Targeting the SUMO pathway for neuroprotection in brain ischaemia

Article Figures & Data

Table 1

Summary of SENP inhibitors identified by screening

Screening target	Screening strategy	Screening library	Representative hit	IC₅₀	Bioactivity in cells	Reference
SENP1	Benzodiazepine-based design	–	Compound 38	9.2 µM	Not tested	42
SENP1	Cleavage of fluorogenic substrate SUMO1-AMC	In-house compound library	GN6958	29.6 µM	Not tested	43
SENP1	Virtual screening	SPECS database	SI2	1.29 µM	Confirmed	44
PfSENP1	SUMO-procleavage assay with SDS-PAGE detection	Cysteine protease inhibitors library	JCP-666	17.9 µM	Not tested	45
SENP1/2	Virtual screening	DTP	NSC5068	µM range	Confirmed	46
SENP2	Combination of virtual screening and FRET-based assay	Namiki-shoji library	1,2,5-oxadiazoles	<10 µM	Not tested	47
SENPs	Cleavage of fluorogenic AFC-based substrates	In-house compound library	VEA499	µM range	No activity	48

DTP, Developmental Therapeutics Program; FRET, fluorescence resonance energy transfer; IC₅₀, half-maximum inhibitory concentration; PfSENP, SENP of Plasmodium falciparum; SENP, SUMO-specific protease; SUMO, small ubiquitin-like modifier.

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