PMID- 22961911 OWN - NLM STAT- MEDLINE DCOM- 20130709 LR - 20220408 IS - 1097-4644 (Electronic) IS - 0730-2312 (Linking) VI - 114 IP - 3 DP - 2013 Mar TI - Recent agents targeting HIF-1alpha for cancer therapy. PG - 498-509 LID - 10.1002/jcb.24390 [doi] AB - The discovery of hypoxia-inducible factor-1 (HIF-1) has led to an increasing understanding of the mechanism of tumor hypoxia in the past two decades. As a key transcriptional regulator, HIF-1 plays a central role in the adaptation of tumor cells to hypoxia by activating the transcription of targeting genes, which regulate several biological processes including angiogenesis, cell proliferation, survival, glucose metabolism and migration. The inhibitors of HIF-1 in cancer have provided us a new clue for the targeting cancer therapy. This review will introduce the general knowledge of the biology characteristic of HIF-1 and mechanism of O(2)-dependent regulation. Moreover, a number of chemical inhibitors plus protein and nucleic acid inhibitors are included and classified mainly based on their different mechanism of inhibiting action. We also prefer to discuss the advantages of protein and nucleic acid inhibitors compared with chemical inhibitors. CI - Copyright (c) 2012 Wiley Periodicals, Inc. FAU - Hu, Yaozhong AU - Hu Y AD - Department of Biochemical Engineering, School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, China. FAU - Liu, Jing AU - Liu J FAU - Huang, He AU - Huang H LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't PT - Review PL - United States TA - J Cell Biochem JT - Journal of cellular biochemistry JID - 8205768 RN - 0 (Antineoplastic Agents) RN - 0 (HIF1A protein, human) RN - 0 (Hypoxia-Inducible Factor 1, alpha Subunit) RN - 0 (Protein Kinase Inhibitors) RN - 0 (Repressor Proteins) RN - EC 1.- (Mixed Function Oxygenases) RN - EC 1.14.11.- (HIF1AN protein, human) RN - IY9XDZ35W2 (Glucose) SB - IM MH - Antineoplastic Agents/pharmacology/*therapeutic use MH - Cell Hypoxia MH - Cell Proliferation MH - Cell Survival MH - Gene Expression Regulation, Neoplastic MH - Glucose/metabolism MH - Humans MH - Hypoxia-Inducible Factor 1, alpha Subunit/*antagonists & inhibitors/chemistry/genetics/*metabolism MH - Mixed Function Oxygenases/metabolism MH - Molecular Targeted Therapy MH - Neoplasms/*drug therapy/metabolism MH - Neovascularization, Pathologic/*drug therapy MH - Protein Kinase Inhibitors/*metabolism MH - Repressor Proteins/metabolism MH - Transcription, Genetic EDAT- 2012/09/11 06:00 MHDA- 2013/07/10 06:00 CRDT- 2012/09/11 06:00 PHST- 2012/05/11 00:00 [received] PHST- 2012/08/30 00:00 [accepted] PHST- 2012/09/11 06:00 [entrez] PHST- 2012/09/11 06:00 [pubmed] PHST- 2013/07/10 06:00 [medline] AID - 10.1002/jcb.24390 [doi] PST - ppublish SO - J Cell Biochem. 2013 Mar;114(3):498-509. doi: 10.1002/jcb.24390.