hiv protease

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-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].

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

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

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].

HIV-1, HIV-2 Protease Substrate is a compound serving as the substrate for the proteases of both HIV-1 and HIV-2, featuring four residues that allow for conservative substitutions at the substrate binding sites of these enzymes [1].

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

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-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-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-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.

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].

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.

HIV-1 protease-IN-4 (Compound II-22), a potent inhibitor of the HIV-1 protease, acts as a prodrug for atazanavir. It notably enhances the bioavailability of atazanavir 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 Protease Substrate I, a chromogenic substrate for HIV-1 protease, contains the protease's cleavage site [1].

HIV-1 protease-IN-10 (Compound 2), exhibiting 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 Protease Substrate IV, a substrate for HIV (human immunodeficiency virus) protease, facilitates the measurement of HIV-1 protease activity [1].

Ritonavir (ABT 538) is a peptidomimetic agent that inhibits both HIV-1 and HIV-2 proteases. Ritonavir is highly inhibited by serum proteins but boosts the effect of other HIV proteases by blocking their degradation by cytochrome P450.

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

2-Amino-6-bromopyridine has inhibitory effect on HIV-68 protease.

L 756423 (L756423) is a novel potent and selective and competitive HIV protease inhibitor with a Ki value of 0.049 nM for HIV-1 PR.L 756423 blocks the spread of HIV(IIIb)-infected MT25 lymphocytes at 0.50-0.1 nM and can be used for the study of Acquired Immunodeficiency Syndrome (AIDS).

DPC-681 is a potent and selective HIV protease inhibitor (IC90s: 4 to 40 nM for wild-type HIV-1).

Lopinavir (ABT-378) is a peptidomimetic HIV protease inhibitor that retains activity against HIV protease with the Val 82 mutation. Lopinavir is less affected by binding to serum proteins than the structurally-related drug ritonavir.

Theaflavin 3,3'-digallate (8-Gingerol) , a major polyphenol found in black tea, is an inducer of oxidative stress which has anti-inflammatory and cancer chemopreventive actions, it reduces tumor angiogenesis by downregulating HIF-1αand VEGF.

Ebselen (CCG-39161) is a organoselenium compound with anti-inflammatory, anti-oxidant and cytoprotective activity. Ebselen acts as a glutathione peroxidase mimetic and is thereby able to prevent cellular damage induced by reactive oxygen species (ROS). In addition, this agent inhibits the activity of a variety of enzymes including nitric oxide synthase (NOS), 5-lipoxygenase, cyclooxygenase, protein kinase C (PKC), NADPH oxidase and gastric H+/K+-ATPase. Furthermore, ebselen may be neuroprotective due to its ability to neutralize free radicals upon NMDA receptor activation thus, reducing lipoperoxidation mediated by glutamate-induced excitotoxicity.

Pepstatin (Pepsin Inhibitor S 735A) is a specific aspartic proteases inhibitor produced by actinomycetes, and inhibits the aspartic proteases cathepsin D, pepsin and renin.

Atazanavir (BMS-232632)(BMS-232632) is an highly effective HIV-1 protease inhibitor.

Nelfinavir (AG1341) is an antiretroviral drug used in the treatment of the human immunodeficiency virus (HIV) (Ki=2 nM). Nelfinavir is a broad-spectrum, anticancer agent.

Plerixafor octahydrochloride (JM3100 octahydrochloride) blocks the binding of stromal cell-derived factor (SDF-1alpha) to the cellular receptor CXCR4, resulting in hematopoietic stem cell (HSC) release from bone marrow and HSC movement into the peripheral circulation. Plerixafor is a bicyclam with hematopoietic stem cell-mobilizing activity.

Ganodermanondiol exhibits potent cytoprotective effects on t-BHP-induced hepatotoxicity in human liver-derived HepG2 cells, presumably through Nrf2-mediated antioxidant enzymes and AMPK.

Ganoderic acid GS-2 inhibits the activity of the human immunodeficiency virus-1 (HIV-1) protease.

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

Ganolucidic acid A exhibits cytotoxicity, has inhibitory activities against human HeLa cervical cancer cell lines. It shows significant anti-human immunodeficiency virus (anti-HIV)-1 protease activity with IC50 values of 20-90 microM.

Absinthin (Absynthin) is a weak HIV-1 protease inhibitor.

Cytochalasin A is a cell-permeable fungal toxin and is an oxidized derivative of cytochalasin B. Cytochalasin A is an inhibitor of HIV-1 protease (IC50 = 3 μM), inhibits actin polymerization and interferes with microtubule assembly by reacting with sulfhy

Jacoumaric acid is a lead molecule from the library or database of natural compounds as a HIV-1 protease inhibitor.

Indinavir (IDV) is an inhibitor of protease that is used as part of highly active antiretroviral therapy for the treatment of HIV/AIDS.

Ganoderic acid GS-1, an extensively oxygenated lanostane-type triterpenoid, exhibits anti-HIV-1 protease activities, displaying an IC50 value of 58 μM [1].

PD 099560 is a non-peptide inhibitor of HIV-1 protease, a significant target enzyme in AIDS research.

PL 100 could inhibit HIV-1 protease.

DMP 323 is a potent inhibitor of HIV-1 protease.

1. Isosinensetin (6-Demethoxynobiletin) shows antioxidant and HIV-1 protease inhibiting activities.

Gomisin G is a natural compound and exhibits potent anti-HIV activity (EC50: 0.006 μg/mL; therapeutic index: 300). It is a good substrate of CYP2C9.

L 694746 is an inhibitor of HIV-1 protease.

ICeD-2, an inducer of cell death, effectively induces the killing of HIV-1 infected cells, a process reliant on HIV-1 protease activity. It significantly inhibits the hydrolysis of Gly-Pro-AMC by dipeptidyl peptidases DPP8 and DPP9, and robustly stabilizes DPP9 in peripheral blood mononuclear cells (PBMCs) [1].

Ac-Ser-Gln-Asn-Tyr-Pro-Val-Val-NH2 is a peptide substrate specific to HIV-1 protease, serving as the variable component in peptidolytic assays designed to measure the enzyme's inhibition [1] [2].

SK&F 108361 is a symmetric diol that binds HIV-1 protease symmetrically.

L-lysine lactam is a building block.1,2It has been used in the synthesis of lysine sulfonamide HIV protease inhibitors, as well as bengamide derivatives within vitroanticancer activity.

VIR-165 is a modified form of virus inhibitory peptide (VIRIP), which corresponds to residues 353 to 372 of C-proximal region of human alpha1-antitrypsin, the most abundant circulating serine protease inhibitor. VIRIP inhibits a wide variety of human immu

PD 135390 is a HIV-1 protease inhibitors identified by rational selection. Inactivation of the protease prevents infectious virion formation.