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The TLR (Toll-like receptor) is one of the major factors in the pathogenesis of autoimmune diseases. TLR signaling pathway plays a crucial role in the activation of innate immune responses, which is the first line of defense against external/foreign substances. TLR immediately responds to the invading pathogenic substances and secretes various cytokines to help the development of acquired immunity. However, if TLR signaling is over-activated, it can cause autoimmune or inflammatory diseases such as systemic lupus erythematosus, psoriasis or rheumatoid arthritis, which can be treated by directly blocking the signal transduction of the TLR.