Powering down the mitochondrial LonP1 protease: a novel strategy for anticancer therapeutics

Figures & data

Figure 1. Functions of LonP1 in cellular homeostasis and cell stress responses that can be exploited by cancer cells (created using BioRender.com).

Table 1. Small molecule inhibitors of LonP1.

Drug	IC50	Mechanism of Action	Reference
Bortezomib	17 nM	Proteolytic active site inhibitor	[6]
CDDO	13 μM	Allosteric ATPase inhibitor	[34]
CDDO-Me	1.9 μM	Allosteric ATPase inhibitor	[34]
CDDO-Im	2 μM	Allosteric ATPase inhibitor	[34]
Compound 14^a	0.059 μM	Proteolytic active site inhibitor^b	[35]
Coumarinic derivatives 4–8	nd	Proteolytic active site inhibitor	[36]
MG262	122 nM	Proteolytic active site inhibitor	[33]
Obtusilactone A	34.1 μM	Proteolytic active site inhibitor^b	[37]
Sesamin	19.9 μM	Proteolytic active site inhibitor^b	[37]

^aBoronic acid-based non-peptide inhibitor.

^bSuggested by computational modeling.

nd – Not determined.

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