Kirkegaard Thomas, Gray James, Priestman David A, Wallom Kerri-Lee, Atkins Jennifer, Olsen Ole Dines, Klein Alexander, Drndarski Svetlana, Petersen Nikolaj H T, Ingemann Linda, Smith David A, Morris Lauren, Bornæs Claus, Jørgensen Signe Humle, Williams Ian, Hinsby Anders, Arenz Christoph, Begley David, Jäättelä Marja, Platt Frances M
Orphazyme ApS, Copenhagen, Denmark.
Department of Pharmacology, University of Oxford, Oxford, U.K.
Sci Transl Med. 2016 Sep 7;8(355):355ra118. doi: 10.1126/scitranslmed.aad9823.
Lysosomal storage diseases (LSDs) often manifest with severe systemic and central nervous system (CNS) symptoms. The existing treatment options are limited and have no or only modest efficacy against neurological manifestations of disease. We demonstrate that recombinant human heat shock protein 70 (HSP70) improves the binding of several sphingolipid-degrading enzymes to their essential cofactor bis(monoacyl)glycerophosphate in vitro. HSP70 treatment reversed lysosomal pathology in primary fibroblasts from 14 patients with eight different LSDs. HSP70 penetrated effectively into murine tissues including the CNS and inhibited glycosphingolipid accumulation in murine models of Fabry disease (Gla(-/-)), Sandhoff disease (Hexb(-/-)), and Niemann-Pick disease type C (Npc1(-/-)) and attenuated a wide spectrum of disease-associated neurological symptoms in Hexb(-/-) and Npc1(-/-) mice. Oral administration of arimoclomol, a small-molecule coinducer of HSPs that is currently in clinical trials for Niemann-Pick disease type C (NPC), recapitulated the effects of recombinant human HSP70, suggesting that heat shock protein-based therapies merit clinical evaluation for treating LSDs.
溶酶体贮积症(LSDs)通常表现为严重的全身症状和中枢神经系统(CNS)症状。现有的治疗选择有限,对疾病的神经学表现没有效果或仅有适度疗效。我们证明,重组人热休克蛋白70(HSP70)在体外可改善几种鞘脂降解酶与其必需辅因子双(单酰基)甘油磷酸的结合。HSP70治疗逆转了来自14例患有8种不同LSDs患者的原代成纤维细胞中的溶酶体病理。HSP70有效地渗透到包括中枢神经系统在内的小鼠组织中,并在法布里病(Gla(-/-))、桑德霍夫病(Hexb(-/-))和尼曼-匹克病C型(Npc1(-/-))的小鼠模型中抑制鞘糖脂积累,并减轻了Hexb(-/-)和Npc1(-/-)小鼠中广泛的疾病相关神经症状。口服阿利莫洛,一种小分子热休克蛋白共诱导剂,目前正在进行尼曼-匹克病C型(NPC)的临床试验,重现了重组人HSP70的效果,表明基于热休克蛋白疗法值得对治疗LSDs进行临床评估。