A02.001 Proteopedia HIV-1_protease - the HIV-1 protease structure in interactive 3D. Proteopedia Flaps_Morph_for_HIV_Protease ... Without effective HIV protease, HIV virions remain uninfectious. Mature HIV protease exists as a 22 kDa homodimer, with each ... With its integral role in HIV replication, HIV protease has been a prime target for drug therapy. HIV protease inhibitors work ... The HIV-1 protease dimer (green and cyan) with active site Asp-25 in red. HIV-1 PR serves a dual purpose. Precursor HIV-1 PR is ...
In common usage HIV usually implies HIV-1. HIV-1 protease is one of the best known aspartic proteases, and an attractive target ... The Stanford HIV RT and Protease Sequence Database (also called the "HIV Drug Resistance Database") was formed in 1998 with HIV ... HIV protease inhibitors fit the active site of the HIV aspartic protease and were rationally designed utilizing knowledge of ... Brower, E. T.; Bacha, U. M.; Kawasaki, Y; Freire, E (2008). "Inhibition of HIV-2 protease by HIV-1 protease inhibitors in ...
HIV protease inhibitors; the antidepressant nefazodone; the cardiovascular drug gemfibrozil; the immunosuppressant ciclosporin ...
HIV-1 protease - a major drug-target for treatment of HIV Plasmepsin - a group of aspartyl proteases found in the Malaria- ... Aspartic proteases (also "aspartyl proteases", "aspartic endopeptidases") are a catalytic type of protease enzymes that use an ... Brik A, Wong CH (January 2003). "HIV-1 protease: mechanism and drug discovery". Organic & Biomolecular Chemistry. 1 (1): 5-14. ... Aspartyl proteases are a highly specific family of proteases - they tend to cleave dipeptide bonds that have hydrophobic ...
The peptide synthesizer was used in the synthesis of the HIV protease by Stephen Kent and others, and the development of a ... "Active HIV protease analog synthesized chemically". Chemical & Engineering News. 73 (9): 38. 27 February 1995. doi:10.1021/cen- ... including the synthesis of HIV-1 protease in a collaboration between Kent and Merck and the analysis of its crystalline ... "Enzymatic activity of a synthetic 99 residue protein corresponding to the putative HIV-1 protease" (PDF). Cell. 54 (3): 363-368 ...
Amprenavir is a HIV protease inhibitor. "Telzir Product information". Health Canada. 25 April 2012. Archived from the original ... Shen CH, Wang YF, Kovalevsky AY, Harrison RW, Weber IT (September 2010). "Amprenavir complexes with HIV-1 protease and its drug ... Fosamprenavir (FPV), sold under the brand names Lexiva and Telzir, is a medication used to treat HIV/AIDS. It is a prodrug of ... Fosamprenavir is used for the treatment of HIV-1 infections, typically but not necessarily in combination with low-dose ...
HIV-1 reverse transcriptase complexed with different inhibitors, by Temiz and Bahar, 2002. - HIV-1 protease, by Micheletti et ...
This effect is also used in HIV therapy, where ritonavir is used in combination with another protease inhibitor to similarly ... Hull MW, Montaner JS (April 2011). "Ritonavir-boosted protease inhibitors in HIV therapy". Annals of Medicine. 43 (5): 375-388 ... Coronaviral proteases cleave multiple sites in the viral polyprotein, usually after there are glutamine residues. Early work on ... The utility of targeting the 3CL protease in a real world setting was first demonstrated in 2018 when GC376 (a prodrug of GC373 ...
As this drug resembles the peptide that is the substrate of the HIV protease, it competes with the substrate in the enzyme's ... Antiviral drugs include protease inhibitors used to treat HIV/AIDS and Hepatitis C, reverse-transcriptase inhibitors targeting ... For example, the structure of another HIV protease inhibitor tipranavir is not based on a peptide and has no obvious structural ... Qiu X, Liu ZP (2011). "Recent developments of peptidomimetic HIV-1 protease inhibitors". Current Medicinal Chemistry. 18 (29): ...
