Discovery of Molecular Therapeutics for Glaucoma: Challenges, Successes, and Promising Directions.
Discovery of Molecular Therapeutics for Glaucoma: Challenges, Successes, and Promising Directions.
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DOI：
10.1021/acs.jmedchem.5b00828
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发表时间：
2016-02-11
影响因子：
7.3
通讯作者：
Lieberman RL
中科院分区：
文献类型：
--
作者：
Donegan RK;Lieberman RL
青光眼是一种影响全球约6000万人的异质性眼部疾病，其特征是视网膜神经节细胞（RGCs）的无痛性神经变性，导致不可逆的视力丧失。现有的治疗方法可以降低眼压升高的常见危险因素，延迟但不能预防RGC死亡和失明。值得注意的是，眼球前段的变化，特别是房水排出的变化，被认为是造成压力变化的原因。因此，在当前和新兴的青光眼治疗中，主要是这个区域的特性被操纵。在这里，我们关注与开发治疗相关的挑战，回顾现有的实验方法来评估新药的治疗潜力，描述新兴的rho激酶抑制剂和腺苷受体配体的开发和评估，这些抑制剂和配体具有改善房水流出和同时保护RGCs的潜力，并提出新的靶点和方法。
Glaucoma, a heterogeneous ocular disorder affecting ~60 million people worldwide, is characterized by painless neurodegeneration of retinal ganglion cells (RGCs), resulting in irreversible vision loss. Available therapies, which decrease the common causal risk factor of elevated intraocular pressure, delay, but cannot prevent, RGC death and blindness. Notably, it is changes in the anterior segment of the eye, particularly in the drainage of aqueous humor fluid, which are believed to bring about changes in pressure. Thus, it is primarily this region whose properties are manipulated in current and emerging therapies for glaucoma. Here, we focus on the challenges associated with developing treatments, review the available experimental methods to evaluate the therapeutic potential of new drugs, describe the development and evaluation of emerging Rho-kinase inhibitors and adenosine receptor ligands that offer the potential to improve aqueous humor outflow and protect RGCs simultaneously, and present new targets and approaches on the horizon.
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