How flexible is tipranavir in complex with the HIV-1 protease active site? [3]

AIDS

Volumn 18, Issue 3, 2004, Pages 579-580

  Schake, Dieter ^a  

^a NONE   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

PROTEINASE INHIBITOR; TIPRANAVIR;

BINDING AFFINITY; BINDING SITE; CRYSTAL STRUCTURE; HUMAN IMMUNODEFICIENCY VIRUS 1; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; HYDROGEN BOND; LETTER; PRIORITY JOURNAL; STRUCTURE ANALYSIS; X RAY ANALYSIS;

HIV PROTEASE; HIV PROTEASE INHIBITORS; HIV-1; HUMANS; PYRIDINES; PYRONES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 1642418876     PISSN: 02699370     EISSN: None     Source Type: Journal    
DOI: 10.1097/00002030-200402200-00033     Document Type: Letter

References (7)

1. McCallister S, Neubacher D, Verbiest W, Mayers DL. Susceptibility profile of tipranavir at baseline and subsequent virologic response in a cohort of patients with multiple-PI failure. In: XIth International HIV Drug Resistance Workshop. Seville, Spain, 2002 [Abstract 127].
2. Larder BA, Hertogs K, Bloor S, van den Eynden C, DeCian W, Wang Y, et al. Tipranavir inhibits broadly protease inhibitor-resistant HIV-1 clinical samples. AIDS 2000; 14:1943-1948.
3. Turner SR, Strohbach JW, Tomassi RA, Aristoff PA, Johnson PD, Skulnick HI, et al. Tipranavir (PNU-140690): a potent, orally bioavailable nonpeptidic HIV protease inhibitor of the 5,6-dihydro-4-hydroxy-2-pyrone sulfonamide class. J Med Chem 1998; 41:3467-3476.
4. Hall D, McCallister S, Neubacher D, Kraft M, Mayers DL. Characterisation of treatment-emergent resistance mutations in two phase II studies of tipranavir (TPV). In: XIIth International HIV Drug Resistance Workshop. Cabo San Lucas, Mexico, 2003 [Abstract 13].
5. McCallister S, Kohlbrenner V, Sqiures K, et al. Characterisation of the impact of genotype, phenotype, and inhibitory quotient (IQ) on antiviral activity of tipranavir (TPV) in highly treatment-experianced (HTE) patients. In: XIIth International HIV Drug Resistance Workshop. Cabo San Lucas, Mexico, 2003 [Abstract 12].
6. Velazquez-Campoy A, Freire E. Incorporating target heterogenity in drug design. J Cell Biochem 2001; 37 (Suppl.):82-88.
7. Ohtaka H, Velazquez-Campoy A, Xie D, Freire E. Overcoming drug resistance in HIV-1 chemotherapy: the binding thermodynamics of amprenavir and TMC-126 to wild-type and drug-resistant mutants of the HIV-1 protease. Protein Sci 2002; 11:1908-1916.