Protease inhibitors, including ritonavir, effectively block HIV-1 protease, a crucial enzyme in the reproductive cycle of HIV-1 ... Ritonavir was demonstrated to have an in vitro potency of EC50=0.02µM on HIV-1 protease and highly sustained concentration in ... "Protease , NIH". clinicalinfo.hiv.gov. Retrieved January 11, 2023. Zhu, Ke-Wei (2023). "Deuremidevir and Simnotrelvir-Ritonavir ... February 1998). "Discovery of ritonavir, a potent inhibitor of HIV protease with high oral bioavailability and clinical ...
Protease inhibitors introduced, allowing HAART therapy against HIV; drastically reduces AIDS mortality. NASA's spacecraft ... Public education about safe sex curbed the spread of the HIV virus in developed countries. Generation X young people often ...
Agenerase (amprenavir), an HIV protease inhibitor, was co-developed by Vertex and GlaxoSmithKline for the treatment of HIV/AIDS ... Drugs developed include amprenavir, an HIV protease inhibitor; telaprevir, a protease inhibitor for treatment of hepatitis C; ... Scientists at Vertex first published the crystal structure for the protease of the hepatitis C virus in 1996. As part of the ... Vertex also developed Telaprevir, a protease inhibitor for treatment of hepatitis C. Telaprevir works by disabling a protein ...
... (DMP-450) is an antiviral drug which was developed as a treatment for HIV/AIDS. It acts as an HIV protease inhibitor ... Li P, Wang S, Wang H, Yan H (2019). "2-Symmetric HIV-1 Protease Inhibitors and Docking Study". Biological & Pharmaceutical ... "The synthesis and evaluation of cyclic ureas as HIV protease inhibitors: modifications of the P1/P1' residues". Bioorganic & ... polarization effects of the HIV-1 protease on selected high affinity inhibitors". Journal of Medicinal Chemistry. 47 (27): 6673 ...
Protease Women's Interagency HIV Study Corales RB, Shrestha NK, Taege AJ, et al. (2001). "Protease-sparing regimen in a real- ... Protease-sparing regimen, often abbreviated as PSR, is a method or therapy for treating people infected with HIV that involves ... It has been argued that such a regimen is not as potent as giving HIV patients with the strongest drugs as soon as it is ... Others believe that this might be considered a long-term strategy in order to reduce the amount of HIV, and in some instances ...
Adams LD, Tomasselli AG, Robbins P, Moss B, Heinrikson RL (Feb 1992). "HIV-1 protease cleaves actin during acute infection of ... Snásel J, Pichová I (1997). "The cleavage of host cell proteins by HIV-1 protease". Folia Biologica. 42 (5): 227-30. doi: ... Alzheimer amyloid precursor protein and pro-interleukin 1 beta as substrates of the protease from human immunodeficiency virus ... "Non-viral cellular substrates for human immunodeficiency virus type 1 protease". FEBS Letters. 278 (2): 199-203. doi:10.1016/ ...
Adams LD, Tomasselli AG, Robbins P, Moss B, Heinrikson RL (Feb 1992). "HIV-1 protease cleaves actin during acute infection of ... Snásel J, Pichová I (1997). "The cleavage of host cell proteins by HIV-1 protease". Folia Biologica. 42 (5): 227-30. doi: ... Alzheimer amyloid precursor protein and pro-interleukin 1 beta as substrates of the protease from human immunodeficiency virus ... "Non-viral cellular substrates for human immunodeficiency virus type 1 protease". FEBS Letters. 278 (2): 199-203. doi:10.1016/ ...
Snásel J, Pichová I (1997). "The cleavage of host cell proteins by HIV-1 protease". Folia Biol. (Praha). 42 (5): 227-30. doi: ... HIV Res. 3 (1): 87-94. doi:10.2174/1570162052773013. PMID 15638726. Le Rouzic E, Benichou S (2006). "The Vpr protein from HIV-1 ... Muthumani K, Desai BM, Hwang DS, Choo AY, Laddy DJ, Thieu KP, Rao RG, Weiner DB (2004). "HIV-1 Vpr and anti-inflammatory ... Zhao RY, Bukrinsky M, Elder RT (2005). "HIV-1 viral protein R (Vpr) & host cellular responses". Indian J. Med. Res. 121 (4): ...
