Tarallo Valeria, De Falco Sandro
Angiogenesis Lab, Institute of Genetics and Biophysics 'Adriano Buzzati-Traverso' - CNR, 80131 Naples, Italy.
Angiogenesis Lab, Institute of Genetics and Biophysics 'Adriano Buzzati-Traverso' - CNR, 80131 Naples, Italy; IRCCS MultiMedica, 20099 Milan, Italy.
Int J Biochem Cell Biol. 2015 Jul;64:185-9. doi: 10.1016/j.biocel.2015.04.008. Epub 2015 May 1.
Angiogenesis is a complex biological phenomenon essential for a correct embryonic development and for post-natal growth. In adult life, it is a tightly regulated process but in several pathological conditions, angiogenesis results abnormal with either excessive or insufficient proliferation of blood vessels. The pro-angiogenic members of VEGF family, VEGF-A, VEGF-B and placental growth factor (PlGF), and the related receptors, VEGFR-1 and VEGFR-2, have a central and decisive role in pathological angiogenesis. Indeed, they are the targets for anti-angiogenic drugs currently approved: bevacizumab and ranibizumab, that specifically inhibit VEGF-A; aflibercept, that is able to prevent the activity of VEGF-A, VEGF-B and PlGF; several multirtarget tyrosine kinase inhibitors that are able to prevent VEGFR-1 and/or VEGFR-2 signaling. The anti-angiogenesis therapy has represented one of the most active fields of drug discovery of last decade and promises to be further expanded due the wide number of diseases for which it may by applied.
血管生成是一种复杂的生物学现象，对胚胎的正常发育和出生后的生长至关重要。在成年期，它是一个受到严格调控的过程，但在几种病理状态下，血管生成会出现异常，表现为血管过度增殖或增殖不足。血管内皮生长因子（VEGF）家族的促血管生成成员，即VEGF-A、VEGF-B和胎盘生长因子（PlGF），以及相关受体VEGFR-1和VEGFR-2，在病理性血管生成中起着核心和决定性作用。事实上，它们是目前已获批的抗血管生成药物的靶点：贝伐单抗和雷珠单抗，它们特异性抑制VEGF-A；阿柏西普，它能够阻断VEGF-A、VEGF-B和PlGF的活性；还有几种多靶点酪氨酸激酶抑制剂，它们能够阻断VEGFR-1和/或VEGFR-2信号传导。抗血管生成治疗一直是过去十年中药物研发最活跃的领域之一，由于其可应用于多种疾病，有望进一步拓展。
