| 靶标 | Hypoxia-inducible factor 1-alpha, HIF-1-alpha, HIF1-alpha, ARNT-interacting protein, Basic-helix-loop-helix-PAS protein MOP1, Class E basic helix-loop-helix protein 78, bHLHe78, Member of PAS protein 1, PAS domain-containing protein 8, HIF1A |
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| 背景 | Hypoxia-inducible factor 1-alpha (HIF1A) is a ~92 kDa protein. Functions as a master transcriptional regulator of the adaptive response to hypoxia. Under hypoxic conditions, activates the transcription of over 40 genes, including erythropoietin, glucose transporters, glycolytic enzymes, vascular endothelial growth factor, HILPDA, and other genes whose protein products increase oxygen delivery or facilitate metabolic adaptation to hypoxia. Plays an essential role in embryonic vascularization, tumor angiogenesis and pathophysiology of ischemic disease. Heterodimerizes with ARNT; heterodimer binds to core DNA sequence 5'-TACGTG-3' within the hypoxia response element (HRE) of target gene promoters. Activation requires recruitment of transcriptional coactivators such as CREBBP and EP300. 1. Jaakkola, P. et al. (2001) Science (New York, N.Y.) 292, 468-72. PMID: 112928612. Masson, N. et al. (2001) The EMBO journal 20, 5197-206. PMID: 115668833. Bae, SH. et al. (2004) Biochemical and biophysical research communications 324, 394-400. PMID: 154650324. Choi, SM. et al. (2006) The Journal of biological chemistry 281, 34056-63. PMID: 169736225. Berta, MA. et al. (2007) Biochemical and biophysical research communications 360, 646-52. PMID: 176108436. Kim, EJ. et al. (2008) Arteriosclerosis, thrombosis, and vascular biology 28, 1796-802. PMID: 186580467. Gimm, T. et al. (2010) FASEB journal : official publication of the Federation of American Societies for Experimental Biology 24, 4443-58. PMID: 206249288. Shan, B. et al. (2012) Endocrine-related cancer 19, 13-27. PMID: 2200979710. Bhattacharya, S. et al. (1999) Genes & development 13, 64-75. PMID: 9887100 |
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