G protein-coupled receptors (GPCRS) are the largest family of membrane proteins of cell surface receptors. It can be activated by various stimuli and play an important role in various physiological and pathological processes. Abnormal regulation of GPCR is associated with various human diseases, such as oncology, metabolic diseases, cardiovascular diseases, and eye diseases. GPCR panel has high availability. Here, we constructed over 170 GPCR overexpression stable cell lines, covering wide families like 5-Hydroxytryptamine, acetylcholine, dopamine, glucagon, and opioid receptors. We also constructed different function assays, including cAMP assay, calcium flux assay, IP1 assay, reporter assay, and β-arrestin NanoBit assay to detect the different second messengers produced by G protein submits and GPCR-mediated multiple signaling pathways. The SPR binding assay, tag lite binding assay, and FACS binding assay are constructed to validate the affinity between GPCR and compounds. These GPCR panel and function assays can be used for target identification, hit-to-lead and lead optimization, also suitable for high-throughput screening.
Idiopathic pulmonary fibrosis (IPF) is a progressive and irreversible chronic disease that kill ten thousand of people in China every year. The risk of IPF is highly correlated with smoke, air pollution, dust, virus infection and aging. Average survival period of patients diagnosed as IPF is around 2.8 years which is less than several types of cancers, therefore, IPF is also thought to be a lung cancer-like disease. In the past few decades, many animal models were created to mimic human IPF, however, induction materials, animal species and strain differences, sex, physiology structure and progress of disease make the choice of IPF animal models selection more difficult. In addition, lack of strong evidence of cytokines biomarker detection hampered the discovery of anti-IPF drugs. Meso Scale Discovery (MSD) instrument is an efficient tool to high throughput analyze the lowest level of several cytokines and other biomarkers in the same time and was used to detect the bleomycin (BLM) induced mouse lung fibrosis in this study.