Garvan Institute of Medical Research and School of Clinical Medicine, UNSW Sydney, Sydney, New South Wales, Australia.
Victor Chang Cardiac Innovation Centre, Victor Chang Cardiac Research Institute, Sydney, New South Wales, Australia.
J Clin Invest. 2022 Oct 3;132(19):e160929. doi: 10.1172/JCI160929.
Mevalonate kinase deficiency (MKD) is characterized by recurrent fevers and flares of systemic inflammation, caused by biallelic loss-of-function mutations in MVK. The underlying disease mechanisms and triggers of inflammatory flares are poorly understood because of the lack of in vivo models. We describe genetically modified mice bearing the hypomorphic mutation p.Val377Ile (the commonest variant in patients with MKD) and amorphic, frameshift mutations in Mvk. Compound heterozygous mice recapitulated the characteristic biochemical phenotype of MKD, with increased plasma mevalonic acid and clear buildup of unprenylated GTPases in PBMCs, splenocytes, and bone marrow. The inflammatory response to LPS was enhanced in compound heterozygous mice and treatment with the NLRP3 inflammasome inhibitor MCC950 prevented the elevation of circulating IL-1β, thus identifying a potential inflammasome target for future therapeutic approaches. Furthermore, lines of mice with a range of deficiencies in mevalonate kinase and abnormal prenylation mirrored the genotype-phenotype relationship in human MKD. Importantly, these mice allowed the determination of a threshold level of residual enzyme activity, below which protein prenylation is impaired. Elevated temperature dramatically but reversibly exacerbated the deficit in the mevalonate pathway and the defective prenylation in vitro and in vivo, highlighting increased body temperature as a likely trigger of inflammatory flares.
甲羟戊酸激酶缺乏症(MKD)的特征是反复发热和全身炎症发作,这是由于 MVK 的双等位基因功能丧失突变引起的。由于缺乏体内模型,炎症发作的潜在疾病机制和触发因素仍不清楚。我们描述了携带 p.Val377Ile (MKD 患者最常见的变异)和 Mvk 无义、移码突变的基因修饰小鼠。复合杂合子小鼠重现了 MKD 的特征生化表型,血浆甲羟戊酸增加,PBMC、脾细胞和骨髓中未prenylated GTPases 明显堆积。复合杂合子小鼠对 LPS 的炎症反应增强,NLRP3 炎性体抑制剂 MCC950 的治疗可防止循环 IL-1β的升高,从而确定了未来治疗方法的潜在炎性体靶点。此外,具有一系列甲羟戊酸激酶缺陷和异常 prenylation 的小鼠系反映了人类 MKD 的基因型-表型关系。重要的是,这些小鼠允许确定残余酶活性的阈值水平,低于该水平时蛋白 prenylation 受损。体温升高显著但可逆转地加剧了甲羟戊酸途径和体外及体内缺陷 prenylation 的缺陷,突出了体温升高可能是炎症发作的一个潜在触发因素。