Kaplan Frederick S, Le Merrer Martine, Glaser David L, Pignolo Robert J, Goldsby Robert E, Kitterman Joseph A, Groppe Jay, Shore Eileen M
Departments of Orthopedic Surgery & Medicine, The University of Pennsylvania School of Medicine, c/o Hospital of The University of Pennsylvania, Philadelphia, PA, USA.
Best Pract Res Clin Rheumatol. 2008 Mar;22(1):191-205. doi: 10.1016/j.berh.2007.11.007.
Fibrodysplasia ossificans progressiva (FOP), a rare and disabling genetic condition of congenital skeletal malformations and progressive heterotopic ossification (HO), is the most catastrophic disorder of HO in humans. Episodic disease flare-ups are precipitated by soft tissue injury, and immobility is cumulative. Recently, a recurrent mutation in activin receptor IA/activin-like kinase 2 (ACVR1/ALK2), a bone morphogenetic protein (BMP) type I receptor, was reported in all sporadic and familial cases of classic FOP, making this one of the most highly specific disease-causing mutations in the human genome. The discovery of the FOP gene establishes a critical milestone in understanding FOP, reveals a highly conserved target for drug development in the transforming growth factor (TGF)-beta/BMP signalling pathway, and compels therapeutic approaches for the development of small molecule signal transduction inhibitors for ACVR1/ALK2. Present management involves early diagnosis, assiduous avoidance of iatrogenic harm, and symptomatic amelioration of painful flare-ups. Effective therapies for FOP, and possibly for other common conditions of HO, may potentially be based on future interventions that block ACVR1/ALK2 signalling.
进行性骨化性纤维发育不良(FOP)是一种罕见且使人致残的先天性骨骼畸形和进行性异位骨化(HO)的遗传性疾病,是人类最具灾难性的HO病症。软组织损伤会引发疾病的间歇性发作,且活动受限会逐渐累积。最近,在所有经典FOP的散发性和家族性病例中均报道了骨形态发生蛋白(BMP)I型受体激活素受体IA/激活素样激酶2(ACVR1/ALK2)的复发性突变,这使其成为人类基因组中最具特异性的致病突变之一。FOP基因的发现是理解FOP过程中的一个关键里程碑,揭示了转化生长因子(TGF)-β/BMP信号通路中药物开发的一个高度保守靶点,并促使人们开发针对ACVR1/ALK2的小分子信号转导抑制剂的治疗方法。目前的治疗包括早期诊断、严格避免医源性伤害以及对疼痛发作进行症状缓解。FOP以及可能其他常见HO病症的有效治疗方法可能基于未来阻断ACVR1/ALK2信号传导的干预措施。