TLR4 (Toll-like receptor) compound of targeting microglia as well as preparation method and application of compound

Abstract

The invention discloses a TLR4 (Toll-like receptor) compound of targeting microglia as well as a preparation method and application of the compound in the pharmaceutical field, and belongs to the field of biomedicine. The compound is formed by binding fusion peptide of Q9 peptide (QQQKKKKKK) and T9 peptide (LTQQVVMKF) and TLR4RNAi through an electrostatic interaction; through a guiding function of the Q9 peptide, the compound can specifically target a specific CX3CR1 receptor on the surface of the microglia; when the T9 peptide acts with the CX3CR1 receptor, the TLR4RNAi is efficiently transfected into the microglia to inhibit activation of the microglia, so as to inhibit an inflammatory reaction after microglia mediated cerebral hemorrhage; the compound can be used for preparing microglia mediated anti-inflammatory drugs, and has good development and application prospects in the field of cerebral hemorrhage treatment.

Description

technical field [0001] The invention belongs to the field of biomedicine and relates to a polypeptide-gene complex, in particular to a TLR4 complex targeting microglial cells, a preparation method thereof, and an application in the field of pharmacy. Background technique [0002] Cerebral hemorrhage is a common critical illness of the nervous system, which has attracted widespread attention due to its high morbidity, disability and mortality. With the improvement of people's living standards and the arrival of aging, the incidence of cerebral hemorrhage is also on the rise. A large number of studies have shown that there is an obvious inflammatory response after cerebral hemorrhage, and the inflammatory response is involved in the pathological process of secondary cerebral edema and brain damage after cerebral hemorrhage. After ICH, inflammatory cells such as microglia around the hematoma are activated and release inflammatory factors such as TNF-α and IL-1. In addition to ...

AI Technical Summary

Problems solved by technology

The study found that the seductive ligand polypeptide T9 derived from the N-terminus of the US28 receptor can block the chemotaxis formed by the human CX3CR1 receptor binding physiological chemokines, but it does not cause chemotactic movement and does not affect intracellular signals Transduction and cell-native activity; it can cause the internalization of the cell surface receptor CX3CR1, but the internalized receptor part can be recycled to the cell surface, and has no obvious effect on the physiological function of the human CX3CR1 receptor

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