Department of Biochemistry, University of Missouri, Columbia, MO, USA.
Regeneron Pharmaceuticals, Tarrytown, NY, USA.
J Bone Miner Res. 2021 Apr;36(4):739-756. doi: 10.1002/jbmr.4223. Epub 2020 Dec 18.
Osteogenesis imperfecta (OI) is a genetic connective tissue disorder characterized by compromised skeletal integrity, altered microarchitecture, and bone fragility. Current OI treatment strategies focus on bone antiresorptives and surgical intervention with limited effectiveness, and thus identifying alternative therapeutic options remains critical. Muscle is an important stimulus for bone formation. Myostatin, a TGF-β superfamily myokine, acts through ActRIIB to negatively regulate muscle growth. Recent studies demonstrated the potential benefit of myostatin inhibition with the soluble ActRIIB fusion protein on skeletal properties, although various OI mouse models exhibited variable skeletal responses. The genetic and clinical heterogeneity associated with OI, the lack of specificity of the ActRIIB decoy molecule for myostatin alone, and adverse events in human clinical trials further the need to clarify myostatin's therapeutic potential and role in skeletal integrity. In this study, we determined musculoskeletal outcomes of genetic myostatin deficiency and postnatal pharmacological myostatin inhibition by a monoclonal anti-myostatin antibody (Regn647) in the G610C mouse, a model of mild-moderate type I/IV human OI. In the postnatal study, 5-week-old wild-type and +/G610C male and female littermates were treated with Regn647 or a control antibody for 11 weeks or for 7 weeks followed by a 4-week treatment holiday. Inhibition of myostatin, whether genetically or pharmacologically, increased muscle mass regardless of OI genotype, although to varying degrees. Genetic myostatin deficiency increased hindlimb muscle weights by 6.9% to 34.4%, whereas pharmacological inhibition increased them by 13.5% to 29.6%. Female +/mstn +/G610C (Dbl.Het) mice tended to have similar trabecular and cortical bone parameters as Wt showing reversal of +/G610C characteristics but with minimal effect of +/mstn occurring in male mice. Pharmacologic myostatin inhibition failed to improve skeletal bone properties of male or female +/G610C mice, although skeletal microarchitectural and biomechanical improvements were observed in male wild-type mice. Four-week treatment holiday did not alter skeletal outcomes. © 2020 American Society for Bone and Mineral Research (ASBMR).
成骨不全症(OI)是一种遗传性结缔组织疾病,其特征为骨骼完整性受损、微结构改变和骨骼脆弱。目前的 OI 治疗策略侧重于骨骼抗吸收剂和手术干预,但效果有限,因此寻找替代治疗方法仍然至关重要。肌肉是骨骼形成的重要刺激因素。肌肉生长抑制素(Myostatin)是 TGF-β 超家族的肌因子,通过 ActRIIB 发挥作用,负调控肌肉生长。最近的研究表明,可溶性 ActRIIB 融合蛋白抑制肌肉生长抑制素可对骨骼特性产生潜在益处,尽管各种 OI 小鼠模型的骨骼反应存在差异。OI 相关的遗传和临床异质性、ActRIIB 诱饵分子对肌肉生长抑制素的特异性不足以及人体临床试验中的不良反应,进一步表明需要阐明肌肉生长抑制素在骨骼完整性方面的治疗潜力和作用。在这项研究中,我们确定了 G610C 小鼠(轻度至中度 1/4 型人类 OI 的模型)中遗传肌肉生长抑制素缺乏和产后药理学肌肉生长抑制素抑制的肌肉骨骼结局。在产后研究中,5 周龄的野生型和+/G610C 雄性和雌性同窝仔鼠接受 Regn647 或对照抗体治疗 11 周或 7 周,然后进行 4 周的治疗假期。无论 OI 基因型如何,肌肉生长抑制素的抑制(无论是遗传抑制还是药理学抑制)都会增加肌肉质量,尽管程度不同。遗传肌肉生长抑制素缺乏使后肢肌肉重量增加 6.9%至 34.4%,而药理学抑制使后肢肌肉重量增加 13.5%至 29.6%。+/mstn+/G610C(双杂合子)雌性小鼠的小梁和皮质骨参数往往与 Wt 相似,表现出+/G610C 特征的逆转,但雄性小鼠中+/mstn 的影响最小。肌肉生长抑制素的药理学抑制未能改善雄性或雌性+/G610C 小鼠的骨骼骨特性,尽管在雄性野生型小鼠中观察到骨骼微结构和生物力学的改善。4 周的治疗假期并未改变骨骼结果。©2020 美国骨骼与矿物质研究协会(ASBMR)。