AX20017 is a small-molecule protein kinase G (PknG) inhibitor with an IC50 of 0.39 μM[3]. Inhibition of PknG by AX20017 reduces mycobacterial survival in in vitro latency models such as hypoxia, persisters, and nutrient starvation[4]. Inhibition of PknG with the highly selective low-molecular-weight inhibitor AX20017 results in mycobacterial transfer to lysosomes and killing of the mycobacteria. The structure of PknG-AX20017 further reveals that the inhibitor is buried deep within the adenosine-binding site, targeting an active conformation of the kinase domain[5]. The available drug molecules and the ligand AX20017 showed hydrogen bond interaction with the aminoacid residues Glu233 and Val235[6].
AX20017 细胞实验
Cell Line
Concentration
Treated Time
Description
References
J774 cells
20 μM
To observe the effect of AX20017 on J774 cell morphology, membrane ruffling, and macropinocytosis
Proc Natl Acad Sci U S A. 2007 Jul 17;104(29):12151-6
macrophages
25 μM
48 h
To evaluate the effect of AX20017 on the survival of Mycobacterium tuberculosis within macrophages. Results showed that AX20017 significantly reduced the intracellular survival of Mtb.
Antimicrob Agents Chemother. 2021 Mar 18;65(4):e02095-20
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