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Adaptability and flexibility of HIV‐1 protease
European Journal of Biochemistry, 2003Even though more than 200 three‐dimensional structures of HIV‐1 protease complexed to a variety of inhibitors are available in the Protein Data Bank; very few structures of unliganded protein have been determined. We have recently solved structures of unliganded HIV‐1 protease tethered dimer mutants to resolutions of 1.9 Å and 2.1 Å, and have found ...
Mukesh, Kumar, Madhusoodan V, Hosur
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Complete mutagenesis of the HIV-1 protease
Nature, 1989Retroviruses encode a protease which needs to be active for the production of infectious virions. A disabling mutation in the protease results in the production of non-infectious virus particles and examination of proteins from these mutant virions reveals unprocessed Gag and Gag-Pol precursor proteins, the substrates of the viral protease.
D D, Loeb +5 more
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Endothiopeptide inhibitors of HIV-1 protease
Bioorganic & Medicinal Chemistry Letters, 1998Endothiopeptide inhibitors of HIV-1 protease were synthesized by chemical and enzymatic methods to individually replace each backbone amide bond in 1 with a thioamide-linkage. Interestingly, agent 7, which contains a thioamide-linkage between the P2' and P3' positions of 1, was the most potent, competitive inhibitor of HIV-1 protease with a Ki of 3.4 ...
S, Yao, R, Zutshi, J, Chmielewski
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Cysteine Nitrosylation Inactivates the HIV-1 Protease
Biochemical and Biophysical Research Communications, 1998Nitric oxide (NO) may modulate the catalytic activity of cysteine-containing enzymes. HIV-1 protease action is modulated by the redox equilibrium of Cys67 and Cys95 regulatory residues. In the present study, the inhibitory effect of NO, released by the NO-donor (+/-)-(E)-4-ethyl-2-[(E)-hydroxyimino]-5-nitro-3-hexenamide (NOR-3), on the aspartyl HIV-1 ...
PERSICHINI T +3 more
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AIDS clinical review, 1997
Objective. —The clinical care of people infected with human immunodeficiency virus (HIV) has been substantially affected by the introduction of HIV-specific protease inhibitors (Pis). The 4 Pls available are saquinavir mesylate, ritonavir, indinavir sulfate, and nelfinavir mesylate.
S G, Deeks, P A, Volberding
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Objective. —The clinical care of people infected with human immunodeficiency virus (HIV) has been substantially affected by the introduction of HIV-specific protease inhibitors (Pis). The 4 Pls available are saquinavir mesylate, ritonavir, indinavir sulfate, and nelfinavir mesylate.
S G, Deeks, P A, Volberding
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The Evolution of Catalytic Function in the HIV-1 Protease
Journal of Molecular Biology, 2011The evolution of species is a complex phenomenon based on the optimization of a multidimensional function referred to as fitness. At the level of biomolecular evolution, the fitness function can be reduced to include physiochemical properties relevant to the biological function of a particular molecule.
Singh, M. K. +3 more
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HIV-1 protease: mechanism and drug discovery
Organic & Biomolecular Chemistry, 2002AbstractFor Abstract see ChemInform Abstract in Full Text.
Ashraf, Brik, Chi-Huey, Wong
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Cold Denaturation of the HIV-1 Protease Monomer
Biochemistry, 2017The human immunodeficiency virus-1 (HIV-1) protease is a complex protein that in its active form adopts a homodimer dominated by β-sheet structures. We have discovered a cold-denatured state of the monomeric subunit of HIV-1 protease that is populated above 0 °C and therefore directly accessible to various spectroscopic approaches.
H. I. Rösner +7 more
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The specificity of the HIV-1 protease
Perspectives in Drug Discovery and Design, 1993The protease of HIV-1 is able to recognize many different sequences as substrates. Despite the diversity of these sequences, some of the determinants of HIV-1 protease specificity have been clarified by recent studies. These studies include the examination of known processing-site sequences, the use of polypeptides and native protein as substrates in ...
Steve C. Pettit +2 more
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Heterocyclic HIV-1 Protease Inhibitors
Organic Letters, 1999[formula: see text] A series of simple heterocyclic HIV-1 protease inhibitors were developed on the basis of size, shape, and electronic complementarity to the active site of the enzyme. The C2-symmetric heterocycles do not contain a transition-state isostere nor are they active site directed irreversible inhibitors; thus, they represent the success of
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