Inhibitors of glucose transport and glycolysis as novel anticancer therapeutics

Qian, Yanrong

doi:10.5528/wjtm.v3.i2.37

Cited by 39 publications

(44 citation statements)

References 267 publications

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“…Of these, phlorizin, the first naturally occurring sodium glucose cotransport (SGLT) inhibitor, has been used to identify the SGLT mechanism (Vick, Diedrich, & Baumann, ). Following this, many natural product glucose transport inhibitors have been characterized, of which several compounds have been tested in vitro and in vivo, and in some cases have reached clinical trials as potential cancer chemotherapeutic agents (Blaschek, ; Choi, ; Granchi et al, ; Qian et al, ).…”

Section: Glucose Transport Inhibitors From Edible Plantsmentioning

confidence: 99%

“…GLUT1 has been found to be upregulated in the majority of cancer types, and GLUT2 expression is increased drastically in liver, pancreatic, gastric, and colon cancers. In addition, GLUT3 is upregulated in lung, neck, head, ovarian, breast, and bladder cancers, while GLUT4 is overexpressed in colon, lymphoid, breast, and pancreatic tumors (Macheda, Rogers, & Best, ; Qian, Wang, & Chen, ).…”

Section: Introduction and Significancementioning

confidence: 99%

“…In previous review articles, the overall information included on glucose transport and metabolism in cancer cells and the progress of new therapeutic developments for glucose transport inhibitors focused on small molecules, with only a limit number of natural products, were summarized (Qian et al, ). Natural product sodium glucose cotransporter (SGLT) inhibitors and their potential antidiabetic activity have been reviewed (Blaschek, ; Choi, ).…”

Section: Introduction and Significancementioning

confidence: 99%

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Plant‐derived glucose transport inhibitors with potential antitumor activity

Shriwas

Chen

Kinghorn

et al. 2019

Phytotherapy Research

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Glucose, a key nutrient utilized by human cells to provide cellular energy and a carbon source for biomass synthesis, is internalized in cells via glucose transporters that regulate glucose homeostasis throughout the human body. Glucose transporters have been used as important targets for the discovery of new drugs to treat cancer, diabetes, and heart disease, owing to their abnormal expression during these disease conditions. Thus far, several glucose transport inhibitors have been used in clinical trials, and increasing numbers of natural products have been characterized as potential anticancer agents targeting glucose transport. The present review focuses on natural product glucose transport inhibitors of plant origin, including alkaloids, flavonoids and other phenolic compounds, and isoprenoids, with their potential antitumor properties also discussed.

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Section: Glucose Transport Inhibitors From Edible Plantsmentioning

confidence: 99%

Section: Introduction and Significancementioning

confidence: 99%

Section: Introduction and Significancementioning

confidence: 99%

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Plant‐derived glucose transport inhibitors with potential antitumor activity

Shriwas

Chen

Kinghorn

et al. 2019

Phytotherapy Research

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“…[3] Extensive efforts have been made to discover new inhibitors of GLUTs,particularly GLUT1, as leads for developing novel anticancer drugs. [4] Although anumber of GLUT inhibitors have been reported, including BAY-876, [5] ap otent and isoform-specific GLUT1 inhibitor,n one has entered the clinic to date.…”

mentioning

confidence: 99%

Discovery of a Potent GLUT Inhibitor from a Library of Rapafucins by Using 3D Microarrays

et al. 2019

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Glucose transporters play an essential role in cancer cell proliferation and survival and have been pursued as promising cancer drug targets. Using microarrays of a library of new macrocycles known as rapafucins, which were inspired by the natural product rapamycin, we screened for new inhibitors of GLUT1. We identified multiple hits from the rapafucin 3D microarray and confirmed one hit as a bona fide GLUT1 ligand, which we named rapaglutin A (RgA). We demonstrate that RgA is a potent inhibitor of GLUT1 as well as GLUT3 and GLUT4, with an IC50 value of low nanomolar for GLUT1. RgA was found to inhibit glucose uptake, leading to a decrease in cellular ATP synthesis, activation of AMP‐dependent kinase, inhibition of mTOR signaling, and induction of cell‐cycle arrest and apoptosis in cancer cells. Moreover, RgA was capable of inhibiting tumor xenografts in vivo without obvious side effects. RgA could thus be a new chemical tool to study GLUT function and a promising lead for developing anticancer drugs.

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“…There are various metabolic inhibitors in the market currently undergoing testing in clinical trials 146 , however as of date, inhibitor of glucose transporters have not passed Phase II 147 . Notably, 2-DG has been tested in mouse models of SLE without toxicity 148,149 , and similarly in our study, mice fed orally with WZB117 were able to safely tolerant the drug throughout the course of our experiment.…”

Section: Chapter 31 Proposed Modelmentioning

confidence: 99%

Metabolic reprogramming of tumor-infiltrating myeloid cells conveys protection against pancreatic ductal adenocarcinoma

Sieow¹

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Inhibitors of glucose transport and glycolysis as novel anticancer therapeutics

Cited by 39 publications

References 267 publications

Plant‐derived glucose transport inhibitors with potential antitumor activity

Plant‐derived glucose transport inhibitors with potential antitumor activity

Discovery of a Potent GLUT Inhibitor from a Library of Rapafucins by Using 3D Microarrays

Metabolic reprogramming of tumor-infiltrating myeloid cells conveys protection against pancreatic ductal adenocarcinoma

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