Division of Pharmaceutical Sciences, School of Pharmacy, University of Missouri-Kansas City, 2464 Charlotte Street, Kansas City, MO 64108-2718, USA.
Curr Drug Targets. 2013 Jul;14(8):919-35. doi: 10.2174/13894501113149990015.
Constant oxygen supply is essential for proper tissue development, homeostasis and function of all eukaryotic organisms. Cellular response to reduced oxygen levels is mediated by the transcriptional regulator hypoxia-inducible factor-1 (HIF-1). It is a heterodimeric complex protein consisting of an oxygen dependent subunit (HIF-1α) and a constitutively expressed nuclear subunit (HIF-1β). In normoxic conditions, de novo synthesized cytoplasmic HIF-1α is degraded by 26S proteasome. Under hypoxic conditions, HIF-1α is stabilized, binds with HIF-1β and activates transcription of various target genes. These genes play a key role in regulating angiogenesis, cell survival, proliferation, chemotherapy, radiation resistance, invasion, metastasis, genetic instability, immortalization, immune evasion, metabolism and stem cell maintenance. This review highlights the importance of hypoxia signaling in development and progression of various vision threatening pathologies such as diabetic retinopathy, retinopathy of prematurity, age-related macular degeneration and glaucoma. Further, various inhibitors of HIF-1 pathway that may have a viable potential in the treatment of oxygen-dependent ocular diseases are also discussed.
持续的氧气供应对于所有真核生物的组织发育、内稳态和功能至关重要。细胞对低氧水平的反应是由转录调节因子缺氧诱导因子-1(HIF-1)介导的。它是一种由氧依赖性亚基(HIF-1α)和组成型表达的核亚基(HIF-1β)组成的异二聚体复合物蛋白。在常氧条件下,新合成的细胞质 HIF-1α 被 26S 蛋白酶体降解。在低氧条件下,HIF-1α 稳定,与 HIF-1β 结合并激活各种靶基因的转录。这些基因在调节血管生成、细胞存活、增殖、化疗、辐射抗性、侵袭、转移、遗传不稳定性、永生化、免疫逃逸、代谢和干细胞维持方面发挥着关键作用。本综述强调了缺氧信号在各种威胁视力的疾病(如糖尿病视网膜病变、早产儿视网膜病变、年龄相关性黄斑变性和青光眼)的发展和进展中的重要性。此外,还讨论了各种可能对治疗依赖氧的眼部疾病具有潜在可行的 HIF-1 通路抑制剂。