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C-5-Modified Tetrahydropyrano-Tetrahydofuran-Derived Protease Inhibitors (PIs) Exert Potent Inhibition of the Replication of HIV-1 Variants Highly Resistant to Various PIs, including Darunavir. (Research article)

Journal of Virology

Feb 2016, 90 (5) 2180-2194; DOI: 10.1128/JVI.01829-15

X-ray structures: PDB IDs: 5COK, 5CON, 5COO and 5COP

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Insights into the mechanism of drug resistance: X-ray structure analysis of multi-drug resistant HIV-1 protease ritonavir complex. (Research article)

Biochemical and Biophysical Research Communications

February 2013, 431(2): 232-238

Related X-ray crystal structure: PDB ID: 4EYR

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A multi-drug resistant HIV-1 protease is resistant to the dimerization inhibitory activity of TLF-PafF. (Research article)

Journal of Molecular Graphics and Modelling

September 2014, 53: 105-111.

DOI: 10.1016/j.jmgm.2014.06.010

Related X-ray crystal structure: PDB ID: 4NKK

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A Conserved Hydrogen-Bonding Network of P2 bis-Tetrahydrofuran-Containing HIV-1 Protease Inhibitors (PIs) with a Protease Active-Site Amino Acid Backbone Aids in Their Activity against PI-Resistant HIV. (Research article)

Antimicrobial Agents and Chemotherapy

Jun 2014, 58 (7) 3679-3688; DOI: 10.1128/AAC.00107-14

X-ray structures: PDB IDs: 4NJS, 4NJT, 4NJU and 4NJV

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P1 and P1′ para-fluoro phenyl groups show enhanced binding and favorable predicted pharmacological properties: Structure-based virtual screening of extended lopinavir analogs against multi-drug resistant HIV-1 protease. (Research article)

Journal of Molecular Graphics and Modelling

February 2014, 47: 18-24

DOI: 10.1016/j.jmgm.2013.10.010

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Conserved hydrogen bonds and water molecules in MDR HIV-1 protease substrate complexes. (Research article)

Biochemical and Biophysical Research Communications

 

January 2013, 430(3): 1022-1027

 

DOI: 10.1016/j.bbrc.2012.12.045

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Crystallographic study of multi-drug resistant HIV-1 protease lopinavir complex: Mechanism of drug recognition and resistance. (Research article)

Biochemical and Biophysical Research Communications

July 2013, 437(2): 199-204

Related X-ray crystal structure: PDB ID: 4L1A

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Design, synthesis and evaluation of a potent substrate analog inhibitor identified by scanning Ala/Phe mutagenesis, mimicking substrate co-evolution, against multidrug-resistant HIV-1 protease. (Research article)

Biochemical and Biophysical Research Communications

September 2013, 438(4): 703-708

DOI: 10.1016/j.bbrc.2013.07.117

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P2′ Benzene Carboxylic Acid Moiety Is Associated with Decrease in Cellular Uptake: Evaluation of Novel Nonpeptidic HIV-1 Protease Inhibitors Containing P2 bis-Tetrahydrofuran Moiety. (Research article)

Antimicrobial Agents and Chemotherapy

Sep 2013, 57 (10) 4920-4927; DOI: 10.1128/AAC.00868-13

X-ray structures: PDB IDs: 4HLA, 4I8W and 4I8Z

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Crystal structure of the extracellular domain of human myelin protein zero. (Structure Note)

Proteins (Structure, Function and Bioinformatics)

January 2012, 80(1): 307-313; DOI: 10.1002/prot.23164

Related X-ray crystal structure: PDB ID: 3OAI

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Crystal structures of multidrug-resistant HIV-1 protease in complex with two potent anti-malarial compounds. (Research article)

Biochemical and Biophysical Research Communications

May 2012, 421(3): 413-417

DOI: 10.1016/j.bbrc.2012.03.096

X-ray crystal structures: PDB IDs: 3R0W and 3R0Y

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Contribution of the 80s loop of HIV-1 protease to the multidrug-resistance mechanism: crystallographic study of MDR769 HIV-1 protease variants. (Research article)

Acta Crystallographica Section D Structural Biology

June 2011, 67(6): 524-532; DOI: 10.1107/S0907444911011541

X-ray structures: PDB IDs: 3PJ6, 3OQ7, 3OQA and 3OQD

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Novel HIV-1 Protease Inhibitors (PIs) Containing a Bicyclic P2 Functional Moiety, Tetrahydropyrano-Tetrahydrofuran, That Are Potent against Multi-PI-Resistant HIV-1 Variants. (Research article)

Antimicrobial Agents and Chemotherapy

Mar 2011, 55 (4) 1717-1727 

DOI: 10.1128/AAC.01540-10

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