Snásel J, Pichová I (1997). "The cleavage of host cell proteins by HIV-1 protease". Folia Biologica. 42 (5): 227-30. doi: ... Adams LD, Tomasselli AG, Robbins P, Moss B, Heinrikson RL (February 1992). "HIV-1 protease cleaves actin during acute infection ... Alzheimer amyloid precursor protein and pro-interleukin 1 beta as substrates of the protease from human immunodeficiency virus ... "Non-viral cellular substrates for human immunodeficiency virus type 1 protease". FEBS Letters. 278 (2): 199-203. doi:10.1016/ ...
Snásel J, Pichová I (1996). "The cleavage of host cell proteins by HIV-1 protease". Folia Biol. (Praha). 42 (5): 227-30. doi: ...
Snásel J, Pichová I (1997). "The cleavage of host cell proteins by HIV-1 protease". Folia Biol. (Praha). 42 (5): 227-30. doi: ... 1991). "Non-viral cellular substrates for human immunodeficiency virus type 1 protease". FEBS Lett. 278 (2): 199-203. doi: ...
Snásel J, Pichová I (1997). "The cleavage of host cell proteins by HIV-1 protease". Folia Biologica. 42 (5): 227-30. doi: ... Anderson JL, Hope TJ (Apr 2004). "HIV accessory proteins and surviving the host cell". Current HIV/AIDS Reports. 1 (1): 47-53. ... Kimura T, Hashimoto I, Nishikawa M, Fujisawa JI (1997). "A role for Rev in the association of HIV-1 gag mRNA with cytoskeletal ...
1992). "HIV-1 protease cleaves actin during acute infection of human T-lymphocytes". AIDS Res. Hum. Retroviruses. 8 (2): 291-5 ... Snásel J, Pichová I (1997). "The cleavage of host cell proteins by HIV-1 protease". Folia Biol. (Praha). 42 (5): 227-30. doi: ... 1991). "Actin, troponin C, Alzheimer amyloid precursor protein and pro-interleukin 1 beta as substrates of the protease from ... 1999). "Functional interaction between the cytoplasmic leucine-zipper domain of HIV-1 gp41 and p115-RhoGEF". Curr. Biol. 9 (21 ...
Snásel J, Pichová I (1997). "The cleavage of host cell proteins by HIV-1 protease". Folia Biol. (Praha). 42 (5): 227-30. doi: ...
Snásel J, Pichová I (1997). "The cleavage of host cell proteins by HIV-1 protease". Folia Biol. (Praha). 42 (5): 227-30. doi: ... 1991). "Non-viral cellular substrates for human immunodeficiency virus type 1 protease". FEBS Lett. 278 (2): 199-203. doi: ...
Snásel J, Pichová I (1997). "The cleavage of host cell proteins by HIV-1 protease". Folia Biologica. 42 (5): 227-30. doi: ... Fibroblasts secrete proteases, including matrix metalloproteinases, that digest the plasma fibronectin, and then the ... Fragmentation of fibronectin by proteases has been suggested to promote wound contraction, a critical step in wound healing. ...
Snásel J, Pichová I (1997). "The cleavage of host cell proteins by HIV-1 protease". Folia Biol. (Praha). 42 (5): 227-30. doi: ...
... and protease inhibitors (HIV treatment). Testosterone can also alter the effects of other drugs: Increases the blood thinning ...
Perales C, Carrasco L, Ventoso I (2003). "Cleavage of eIF4G by HIV-1 protease: effects on translation". FEBS Lett. 533 (1-3): ...
Snásel J, Pichová I (1997). "The cleavage of host cell proteins by HIV-1 protease". Folia Biologica. 42 (5): 227-230. doi: ... Lake JA, Carr J, Feng F, Mundy L, Burrell C, Li P (February 2003). "The role of Vif during HIV-1 infection: interaction with ...
Snásel J, Pichová I (1997). "The cleavage of host cell proteins by HIV-1 protease". Folia Biologica. 42 (5): 227-30. doi: ... Adams LD, Tomasselli AG, Robbins P, Moss B, Heinrikson RL (February 1992). "HIV-1 protease cleaves actin during acute infection ... Alzheimer amyloid precursor protein and pro-interleukin 1 beta as substrates of the protease from human immunodeficiency virus ... "Non-viral cellular substrates for human immunodeficiency virus type 1 protease". FEBS Letters. 278 (2): 199-203. doi:10.1016/ ...
"Computing Clinically Relevant Binding Free Energies of HIV-1 Protease Inhibitors". Journal of Chemical Theory and Computation. ...