Literature DB >> 10987413

Targeting the dimerization interface for irreversible inhibition of HIV-1 protease.

R Zutshi1, J Chmielewski.   

Abstract

A novel strategy was used to irreversibly inhibit HIV-1 protease. The inhibitor was designed to form a disulfide bond with Cys95, present at the dimerization interface of HIV-1 protease. The inhibitor was shown to be active against HIV-1 protease with K(inact) = 3.7 microM and V(inact) = 0.012 min(-1).

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Year:  2000        PMID: 10987413     DOI: 10.1016/s0960-894x(00)00369-3

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  9 in total

1.  Thermodynamics of strongly allosteric inhibition: a model study of HIV-1 protease.

Authors:  S Kimura; R A Broglia; G Tiana
Journal:  Eur Biophys J       Date:  2012-10-05       Impact factor: 1.733

2.  Rapid structural fluctuations of the free HIV protease flaps in solution: relationship to crystal structures and comparison with predictions of dynamics calculations.

Authors:  Darón I Freedberg; Rieko Ishima; Jaison Jacob; Yun-Xing Wang; Irina Kustanovich; John M Louis; Dennis A Torchia
Journal:  Protein Sci       Date:  2002-02       Impact factor: 6.725

3.  HIV-1 protease function and structure studies with the simplicial neighborhood analysis of protein packing method.

Authors:  Shuxing Zhang; Andrew H Kaplan; Alexander Tropsha
Journal:  Proteins       Date:  2008-11-15

4.  Current and Novel Inhibitors of HIV Protease.

Authors:  Jana Pokorná; Ladislav Machala; Pavlína Rezáčová; Jan Konvalinka
Journal:  Viruses       Date:  2009-12-11       Impact factor: 5.048

5.  Targeting human immunodeficiency virus type 1 assembly, maturation and budding.

Authors:  Johanna Wapling; Seema Srivastava; Miranda Shehu-Xhilaga; Gilda Tachedjian
Journal:  Drug Target Insights       Date:  2007-07-20

6.  Computer applications for prediction of protein-protein interactions and rational drug design.

Authors:  Solène Grosdidier; Max Totrov; Juan Fernández-Recio
Journal:  Adv Appl Bioinform Chem       Date:  2009-11-10

7.  The N-terminal octapeptide acts as a dimerization inhibitor of SARS coronavirus 3C-like proteinase.

Authors:  Ping Wei; Keqiang Fan; Hao Chen; Liang Ma; Changkang Huang; Lei Tan; Dong Xi; Chunmei Li; Ying Liu; Aoneng Cao; Luhua Lai
Journal:  Biochem Biophys Res Commun       Date:  2005-11-28       Impact factor: 3.575

Review 8.  An Overview of Severe Acute Respiratory Syndrome-Coronavirus (SARS-CoV) 3CL Protease Inhibitors: Peptidomimetics and Small Molecule Chemotherapy.

Authors:  Thanigaimalai Pillaiyar; Manoj Manickam; Vigneshwaran Namasivayam; Yoshio Hayashi; Sang-Hun Jung
Journal:  J Med Chem       Date:  2016-02-29       Impact factor: 7.446

Review 9.  Development of peptide inhibitors of HIV transmission.

Authors:  Siyu Shi; Peter K Nguyen; Henry J Cabral; Ramon Diez-Barroso; Paul J Derry; Satoko M Kanahara; Vivek A Kumar
Journal:  Bioact Mater       Date:  2016-09-16
  9 in total

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