Anti-integrin therapy for retinovascular diseases.
Anti-integrin therapy for retinovascular diseases.
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DOI：
10.1080/13543784.2020.1795639
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发表时间：
2020-09
影响因子：
6.1
通讯作者：
Ciulla, Thomas
中科院分区：
文献类型：
--
作者：
Bhatwadekar, Ashay D.;Kansara, Viral;Luo, Qianyi;Ciulla, Thomas
关键词：
整合素是一类多功能细胞粘附分子，异二聚体受体，连接细胞外基质（ECM）和细胞皮层的肌动蛋白细胞骨架，从而调节细胞的粘附、迁移、增殖、侵袭、存活和凋亡。因此，整合素在炎症、血管生成和纤维化中发挥作用。本文综述了抗整合素药物的化学性质、给药途径和抗整合素作用。它还提供了临床前和临床研究的总结。目前的临床候选药物包括risuteganib、THR-687和SF-0166，这些药物在早期临床研究中显示出治疗糖尿病黄斑水肿（DME）和/或年龄相关性黄斑变性（AMD）的前景。临床前候选药物包括SB-267268、AXT-107、JNJ-26076713、Cilengitide和Lebecetin，它们表现出视网膜通透性、血管生成和/或脉络膜新生血管（CNV）的降低。抗整合素疗法在治疗视网膜疾病方面显示出潜力。抗整合素药物解决了糖尿病视网膜病变（DR）和AMD的多因素性质，并在临床前和早期临床研究中显示出作为注射和局部药物的希望。整合素抑制有潜力作为主要治疗，辅助治疗抗血管内皮生长因子药物，或二次治疗难治性病例。
Integrins are a family of multi-functional cell-adhesion molecules, heterodimeric receptors that connect extracellular matrix (ECM) to actin cytoskeleton in the cell cortex, thus regulating cellular adhesion, migration, proliferation, invasion, survival, and apoptosis. Consequently, integrins play a role in inflammation, angiogenesis and fibrosis. This review examines individual anti-integrin agents in terms of their chemical nature, route of administration, and anti-integrin action. It also provides a summary of preclinical and clinical studies. Current clinical candidates include risuteganib, THR-687, and SF-0166, which have shown promise in treating diabetic macular edema (DME) and/or age-related macular degeneration (AMD) in early clinical studies. Preclinical candidates include SB-267268, AXT-107, JNJ-26076713, Cilengitide and Lebecetin, which exhibit a decrease in retinal permeability, angiogenesis and/or choroidal neovascularization (CNV). Anti-integrin therapies show potential in treating retinal diseases. Anti-integrin agents tackle the multi-factorial nature of diabetic retinopathy (DR) and AMD and show promise as injectable and topical agents in preclinical and early clinical studies. Integrin inhibition has potential to serve as primary therapy, adjunctive therapy to anti-vascular endothelial growth factor agents, or secondary therapy in refractory cases.
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DOI：
10.1073/pnas.93.18.9764
发表时间：
1996-09-03
影响因子：
11.1
作者：
Friedlander, M;Theesfeld, CL;Cheresh, DA
通讯作者：
Cheresh, DA
影响因子：
56.9
作者：
BROOKS, PC;CLARK, RAF;CHERESH, DA
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CHERESH, DA
影响因子：
7.7
作者：
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Lorenzi, Mara
DOI：
10.1136/bjophthalmol-2020-315933
发表时间：
2021-03
期刊：
The British journal of ophthalmology
影响因子：
--
作者：
Ciulla TA;Pollack JS;Williams DF
通讯作者：
Williams DF
影响因子：
16.2
作者：
Ambati J;Fowler BJ
通讯作者：
Fowler BJ