title: Vitamin K(3) and K(5) are inhibitors of tumor pyruvate kinase M2.
abstract: Pyruvate kinase M2 (PKM2) is a rate-limiting enzyme of aerobic glycolysis in cancer cells and plays important roles in cancer metabolism and growth. Here we show that vitamin K(3) and K(5) (VK(3) and VK(5)) are relatively specific PKM2 inhibitors. VK(3) and VK(5) showed a significantly stronger potency to inhibit PKM2 than to inhibit PKM1 and PKL, 2 other isoforms of PK dominantly expressed in most adult tissues and liver. This study combined with previous reports supports that VK(3) and VK(5) have potential as adjuvant for cancer chemotherapy.
authors.affiliation: Cancer Institute a Key Laboratory for Cancer Prevention & Intervention, National Ministry of Education, The Second Affiliated Hospital, Zhejiang University School of Medicine, Hangzhou, Zhejiang, China.
authors.forename: Jing
authors.initials: J
authors.lastname: Chen
authors.forename: Zheng
authors.initials: Z
authors.lastname: Jiang
authors.forename: Beibei
authors.initials: B
authors.lastname: Wang
authors.forename: Yanguang
authors.initials: Y
authors.lastname: Wang
authors.forename: Xun
authors.initials: X
authors.lastname: Hu
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology*; D002352:Carrier Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D045744:Cell Line, Tumor; D005947:Glucose / Q000378:metabolism; D006367:HeLa Cells; D006801:Humans; D019344:Lactic Acid / Q000378:metabolism; D008565:Membrane Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D009369:Neoplasms / Q000188:drug therapy*; D047428:Protein Kinase Inhibitors / Q000494:pharmacology*; D013963:Thyroid Hormones / Q000378:metabolism; D024483:Vitamin K 3 / Q000031:analogs & derivatives* / Q000494:pharmacology*; D000097810:Thyroid Hormone-Binding Proteins
chemical_list: D000970:Antineoplastic Agents; D002352:Carrier Proteins; D005947:Glucose; D019344:Lactic Acid; D008565:Membrane Proteins; D047428:Protein Kinase Inhibitors; D013963:Thyroid Hormones; D024483:Vitamin K 3; D000097810:Thyroid Hormone-Binding Proteins; C024534:vitamin k5