esculetin.
HostingRepository	PRIDE
AnnounceDate	2020-03-03
AnnouncementXML	Submission_2020-04-30_03:28:55.xml
DigitalObjectIdentifier
ReviewLevel	Peer-reviewed dataset
DatasetOrigin	Original dataset
RepositorySupport	Unsupported dataset by repository
PrimarySubmitter	Songtao Wu
SpeciesList	scientific name: Homo sapiens (Human); NCBI TaxID: 9606;
ModificationList	No PTMs are included in the dataset
Instrument	LTQ

Revision	Datetime	Status	ChangeLog Entry
0	2020-03-02 02:47:50	ID requested
1	2020-03-03 02:06:31	announced
⏵ 2	2020-04-30 03:32:05	announced	2020-04-30: Updated publication reference for PubMed record(s): 32292350.

Wu ST, Liu B, Ai ZZ, Hong ZC, You PT, Wu HZ, Yang YF, Esculetin Inhibits Cancer Cell Glycolysis by Binding Tumor PGK2, GPD2, and GPI. Front Pharmacol, 11():379(2020) [pubmed]

submitter keyword: Keywords: glycolysis, esculetin, proteomics, microscale thermophoresis, transcriptome, protein inhibitor, GPD2/GPI.

Song-Tao Wu
contact affiliation	Faculty of Pharmacy, Hubei University of Chinese Medicine
contact email	songt1wu@163.com
lab head
Songtao Wu
contact affiliation	Faculty of Pharmacy, Hubei University of Chinese Medicine
contact email	songt1wu@163.com
dataset submitter

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PRIDE project URI

• PRIDE
  1. PXD017819
     1. Label: PRIDE project
     2. Name: Esculetin inhibits cancer cell glycolysis by binding tumor PGK2, GPD2, and GPI