Hypoxia-inducible factor-1α: A promising therapeutic target for vasculopathy in diabetic retinopathy

• Currently, diabetic retinopathy is one of the major blinding eye diseases, and one of its main pathologies is abnormal proliferation of blood vessels in the eye. • HIF-1α functions more widely than VEGF, thus blocking HIF-1α better therapeutic effect than blocking VEGF may occur. • And current study also found that some small molecules that inhibit HIF-1α have a better effect than VEGF inhibitors. • In this review, HIF-1α was introduced in terms of its mechanism of action in diabetic retinopathy and its inhibitors, which provided a new therapeutic idea for the treatment of diabetic retinopathy. Diabetic retinopathy (DR) is a serious condition that can cause blindness in diabetic patients. It is a neurovascular disease, but the pathogenesis leading to the onset of this disease is still not completely understood. However, hypoxia with subsequent neovascularization is a characteristic phenomenon observed with DR. Cellular response to hypoxia is mediated by the transcriptional regulator hypoxia-inducible factor (HIF). Long-term research has shown that one isotype of HIF, HIF-1α, may play a pivotal role under hypoxic conditions, and an increasing number of studies have shown that HIF-1α and its target genes contribute to retinal neovascularization. Therefore, targeting HIF-1α may lead to more effective DR treatments. This review describes the possible mechanisms of HIF-1α in neovascularization of DR. Furthermore, various inhibitors of HIF-1α that may have viable potential in the treatment of DR are also discussed.