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*  Discovery and development of HIV-protease inhibitors
Tipranavir is a nonpeptidic HIV-1 protease inhibitor and reached the market in 2005. Unlike other HIV protease inhibitors on ... HIV protease inhibitors fit the active site of the HIV aspartic protease and were rationally designed utilizing knowledge of ... In 2009, ten protease inhibitors have reached the market for treatment against HIV but one protease inhibitor, amprenavir, was ... All the FDA approved protease inhibitors are listed below. All the HIV protease inhibitors on the market contain a central core ...
*  Simvastatin
HIV protease inhibitors; the antidepressant nefazodone; the cardiovascular drug gemfibrozil; the immunosuppressant ciclosporin ... Tobert JA (2003). "Lovastatin and beyond: the history of the HMG-CoA reductase inhibitors". Nat Rev Drug Discov. 2 (7): 517-26 ... This discovery encouraged scientists worldwide to find an effective inhibitor of this enzyme.[citation needed] By 1976, Akira ... While developing and researching lovastatin, Merck scientists synthetically derived a more potent HMG-CoA reductase inhibitor ...
*  Castor oil
... an HIV protease inhibitor; Tacrolimus, an immunosuppressive drug (contains HCO-60, polyoxyl 60 hydrogenated castor oil);[ ... April 2001). "Circulating metabolites of the human immunodeficiency virus protease inhibitor nelfinavir in humans: Structural ... as a mold inhibitor, and in packaging. Polyoxyethylated castor oil (e.g., Kolliphor EL) is also used in the food industries. In ... a mitotic inhibitor used in cancer chemotherapy; Sandimmune (cyclosporine injection, USP), an immunosuppressant drug widely ...
*  Lopinavir/ritonavir
... like several HIV protease inhibitors, its blood levels are greatly increased by low doses of ritonavir, a potent inhibitor of ... researchers found the points of attack of the HIV protease inhibitors - agents that block the breakdown of proteins. Protease ... Both medications are HIV protease inhibitors. Ritonavir functions by slowing down the breakdown of lopinavir. Lopinavir/ ... in an attempt to improve on the HIV resistance and serum protein-binding properties of the company's earlier protease inhibitor ...
*  Fosamprenavir
Amprenavir is a HIV protease inhibitor. Eron J Jr; Yeni P; Gathe J Jr; et al. (2006). "The KLEAN study of fosamprenavir- ... is a drug for the treatment of HIV infections. It is a pro-drug of the protease inhibitor and antiretroviral drug amprenavir. ... Shen, C. H.; Wang, Y. F.; Kovalevsky, A. Y.; Harrison, R. W.; Weber, I. T. (2010). "Amprenavir complexes with HIV-1 protease ... When combining fosamprenavir with low doses of the CYP3A4 inhibitor ritonavir, this interaction is intended as it allows for ...
*  Joshua Boger
Drugs developed include amprenavir, an HIV protease inhibitor; telaprevir, a protease inhibitor for treatment of hepatitis C; ... Agenerase (amprenavir), an HIV protease inhibitor, was co-developed by Vertex and GlaxoSmithKline for the treatment of HIV/Aids ... Vertex also developed Telaprevir, a protease inhibitor for treatment of hepatitis C. Telaprevir works by disabling a protein ... Scientists at Vertex first published the crystal structure for the protease of the hepatitis C virus in 1996. As part of the ...
*  OX1001
... is an analog of the already approved HIV protease inhibitor, saquinavir. HIV protease inhibitor drugs not only work ... Adding a nitrate ester functional group to HIV protease inhibitors has been found to curb these negative effects as well as ... OX1001 is a nitrate ester analog of the approved HIV protease inhibitor, saquinavir. This modification increases the anti- ... "The new and less toxic protease inhibitor saquinavir-NO maintains anti-HIV-1 properties in vitro indistinguishable from those ...
