hiv-1 protease

HIV-1 Protease is synthesized as part of the larger Gag-Pol precursor protein. This enzyme is crucial for cleaving itself from the precursor and processing the Gag and Gag-Pol polyproteins into the mature, structurally and functionally essential proteins needed for viral maturation.

Ursonic Acid (TOS-BB-0966) belongs to the family of Ursane Triterpenes whose structure is based on the pentacyclic ursane skeleton. It has potential as HIV-1 Protease Inhibitor.

The N-dealkylated metabolite (M1) of Atazanavir, a HIV protease inhibitor.

Cytochalasin A, a cell-permeable fungal toxin and oxidized derivative of cytochalasin B, is an inhibitor of HIV-1 protease (IC50 = 3 μM). It inhibits actin polymerization, interferes with microtubule assembly by reacting with sulfhydryl groups, and serves as an antibiotic and bactericidal active agent.

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.

Escin IA (Escin IA;Aescin IA) is a triterpene saponin isolated from horse chestnut, which inhibits HIV-1 protease with IC50 values of 35 μM. Escin IA has anti-TNBC metastasis activity, and its action mechanisms involved inhibition of epithelial-mesenchymal transition process by down-regulating LOXL2 expression[1][2].

Ganoderic acid B is a chemical marker in quality control of G. lucidum and related products. Ganoderic acid B-containing herbs has potential influence towards therapeutic window of trifluoperazine.Ganoderic acid B has antinociceptive effect

Ganoderic acid C1 has anti-inflammatory activity, has potential for treating TNF-α± mediated inflammation in asthma and other inflammatory diseases. Ganoderic acid C1 has anti-tumor-promoting activity. It is moderately active inhibitors against HIV-1 prot

Oleoside can be extracted from Olea europaea and Zizyphus lotus L. twigs and may be used to inhibit HIV-1 protease.

HIV-1protease-IN-13 (compound 18d) is a potent inhibitor of HIV-1 protease (HIV-1protease) with an IC50 value of 0.54 nM. Additionally, HIV-1protease-IN-13 demonstrates effective activity against both HIV-1DRVRS (DRV resistant mutation) and HIV-1NL4_3 variants (wild-type).

HIV-1protease-IN-15 (Compound 27) is an orally active selective inhibitor of HIV-1 protease (HIV-1protease) with a pIC50 of 9.347. It inhibits the maturation of HIV proteins, effectively blocking viral replication. HIV-1protease-IN-15 shows potential for research into HIV-1 infection.

HIV-1 protease-IN-1 is a potent inhibitor of HIV-1 protease (IC50: 90 pM). HIV-1 protease-IN-1 has antiviral activity against B-HIV (EC50: 89 nM): HIV-1 protease-IN-1 was able to act on C-HIV strain ZM246 (EC50: 13.59 nM) and C-HIV strain Indie (EC50: 8.23 nM).

HIV-1 protease-IN-6 (compound 17d) is a potent HIV-1 protease inhibitor with an IC50 of 21 pM and a Ki of 4.7 pM, demonstrating significant antiviral activity against DRV (darunavir) resistant mutants, surpassing its inhibition efficacy against wild-type viruses.

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

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.

HIV-1 protease-IN-4 (Compound II-22), a potent inhibitor of the HIV-1 protease, acts as a prodrug for atazanavir and significantly enhances its bioavailability in rat plasma, achieving a 5-fold increase in the area under the curve (AUC) and a 67-fold increase in concentration at 24 hours (C24) compared to oral administration of atazanavir alone [1].

HIV-1 protease-IN-7 (compound 16) is an orally active HIV-1 protease inhibitor with an IC50 of 3.52 nM and an EC50 of 37 nM [1].

HIV-1 protease-IN-8 (compound 34b) is a potent inhibitor of the HIV-1 protease enzyme with an IC50 of 0.32 nM. It exhibits 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].

HIV-1 protease-IN-9 (compound 5b), a potent HIV-1 protease inhibitor, exhibits strong antiviral efficacy with a dissociation constant (K_i) of 0.028 nM and a half-maximal inhibitory concentration (IC_50) of 66.8 nM [1].

HIV-1 protease-IN-10 (Compound 2) exhibits HIV-1 latency reversing activity (IC50: 0.22 μM), selectively binds to the PKCδ C1b domain (IC50: 0.69 μM), and demonstrates stability against esterase-mediated hydrolysis [1].

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 a drug-resistant variant [1].

HIV-1 protease-IN-12 (compound 35b) is a potent HIV-1 protease inhibitor with an IC50 value of 0.51 nM, demonstrating efficacy against drug-resistant variants [1].

HIV-1protease-IN-14 (compound 5ae) is an effective inhibitor of HIV-1protease, exhibiting Ki values of 0.28 nM and 56.9 nM against WTHIV-1PR and R41THIV-1PR, respectively. This compound also demonstrates low cytotoxicity.

HIV-1, HIV-2 Protease Substrate serves as a substrate for the proteases of both HIV-1 and HIV-2, featuring four residues that permit conservative substitutions at the enzyme substrate binding sites [1].