Department of Ophthalmology, Eugene and Marilyn Glick Eye Institute, Indiana University, Indianapolis, IN, USA.
Preclinical and Clinical Development, Clearside Biomedical, Inc, Alpharetta, GA, USA.
Expert Opin Biol Ther. 2021 May;21(5):603-613. doi: 10.1080/14712598.2021.1856365. Epub 2020 Dec 16.
In the retina, noncoding RNA (ncRNA) plays an integral role in regulating apoptosis, inflammatory responses, visual perception, and photo-transduction, with altered levels reported in diseased states.
MicroRNA (miRNA), a class of ncRNA, regulates post-transcription gene expression through the binding of complementary sites of target messenger RNA (mRNA) with resulting translational repression. Small-interfering RNA (siRNA) is a double-stranded RNA (dsRNA) that regulates gene expression, leading to selective silencing of genes through a process called RNA interference (RNAi). Another form of RNAi involves short hairpin RNA (shRNA). In age-related macular degeneration (AMD) and diabetic retinopathy (DR), miRNA has been implicated in the regulation of angiogenesis, oxidative stress, immune response, and inflammation.
Many RNA-based therapies in development are conveniently administered intravitreally, with the potential for pan-retinal effect. The majority of these RNA therapeutics are synthetic ncRNA's and hold promise for the treatment of AMD, DR, and inherited retinal diseases (IRDs). These RNA-based therapies include siRNA therapy with its high specificity, shRNA to 'knock down' autosomal dominant toxic gain of function-mutated genes, antisense oligonucleotides (ASOs), which can restore splicing defects, and translational read-through inducing drugs (TRIDs) to increase expression of full-length protein from genes with premature stop codons.
在视网膜中,非编码 RNA(ncRNA)在调节细胞凋亡、炎症反应、视觉感知和光转导方面发挥着重要作用,在疾病状态下其水平发生改变。
微小 RNA(miRNA)是一类 ncRNA,通过与靶信使 RNA(mRNA)互补结合位点的结合,来调控转录后基因表达,从而导致翻译抑制。小干扰 RNA(siRNA)是一种双链 RNA(dsRNA),通过 RNA 干扰(RNAi)过程调节基因表达,导致基因的选择性沉默。另一种形式的 RNAi 涉及短发夹 RNA(shRNA)。在年龄相关性黄斑变性(AMD)和糖尿病性视网膜病变(DR)中,miRNA 被认为参与了血管生成、氧化应激、免疫反应和炎症的调节。
许多正在开发的基于 RNA 的疗法通过玻璃体内给药非常方便,具有全视网膜效应的潜力。这些 RNA 疗法中的大多数是合成的 ncRNA,为 AMD、DR 和遗传性视网膜疾病(IRDs)的治疗带来了希望。这些基于 RNA 的疗法包括具有高特异性的 siRNA 疗法、用于“敲低”常染色体显性毒性获得性功能突变基因的 shRNA、可以修复剪接缺陷的反义寡核苷酸(ASO),以及用于增加具有提前终止密码子的全长蛋白表达的翻译通读诱导药物(TRIDs)。