protease-resistant

TCS PrP Inhibitor 13 (5-(4-Nitrophenyl)-2-Phenyl-4H-Pyrazol-3-One) is an antiprion agent inhibiting protease-resistant prion protein (PrP-res) accumulation.

SM111 inhibits in vitro replication of HIV-1, including strains resistant to reverse transcriptase, licensed protease, and integrase inhibitors, without major cellular toxicity.

HIV-1 protease-IN-11 (compound 34a), an HIV-1 protease inhibitor, demonstrates potent inhibition with an IC50 of 0.41 nM and maintains substantial efficacy against drug-resistant variant [1].

Tipranavir is a protease inhibitor that inhibits HIV-1 resistant to more than 1 protease inhibitor .Tipranavir effectively inhibits HIV-1 protease enzyme activity and dimerisation and has potent activity against multiple protease inhibitor (PI) HIV-1 isolates (IC50 of 66-410 nM). Tipranavir inhibits SARS-CoV-2 3CLpro activity.

HIV-1 protease-IN-8 (compound 34b) is a potent inhibitor of the HIV-1 protease enzyme, exhibiting an IC50 of 0.32 nM. It demonstrates IC50 values of 0.29 μM for the wild-type HIV-1 (HIV-1 NL4-3) and 1.90 μM against a drug-resistant variant (HIV-1 MDR), indicating strong antiviral activity against both strains [1].

CI-1029 is an HIV protease inhibitor that is effective against mutant HIV proteases and drug-resistant HIV strains. It has excellent protease activity, good antiviral efficacy in cell tests, and has good bioavailability in a variety of animal species.

HIV-1 protease-IN-6 (compound 17d) is a potent inhibitor of HIV-1 protease (IC50: 21 pM, Ki: 4.7 pM). HIV-1 protease-IN-6 showed significant antiviral activity against DRV (darunavir) resistant mutants, even exceeding the intensity of inhibition against wild-type viruses.

Rab8a GTPase-binding stapled peptide (Kd = 12.7 μM). Cell permeable; localizes to the endomembrane system. Cromm et al (2016) Protease-resistant and cell-permeable double-stapled peptides targeting the Rab8a GTPase. ACS Chem.Biol. 11 2375 PMID:27336832

Grazoprevir (MK-5172) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Ki of 0.01 nM (gt1a), 0.08 nM (gt2a), 0.90 nM (gt3a), 0.01 nM (gt1b), 0.15 nM (gt2b), respectively.

HIV-1 protease-IN-5 is an HIV-1 protease inhibitor (IC50: 1.64 nM). HIV-1 protease-IN-5 exhibits significant effects on wild-type and DRV-resistant HIV-1.

AG-7404 is a potent protease inhibitor with anti-poliovirus activity. AG-7404 was active against all virus with EC50 values ranging from 0.080 to 0.674 μM. AG-7404 was fully active against V-073-resistant variants with EC50 values ranging from 0.218 to 0.

BI-1388 is a highly potent inhibitor of HCV NS3 protease activity, inhibiting viral replication for various HCV genotypes and for resistant mutants D168V and R155K.

HIV-1 protease-IN-2 is a potent inhibitor of HIV-1 protease (IC50: 2.53 nM). HIV-1 protease-IN-2 exhibits antiviral effects against DRV (Darunavir) sensitive or drug resistant HIV-1 mutants.

Grazoprevir, a second generation hepatitis C virus protease inhibitor acting at the NS3/4a protease targets, has good activity against a range of hepatitis C virus genotype variants, including some that are resistant to most currently used antiviral medic

Cysteine protease inhibitor-3 (Compound 15), a cysteine protease inhibitor, exhibits anti-plasmodial activity, effectively inhibiting Pf3D7 (IC50 = 0.74 μM), PfW2 (IC50 = 1.05 μM), PfFP2 (IC50 = 3.5 μM), and PfFP3 (IC50 = 4.9 μM). It demonstrates efficacy against both drug-sensitive and drug-resistant parasites [1].

Grazoprevir sodium salt is a selective Hepatitis C virus NS3/4a protease inhibitor with broad activity across genotypes and resistant variants.

HIV-1 protease-IN-12 (compound 35b) serves as a potent inhibitor of HIV-1 protease, exhibiting an IC50 value of 0.51 nM, and demonstrates efficacy against drug-resistant variant [1].