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HIV Protease

Human immunodeficiency virus (HIV) protease, belonging to the aspartic proteinase family, is an enzyme encoded by the pol open reading frame (ORF) of HIV genome that catalyze the posttranslational processing of the HIV polyproteins to yield structural proteins of the viral core and enzymes. The chemical structure of a HIV protease molecule is a symmetrical homodimer in which the interface is formed primarily by a four-stranded antiparallel β-sheet. A conserved D25-T26-G27 triad has been identified in each HIV protease monomer, which is positioned in a loop forming part of the catalytic site. HIV protease has been found to cleave peptide bonds in the p55 gag and p160 gag-pol polyproteins as well as in various cellular proteins in vitro, including calmodulin, pro-interleukin 1β and NF-KB.

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  1. Cat.No. Product Name Information
  2. A8204 Lopinavir Lopinavir (also known as ABT-378) is a highly potent inhibitor of human immunodeficiency virus (HIV) protease that potently inhibits wild-type and mutant HIV protease with inhibition constant Ki values ranging from 1.3 to 3.6 pM.
  3. B4950 Darunavir Ethanolate
  4. A8205 Atazanavir Atazanavir is a novel and potent azapeptide protease inhibitor that specifically inhibits the human immunodeficiency virus type 1 (HIV-1) protease enzyme with inhibition constant Ki of 66 nmol/L and also inhibits the viral replication of HIV-1 with 50% effective concentration EC50 ranging from 2.6 to 5.3 nmol/L.
  5. A4040 Atazanavir sulfate (BMS-232632-05) Atazanavir sulfate (BMS-232632-05) is the sulfate salt form of atazanavir, a potent protease inhibitor (IP) for the treatment of human immunodeficiency virus 1 (HIV-1) infection, which prevents the formation of mature HIV virions through the selective inhibition of the virus-specific processing of viral gag and gag-pol polyproteins in infected cells.
  6. A8203 Ritonavir Ritonavir, previously known as ABT-538, is a potent inhibitor of human immunodeficiency virus type 1 (HIV-1) protease that exhibits potent in vitro inhibition against HIV-1 strain as well as HIV-2 strain with 50% effective concentration EC50 values of 0.022 μM and 0.16 μM respectively.
  7. A8206 Darunavir Darunavir is an orally-bioavailable non-peptidic inhibitor of human immunodeficiency virus type 1 (HIV-1) protease that selectively inhibits HIV-1 protease enzyme induced cleavage of gag and gag-pol poly-proteins preventing the maturation of virions and also inhibits the dimerization of HIV-1 protease suppressing proteolytic activity and subsequent replication of HIV-1.
  8. A8201 Amprenavir (agenerase) Amprenavir (agenerase), an N,N-disubstituted hydroxyethylamino sulfonamide, is a novel inhibitor of human immunodeficiency virus type 1 (HIV-1) protease that potently inhibits the activity of HIV-1 protease with a value of 50% inhibition concentration IC50 of 0.6 nM and also weakly inhibits HIV-2 protease with IC50 value of 19 nM.
  9. A3253 BMS-626529 BMS-626529 is a member of the new drug class of HIV-1 attachment inhibitors currently in development.
  10. A3421 Fosamprenavir Calcium Salt GW433908G is a selective inhibitor of antiretroviral protease with the concentration of 1395 mg nM once daily in clinical trial [1].
  11. A3462 HIV-1 integrase inhibitor 2 The human immunodeficiency virus (HIV) is the causative agent for the acquired immunodeficiency syndrome (AIDS), then HIV integrase is an attractive target for new anti-HIV drugs.

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