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.

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].

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

Darunavir Ethanolate (UIC 94017) is an HIV PROTEASE INHIBITOR that is used in the treatment of AIDS and HIV INFECTIONS. Due to the emergence of ANTIVIRAL DRUG RESISTANCE when used alone, it is administered in combination with other ANTI-HIV AGENTS.