1.Targeted inhibition of GRK2 kinase domain by CP-25 to reverse fibroblast-like synoviocytes dysfunction and improve collagen-induced arthritis in rats.
Chenchen HAN ; Yifan LI ; Yuwen ZHANG ; Yang WANG ; Dongqian CUI ; Tingting LUO ; Yu ZHANG ; Qian LIU ; Hao LI ; Chun WANG ; Dexiang XU ; Yang MA ; Wei WEI
Acta Pharmaceutica Sinica B 2021;11(7):1835-1852
Rheumatoid arthritis (RA) is an autoimmune disease and is mainly characterized by abnormal proliferation of fibroblast-like synoviocytes (FLS). The up-regulated cellular membrane expression of G protein coupled receptor kinase 2 (GRK2) of FLS plays a critical role in RA progression, the increase of GRK2 translocation activity promotes dysfunctional prostaglandin E4 receptor (EP4) signaling and FLS abnormal proliferation. Recently, although our group found that paeoniflorin-6'-
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