*  Chiral auxiliary
The HIV protease inhibitor Tipranavir is marketed for the treatment of AIDS. The first enantioselective medicinal chemistry ... 1998). "Tipranavir (PNU-140690): A Potent, Orally Bioavailable Nonpeptidic HIV Protease Inhibitor of the 5,6-Dihydro-4-hydroxy- ... 1991). "Inhibitors of Cholesterol Biosynthesis. 3. Tetrahydro-4-hydroxy-6-[2-( lH-pyrrol-l-yl)ethyl]-2H-pyran-2-one Inhibitors ... In the presence of butylated hydroxytoluene (BHT) used as a polymerization inhibitor, a toluene solution of the adduct between ...
*  Inte:Ligand
Parallel Screening and Activity Profiling with HIV Protease Inhibitor Pharmacophore Models J. Chem. Inf. Model; 2007; 47(2); ... Other applications include the discovery of new Myeloperoxidase ligands, HIV reverse transcriptase inhibitors, applications in ... the development of models to predict HIV Protease activity, Cytochrome P450 activity prediction , and simulation models for the ... 3-dicarboxylic acid inhibitors of bacterial MurD and MurE ligases by structure-based virtual screening approach". Bioorganic & ...
*  Atazanavir
doi:10.2147/HIV.S79956. PMC 4396582 . Graziani, Amy L (June 17, 2014). "HIV protease inhibitors". UpToDate. Bold, G; Fässler, A ... It is of the protease inhibitor (PI) class and works by blocking HIV protease. Atazanavir was approved for medical use in the ... Lv, Z; Chu, Y; Wang, Y (2015). "HIV protease inhibitors: a review of molecular selectivity and toxicity. ". HIV/AIDS - Research ... "New Aza-Dipeptide Analogues as Potent and Orally Absorbed HIV-1 Protease Inhibitors: Candidates for Clinical Development". ...
*  Ice-nine
"Elucidation of crystal form diversity of the HIV protease inhibitor ritonavir by high-throughput crystallization". Proc. Natl. ...
*  Nelfinavir
... is a protease inhibitor: it inhibits HIV-1 and HIV-2 proteases. HIV protease is an aspartate protease which splits ... All protease inhibitors bind to the protease, the precise mode of binding determines how the molecule inhibits the protease. ... Antiviral for AIDS, HIV-1 protease inhibitor. X. Rabasseda, A.M. Martel, J. Castañer. Pai, VB; Nahata, MC (March 1999). " ... Pyrko P, Kardosh A, Wang W, Xiong W, Schönthal AH, Chen TC (2007). "HIV-1 protease inhibitors nelfinavir and atazanavir induce ...
*  Paul S. Berry
"A randomized double-blind study of the oral HIV protease inhibitor, L-735,524 vs. Zidovudine (ZDV) in p24 antigenemic, HIV-1 ... "Efficacy and safety of the HIV protease inhibitor indinavir sulfate (MK 639) at escalating doses". 3rd Annual Conference of ... Through the 1990s, HIV/AIDS rapidly became a manageable long term disease in non-third world industrialized nations, and Berry ... "Effects of Administration of Antibody to Human Alpha-Fetoprotein in Persons Seropositive for HIV-1 on CD4+ Cell Count and Viral ...
*  Ritonavir
... was originally developed as an inhibitor of HIV protease. It is one of the most complex inhibitors. It is now rarely ... Ritonavir is of the protease inhibitor class. It is often used to inhibit the enzyme that metabolizes other protease inhibitors ... "Elucidation of crystal form diversity of the HIV protease inhibitor ritonavir by high-throughput crystallization". Proc. Natl. ... "Pharmacological and therapeutic properties of ritonavir-boosted protease inhibitor therapy in HIV-infected patients". Journal ...
*  Cobicistat
Including HIV Protease Inhibitors and GS-7340, in Vitro". Antimicrobial Agents and Chemotherapy. 56 (10): 5409-5413. doi: ... Additionally, in existence are a fixed-dose combination of cobicistat and protease inhibitor darunavir (darunavir/cobicistat; ... Highleyman, L. Elvitegravir "Quad" Single-tablet Regimen Shows Continued HIV Suppression at 48 Weeks. HIV and Hepatitis.com R ... an HIV integrase inhibitor. By combining cobicistat with elvitegravir, higher concentrations of the latter are achieved in the ...
