a Centro de Investigaciones Biológicas, Consejo Superior de Investigaciones Científicas (CSIC), and Centro de Investigación Biomédica en Red de Enfermedades Raras (CIBERER) , Madrid , Spain.
b Faculté de Pharmacie , Paris Descartes University, Sorbonne Paris Cité and Inserm UMR-S1140 , Paris , France.
Expert Opin Ther Targets. 2017 Oct;21(10):933-947. doi: 10.1080/14728222.2017.1365839. Epub 2017 Aug 20.
Hereditary Haemorrhagic Telangiectasia (HHT) is as an autosomal dominant trait characterized by frequent nose bleeds, mucocutaneous telangiectases, arteriovenous malformations (AVMs) of the lung, liver and brain, and gastrointestinal bleedings due to telangiectases. HHT is originated by mutations in genes whose encoded proteins are involved in the transforming growth factor β (TGF-β) family signalling of vascular endothelial cells. In spite of the great advances in the diagnosis as well as in the molecular, cellular and animal models of HHT, the current treatments remain just at the palliative level. Areas covered: Pathogenic mutations in genes coding for the TGF-β receptors endoglin (ENG) (HHT1) or the activin receptor-like kinase-1 (ACVRL1 or ALK1) (HHT2), are responsible for more than 80% of patients with HHT. Therefore, ENG and ALK1 are the main potential therapeutic targets for HHT and the focus of this review. The current status of the preclinical and clinical studies, including the anti-angiogenic strategy, have been addressed. Expert opinion: Endoglin and ALK1 are attractive therapeutic targets in HHT. Because haploinsufficiency is the pathogenic mechanism in HHT, several therapeutic approaches able to enhance protein expression and/or function of endoglin and ALK1 are keys to find novel and efficient treatments for the disease.
遗传性出血性毛细血管扩张症(HHT)是一种常染色体显性遗传疾病,其特征为频繁流鼻血、黏膜皮肤毛细血管扩张、肺、肝和脑动静脉畸形(AVMs),以及由于毛细血管扩张导致的胃肠道出血。HHT 是由编码蛋白参与血管内皮细胞转化生长因子 β(TGF-β)家族信号的基因突变引起的。尽管在 HHT 的诊断以及分子、细胞和动物模型方面取得了巨大进展,但目前的治疗方法仍仅处于姑息治疗水平。 涵盖领域:编码 TGF-β 受体内格林(ENG)(HHT1)或激活素受体样激酶-1(ACVRL1 或 ALK1)(HHT2)的基因突变负责超过 80%的 HHT 患者。因此,ENG 和 ALK1 是 HHT 的主要潜在治疗靶点,也是本综述的重点。包括抗血管生成策略在内的临床前和临床研究的现状已被涉及。 专家意见:ENG 和 ALK1 是 HHT 有吸引力的治疗靶点。由于 HHT 的致病机制是杂合子不足,因此能够增强 ENG 和 ALK1 蛋白表达和/或功能的几种治疗方法是寻找该疾病新的有效治疗方法的关键。