2019
DOI: 10.1016/j.ejmech.2019.01.085
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Synthesis and biological evaluation of anthraquinone derivatives as allosteric phosphoglycerate mutase 1 inhibitors for cancer treatment

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Cited by 27 publications
(25 citation statements)
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“…In this study, we investigate the function of PGAM1 in various types of cancer. PGAM1 is a glycolytic enzyme in nature that catalyzes the conversion of 2-phosphoglycerate and 3-phosphoglycerate [ 35 ]. PGAM1 overexpression in both 2PG and 3PG has additional biological functions and is affected in the anabolic condition.…”
Section: Resultsmentioning
confidence: 99%
“…In this study, we investigate the function of PGAM1 in various types of cancer. PGAM1 is a glycolytic enzyme in nature that catalyzes the conversion of 2-phosphoglycerate and 3-phosphoglycerate [ 35 ]. PGAM1 overexpression in both 2PG and 3PG has additional biological functions and is affected in the anabolic condition.…”
Section: Resultsmentioning
confidence: 99%
“…N‐(1‐Hydroxy‐7‐nitro‐9‐oxo‐9H‐xanthen‐3‐yl)‐[1, 10‐biphenyl]‐4‐sulfonamide has been recently found as effective PGAM1 inhibitor with IC 50 value of 2.1 μM that is fivefold more potent than PGMI‐004A with effective antiproliferative activity against H1299 cells . A novel anthraquinone derivative was found to be most potent among known inhibitors of PGAM1 having EC 50 value of 97 nM with effective inhibitory potential against tumor growth in xenografted H1229 mouse model with no distant toxicity …”
Section: Pharmacological Inhibitors Of Pgam1mentioning
confidence: 99%
“…39 A novel anthraquinone derivative was found to be most potent among known inhibitors of PGAM1 having EC 50 value of 97 nM with effective inhibitory potential against tumor growth in xenografted H1229 mouse model with no distant toxicity. 49 EGCG is an important natural catechin that is obtained from green tea and discovered as potential PGAM1 inhibitor. (C) Xanthon EGCG attenuates glycolysis and oxidative PPP by reducing the intracellular level of 2-PG at 1 μM concentration.…”
Section: Pharmacological Inhibitors Of Pgam1mentioning
confidence: 99%
“…PGAM1 is over expressed in numerous kinds of aggressive human cancers mainly breast, prostate, lung, colorectal, hepatocellular carcinoma and pancreatic ductal adenocarcinoma (Sharif et al, 2019). Previous studies have also demonstrated that PGAM1-mediated glycolysis plays critical role in tumor development, survival, and migration of cancer cells (Huang et al, 2019), thus, PGAM1 inhibition has potential to kill cancer cells selectively.…”
Section: Introductionmentioning
confidence: 99%