hiv protease

HIV Protease Substrate 1 is a fluorogenic compound that offers insights into the enzymatic activity of HIV protease, making it a valuable tool for studying this aspect.

HIV protease-IN-1 (compound 1·succinate), a potent non-peptidic inhibitor of HIV protease, is used in AIDS research [1].

HIV Protease Substrate 1 TFA, a fluorogenic substrate for HIV protease, facilitates the investigation of the enzyme's activity [1].

HIV Protease Substrate I, a chromogenic substrate for HIV-1 protease, contains the protease's cleavage site [1].

HIV Protease Substrate IV, a substrate for HIV (human immunodeficiency virus) protease, facilitates the measurement of HIV-1 protease activity [1].

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, 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].

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-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.

5-Fluorouracil (5-FU) is a uracil analog and inhibitor of DNA synthesis, exhibiting antitumor activity by affecting pyrimidine synthesis through thymidylate synthase inhibition; it induces apoptosis and autophagy.

(-)-Epigallocatechin Gallate (EGCG) is a phenolic antioxidant polyphenol flavonoid found in plants such as green and black tea, which inhibits telomerase and DNA methyltransferase, blocks the activation of EGF receptors and HER-2 receptors, inhibits cellular oxidation, and prevents free radical damage to cells.

Q-VD-OPh is an irreversible caspase inhibitor with an IC50 value of 48 nM against caspase-7 and between 25 and 400 nM against caspase-1, 3, 8, 9, 10, 12. Q-VD-OPh inhibits HIV infection and can cross the blood-brain barrier.

3-Deazaadenosine hydrochloride is an inhibitor of S-adenosylhomocysteine hydrolase (Ki: 3.9 µM). It has anti-inflammatory, anti-proliferative, and anti-HIV activity.

Doxorubicin hydrochloride is an anthracycline antibiotic with cytotoxic and antitumor activity. It is an effective inhibitor of human DNA topoisomerase I and II, with IC50 values of 0.8 μM and 2.67 μM, respectively. In addition to inhibiting DNA topoisomerases, it can reduce the phosphorylation of AMPK and its downstream target, acetyl-CoA carboxylase. Doxorubicin hydrochloride also induces apoptosis and autophagy. In animal studies, it is commonly used to induce models of acute renal failure, chronic kidney injury, and heart failure.