Vertex Pharmaceuticals Incorporated, Boston, Massachusetts, USA.
Foundation Hubrecht Organoid Technology, Utrecht, The Netherlands.
Clin Transl Sci. 2021 Mar;14(2):656-663. doi: 10.1111/cts.12927. Epub 2020 Dec 6.
In previous work, participants with a G970R mutation in cystic fibrosis transmembrane conductance regulator (CFTR) (c.2908G>C) had numerically lower sweat chloride responses during ivacaftor treatment than participants with other CFTR gating mutations. The objective of this substudy was to characterize the molecular defect of the G970R mutation in vitro and assess the benefit of ivacaftor in participants with this mutation. This substudy assessed sweat chloride, spirometry findings, and nasal potential difference on and off ivacaftor treatment in three participants with a G970R/F508del genotype. Intestinal organoids derived from rectal biopsy specimens were used to assess ivacaftor response ex vivo and conduct messenger RNA splice and protein analyses. No consistent or meaningful trends were observed between on-treatment and off-treatment clinical assessments. Organoids did not respond to ivacaftor in forskolin-induced swelling assays; no mature CFTR protein was detected in Western blots. Organoid RNA analysis demonstrated that 3 novel splice variants were created by G970R-CFTR: exon 17 truncation, exons 13-15 and 17 skipping, and intron 17 retention. Functional and molecular analyses indicated that the c.2908G>C mutation caused a cryptic splicing defect. Organoids lacked an ex vivo response with ivacaftor and supported identification of the mechanism underlying the CFTR defect caused by c.2908G>C. Analysis of CFTR mutations indicated that cryptic splicing was a rare cause of mutation misclassification in engineered cell lines. This substudy used organoids as an alternative in vitro model for mutations, such as cryptic splice mutations that cannot be fully assessed using cDNA expressed in recombinant cell systems.
在以前的研究中,囊性纤维化跨膜电导调节因子 (CFTR) 中 G970R 突变(c.2908G>C)的参与者在接受 ivacaftor 治疗时的汗液氯化物反应数值低于其他 CFTR 门控突变的参与者。本亚研究的目的是体外表征 G970R 突变的分子缺陷,并评估 ivacaftor 对该突变参与者的疗效。本亚研究评估了三位 G970R/F508del 基因型参与者在接受和不接受 ivacaftor 治疗时的汗液氯化物、肺功能检查结果和鼻电位差。使用直肠活检标本衍生的肠类器官评估 ivacaftor 的体外反应,并进行信使 RNA 剪接和蛋白分析。在治疗期间和治疗结束时的临床评估之间没有观察到一致或有意义的趋势。在 forskolin 诱导的肿胀测定中,类器官对 ivacaftor 没有反应;Western blot 中未检测到成熟的 CFTR 蛋白。类器官 RNA 分析表明,G970R-CFTR 产生了 3 种新的剪接变异:外显子 17 截断、外显子 13-15 和 17 跳跃以及内含子 17 保留。功能和分子分析表明,c.2908G>C 突变导致了隐蔽性剪接缺陷。类器官缺乏体外 ivacaftor 反应,并支持鉴定 c.2908G>C 引起的 CFTR 缺陷的机制。CFTR 突变分析表明,隐蔽性剪接是工程细胞系中突变分类错误的罕见原因。本亚研究使用类器官作为替代体外模型,用于无法通过重组细胞系统中表达的 cDNA 充分评估的突变,如隐蔽性剪接突变。