Biochemical profiling of anti-HIV prodrug Elsulfavirine (Elpida^®) and its active form VM1500A against a panel of twelve human carbonic anhydrase isoforms

Figures & data

Figure 1. Elsufavirine (Elpida) and VM1500A.

Figure 2. Schematic representation of a sulphonamide-based CAI bound in the active site of CA.

Table 1. hCA isoform inhibitory profile of acetazolamide (AAZ), VM1500-A and elsulfavirine.

hCA isoform	Ki (nM)*
	AAZ	VM1500A	elsulfavirine
hCA I	250	514	52,400
hCA II	12	35.5	12,500
hCA III	20,000	>100,000	>100,000
hCA IV	74	158	>100,000
hCA VA	63	537	4,290
hCA VB	54	221	14,200
hCA VI	11	125	5,670
hCA VII	2.5	9.7	2,390
hCA IX	25	72.1	6,650
hCA XII	5.7	62.3	980,1
hCA XIII	17	52.2	4,820
hCA XIV	41	15.4	1,960

*Mean from 3 different assays, by a stopped flow technique (errors were in the range of ±5–10% of the reported values).

Figure 3. Predicted binding pose of VM1500A (green) within the active site of hCA VII.