Emory University School of Medicine, Department of Dermatology, 101 Woodruff Cr., Suite 5001, Atlanta, GA 30322, USA.
Arch Biochem Biophys. 2011 Apr 15;508(2):222-6. doi: 10.1016/j.abb.2010.12.016. Epub 2010 Dec 21.
Because angiogenesis underlies the pathogenesis of numerous conditions (cancer, psoriasis, macular degeneration), there is a pressing need for continued investigations into angiogenic signaling and potential drug targets. Antiangiogenic agents can be classified as either direct or indirect. Direct antiangiogenics act on untransformed endothelial cells to prevent differentiation and proliferation; indirect antiangiogenics act to inhibit factors involved in proangiogenic signaling. Agents currently available with dermatologic indications are few; while several established and novel biologics targeting various proangiogenic factors are currently being investigated for potential dermatologic uses, but the jury is still out on their efficacy and safety. In this review, we highlight our experience with a group of existing and novel, small molecules that combine several modes of action against angiogenesis in addition to other properties--triarylmethane dyes and fulvene derivatives.
由于血管生成是许多疾病(癌症、银屑病、黄斑变性)发病机制的基础,因此迫切需要对血管生成信号和潜在药物靶点进行持续研究。抗血管生成剂可分为直接和间接两种。直接抗血管生成剂作用于未转化的内皮细胞,以防止其分化和增殖;间接抗血管生成剂作用于抑制参与促血管生成信号的因子。目前具有皮肤科适应证的药物很少;虽然有几种针对各种促血管生成因子的已确立和新型生物制剂正在被研究用于潜在的皮肤科用途,但它们的疗效和安全性仍存在争议。在这篇综述中,我们重点介绍了我们在一组现有和新型小分子药物方面的经验,这些药物除了具有其他特性外,还结合了几种针对血管生成的作用模式——三芳基甲烷染料和富烯衍生物。