title: Glycolysis Inhibitors for Anticancer Therapy: A Review of Recent Patents.
abstract: BACKGROUND
  The aerobic glycolysis in tumor cells known as Warburg effect is one of the most important hallmarks of cancer. It is proposed that the upregulation of the series of metabolic enzymes along the glycolytic pathway may contribute to the Warburg effect.
  
  
  OBJECTIVE
  The inhibition of these glycolytic enzymes has been found to be a novel strategy for anticancer treatment. This review summaries recent patents in the development of small molecule inhibitors for the key enzymes in tumor glycolysis. The targeted enzymes are GLUTs, HKs, PFK, PGAM1, PKM2, LDHA, MCTs and PDK.
  
  
  CONCLUSIONS
  Although most inhibitors are still in the preclinical phase, the inhibition of glycolytic enzymes represents a very promising approach for anticancer treatment. The future development could be more focused on the discovery of new metabolic enzyme that is specifically expressed in tumor cells.
authors.affiliation: Department of Chemistry, Purdue University, 560 Oval Drive, West Lafayette, IN 47906, USA. weijuantang@gmail.com.
authors.forename: Huaming
authors.initials: H
authors.lastname: Sheng
authors.forename: Weijuan
authors.initials: W
authors.lastname: Tang
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000627:therapeutic use*; D055808:Drug Discovery; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000627:therapeutic use*; D051246:Glucose Transport Proteins, Facilitative / Q000037:antagonists & inhibitors / Q000378:metabolism; D006019:Glycolysis / Q000187:drug effects*; D006593:Hexokinase / Q000037:antagonists & inhibitors / Q000378:metabolism; D006801:Humans; D015394:Molecular Structure; D058990:Molecular Targeted Therapy; D009369:Neoplasms / Q000188:drug therapy* / Q000201:enzymology / Q000473:pathology; D010330:Patents as Topic; D025221:Phosphofructokinases / Q000037:antagonists & inhibitors / Q000378:metabolism; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors / Q000378:metabolism; D000081382:Pyruvate Dehydrogenase Acetyl-Transferring Kinase; D011770:Pyruvate Kinase / Q000037:antagonists & inhibitors / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D051246:Glucose Transport Proteins, Facilitative; D000081382:Pyruvate Dehydrogenase Acetyl-Transferring Kinase; D025221:Phosphofructokinases; D006593:Hexokinase; D011770:Pyruvate Kinase; D017346:Protein Serine-Threonine Kinases