Journal: eBioMedicine
Article Title: HIV protease inhibitor nelfinavir is a potent drug candidate against echinococcosis by targeting Ddi1-like protein
doi: 10.1016/j.ebiom.2022.104177
Figure Lengend Snippet: Nelfinavir inhibits the proteolysis activity of recombinant Emu Ddi1 . Emu Ddi1 was expressed in an E. coli system. Based on the amino acid compositions, this molecular weight of the recombinant protein was predicted to be appropriately 45 KD in the monomer (left) and 90 KD in the dimer (right) (a). At an optimum pH of 7.2, the recombinant Emu Ddi1 was able to hydrolyze the retro-pepsin substrate with a Km = 1.28 (95% CI: 0.80 to 2.02) μM and a Kcat = 0.36 s –1 (b). The HIVPIs, including lopinavir (LPV), indinavir (IDV), darunavir (DRV), fosamprenavir (FAPV), ritonavir (RTV), tipranavir (TPV), atazanavir (ATV), amprenavir (APV), nelfinavir (NFV) and saquinavir (SQV) were tested (n = 3). The enzyme activity of this recombinant protein (at 0.5 μM) could be apparently blocked by nelfinavir (NFV) and saquinavir (SQV) (40 μM) (c). The half-maximal inhibitory concentration (IC 50 ) of nelfinavir on the recombinant Emu Ddi1 was 45.95 μM (d). The results shown are representative of two or more independent experiments. Data shown are represented as mean ± SD.
Article Snippet: HIV protease inhibitors (HIVPIs), including nelfinavir (NFV, CAS NO. 159989-64-7), lopinavir (LPV, CAS NO. 192725-17-0), indinavir (IDV, CAS NO.180686-37-8), darunavir (DRV, CAS NO. 206361-99-1), fosamprenavir (FAPV, CAS NO. 226700-79-4), ritonavir (RTV, CAS NO. 176655-55-3), tipranavir (TPV, CAS NO. 174484-41-4), atazanavir (ATV, CAS NO. 198904-31-3), saquinavir (SQV, CAS NO. 149845-06-7), and amprenavir (APV, CAS NO. 161814-49-9), were purchased from Macklin (Shanghai, China).
Techniques: Activity Assay, Recombinant, Molecular Weight, Concentration Assay