*  Amprenavir
Structure-activity studies on renin inhibitors proved to be of great value for developing HIV protease inhibitors. ... Amprenavir (original brand name Agenerase, GlaxoSmithKline) is a protease inhibitor used to treat HIV infection. It was ... Shen, C. H.; Wang, Y. F.; Kovalevsky, A. Y.; Harrison, R. W.; Weber, I. T. (2010). "Amprenavir complexes with HIV-1 protease ... The amino acid sequence cleaved by renin was found to be fortuitously the same as that required to produce the HIV peptide coat ...
*  Pravastatin
Specific HIV protease inhibitors such as: lopinavir and ritonavir (Kaletra), and ritonavir (Norvir) taken with darunavir ( ... Jonathan A. Tobert Lovastatin and beyond: the history of the HMG-CoA reductase inhibitors Nature Reviews Drug Discovery 2, 517- ... As a reversible competitive inhibitor, pravastatin sterically hinders the action of HMG-CoA reductase by occupying the active ...
*  Johnson & Johnson
... a non-nucleoside HIV polymerase inhibitor; and Prezista (darunavir), an HIV protease inhibitor. Telaprevir sales are expected ... Darunavir in combination with HIV polymerase inhibitors is recommended as a first line treatment option for treatment naive ... Key infectious diseases products include Incivio (telaprevir), a hepatitis C protease inhibitor; Intelence (Etravirine), ... In March 2015, Janssen licensed Tipofarnib (a farnesyl transferase inhibitor) to Kura Oncology who will assume sole ...
*  Scott Kurowski
In 2000, he built a grid computing system searching for HIV protease inhibitors for The Scripps Research Institute. In 2002 he ...
*  Ivermectin
These drugs include statins, HIV protease inhibitors, many calcium channel blockers, and glucocorticoids such as dexamethasone ... of increased absorption past the blood-brain barrier exists when ivermectin is administered along with other CYP3A4 inhibitors ...
*  Management of HIV/AIDS
... protease inhibitor (PI) or Integrase inhibitors (also known as integrase nuclear strand transfer inhibitors or INSTIs) as a " ... both latter are protease inhibitors) In the case of the protease inhibitor based regimens, ritonavir is used at low doses to ... Examples of HIV protease inhibitors are lopinavir, indinavir, nelfinavir, amprenavir and ritonavir. Darunavir and atazanavir ... Protease inhibitors block the viral protease enzyme necessary to produce mature virions upon budding from the host membrane. ...
*  Multidrug resistance-associated protein 2
Gimenez F, Fernandez C, Mabondzo A (June 2004). "Transport of HIV protease inhibitors through the blood-brain barrier and ... The nucleoside phosphonate adefovir is a MRP2 inhibitor that has been linked to kidney disease. Tenofovir and cidofovir are ... and non-nucleoside reverse transcriptase inhibitors". Drug Metab. Dispos. 35 (3): 340-4. doi:10.1124/dmd.106.012765. PMID ...
*  Felodipine
HIV protease inhibitors, and grapefruit juice. CYP3A4 activators, which decrease the amount of felodipine available per dose, ... CYP3A4 inhibitors, which increase the amount of felodipine available per dose, include cimetidine, erythromycin, itraconazole, ...
*  Alfred L. Wilds
70+ years later, synthesis of such complex targets as HIV protease inhibitors are as a result of the equilenin synthesis by Al ...
*  WHO Model List of Essential Medicines for Children
For use only in patients with HIV receiving protease inhibitors. For treatment of latent TB infection (LTBI) only Terizidone ... Nucleoside/Nucleotide reverse transcriptase inhibitors Entecavir No listings in this section. Diloxanide Metronidazole ...
*  Caspase-activated DNase
Nie Z, Phenix BN, Lum JJ, Alam A, Lynch DH, Beckett B, Krammer PH, Sekaly RP, Badley AD (November 2002). "HIV-1 protease ... Once the inhibitor is released and in order to properly function, two CAD monomers need to come together to form a functional ... Therefore, ICAD has a double function; it acts as a CAD inhibitor and also as a chaperone for CAD synthesis assisting the ... McCarty JS, Toh SY, Li P (October 1999). "Study of DFF45 in its role of chaperone and inhibitor: two independent inhibitory ...