a-magnetic-bead-based-negative-selection-flow-cytometry-protocol-for

A Magnetic Bead-Based Negative Selection and Flow Cytometry Protocol for Evaluating Licochalcone A-Mediated Inhibition of Murine Th17 Differentiation

Na&#239;ve CD4&#8314; T cell differentiation into Th17 cells is a key driver of autoimmune and chronic inflammatory skin diseases. Licochalcone A ...

The First Affiliated Hospital of Chongqing College of Traditional Chinese Medicine

The Src-homology 2 domain-containing phosphatase 2 (SHP2), which is encoded by PTPN11, participates in many cellular signaling pathways and is closely related to various tumorigenesis. Inhibition of the abnormal activity of SHP2 by small molecules is an important part of cancer treatment. Here, three abietane diterpenoids, named compounds -, were isolated from  var. . Spectroscopic analysis was used to identify the exact structure of the compounds. The enzymatic kinetic experiment and the cellular thermal shift assay showed compound  selectively inhibited SHP2 activity in vitro. Molecular docking indicated compound  targeted the SHP2 catalytic domain. The predicted pharmacokinetic properties by SwissADME revealed that compound  passed the majority of the parameters of common drug discovery rules. Compound  restrained A549 proliferation (IC = 8.68 ± 0.96 μM), invasion and caused A549 cell apoptosis by inhibiting the SHP2-ERK/AKT signaling pathway. Finally, compound  (Ajuforrestin A) is a potent and efficacious SHP2 inhibitor and may be a promising compound for human lung epithelial cancer treatment.

Fujin Yang

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