Angel Thomas E, Chen Zhuo, Moghieb Ahmed, Ng Sze-Ling, Beal Allison M, Capriotti Carol, Azzarano Leonard, Comroe Debra, Adam Michael, Moore Patrick, Hoang Bao, Blough Kelly, Kuziw Joanne, Ramanjulu Joshi M, Pesiridis G Scott
In vitro/In vivo Translation, Research and Development, GlaxoSmithKline, Collegeville, Pennsylvania, United States of America.
Respiratory and Immunology Research Unit, Research and Development, GlaxoSmithKline, Collegeville, Pennsylvania, United States of America.
PLoS One. 2025 Feb 25;20(2):e0319216. doi: 10.1371/journal.pone.0319216. eCollection 2025.
Drugs targeting the ER-resident innate immune receptor Stimulator of Interferon Genes (STING) are in development for treatments of cancer and inflammatory diseases. Accurate determination of STING receptor levels in normal and disease tissue is an essential component of modeling pharmacology and drug-target disposition. Using metabolic labeling with deuterium oxide paired with high resolution mass spectrometry, we report the protein fractional synthesis rates and turnover of STING in wild-type (C57BL/6) and inflamed mice carrying the Trex1 D18N mutation (Trex1D18N) as a STING-dependent model of human Acardi-Goutiéres syndrome. Remarkably, STING protein half-life is tissue specific with the shortest half-life of 4 days in colon and lymph node and longest half-life of 24 days in skeletal muscle. Despite the relative increase in STING protein abundance in the inflamed Trex1D18N mouse, the overall kinetics of protein degradation and resynthesis was similar between Trex1D18N and WT mice. The extent of tissue specific interferon stimulated gene transcription, a hallmark of SLE linked pathophysiology, correlates with the extend of increased STING levels in Trex1D18N tissues and appears inversely proportional to the turnover rate of STING. Understanding STING's fractional protein synthesis rate and half-life provides a valuable component of quantitative modeling of drug pharmacology, dose frequency and targeting tissues of STING directed therapies.
靶向内质网驻留先天免疫受体干扰素基因刺激物(STING)的药物正在研发中,用于治疗癌症和炎症性疾病。准确测定正常组织和疾病组织中的STING受体水平是药物药理学建模和药物靶点处置的重要组成部分。我们使用氧化氘代谢标记结合高分辨率质谱,报告了野生型(C57BL/6)小鼠和携带Trex1 D18N突变(Trex1D18N)的炎症小鼠(作为人类Acardi-Goutiéres综合征的STING依赖性模型)中STING的蛋白质合成分数率和周转率。值得注意的是,STING蛋白半衰期具有组织特异性,在结肠和淋巴结中最短,为4天,在骨骼肌中最长,为24天。尽管在炎症性Trex1D18N小鼠中STING蛋白丰度相对增加,但Trex1D18N小鼠和野生型小鼠之间蛋白质降解和再合成的总体动力学相似。组织特异性干扰素刺激基因转录的程度是系统性红斑狼疮相关病理生理学的一个标志,与Trex1D18N组织中STING水平升高的程度相关,并且似乎与STING的周转率成反比。了解STING的蛋白质合成分数率和半衰期为STING导向疗法的药物药理学、给药频率和靶向组织的定量建模提供了有价值的组成部分。