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Träfflista för sökning "WFRF:(OBERG B) "

Search: WFRF:(OBERG B)

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  • Andersson, H.O., et al. (author)
  • Optimization of P1-P3 groups in symmetric and asymmetric HIV-1 protease inhibitors
  • 2003
  • In: European Journal of Biochemistry. - : Wiley. - 0014-2956 .- 1432-1033. ; 270:8, s. 1746-1758
  • Journal article (peer-reviewed)abstract
    • HIV-1 protease is an important target for treatment of AIDS, and efficient drugs have been developed. However, the resistance and negative side effects of the current drugs has necessitated the development of new compounds with different binding patterns. In this study, nine C-terminally duplicated HIV-1 protease inhibitors were cocrystallised with the enzyme, the crystal structures analysed at 1.8-2.3 Å resolution, and the inhibitory activity of the compounds characterized in order to evaluate the effects of the individual modifications. These compounds comprise two central hydroxy groups that mimic the geminal hydroxy groups of a cleavage-reaction intermediate. One of the hydroxy groups is located between the d-oxygen atoms of the two catalytic aspartic acid residues, and the other in the gauche position relative to the first. The asymmetric binding of the two central inhibitory hydroxyls induced a small deviation from exact C2 symmetry in the whole enzyme-inhibitor complex. The study shows that the protease molecule could accommodate its structure to different sizes of the P2/P2' groups. The structural alterations were, however, relatively conservative and limited. The binding capacity of the S3/S3' sites was exploited by elongation of the compounds with groups in the P3/P3' positions or by extension of the P1/P1' groups. Furthermore, water molecules were shown to be important binding links between the protease and the inhibitors. This study produced a number of inhibitors with Ki values in the 100 picomolar range.
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  • Nordenfelt, E, et al. (author)
  • No in vivo effect of trisodium phosphonoformate on woodchuck hepatitis virus production
  • 1982
  • In: Acta pathologica, microbiologica, et immunologica Scandinavica. Section B, Microbiology. - 0108-0180. ; 90:6, s. 449-451
  • Journal article (peer-reviewed)abstract
    • The efficient in vitro inhibition of hepatitis B virus DNA polymerase by trisodium phosphonoformate (PFA, INN: foscarnet sodium) and its low toxicity suggested that PFA could be used as a therapeutic agent for hepatitis B infection. PFA was also found to inhibit woodchuck hepatitis virus (WHV) DNA polymerase in vitro. As a model to test PFA's eventual effect, chronically WHV infected woodchucks were treated with PFA. The animals were treated twice daily in a dosage which gave a minimum serum level of PFA corresponding to an in vitro inhibiting effect on WHV DNA polymerase of about 40%. The concentration in liver tissue was found to be 15% below serum level. The amount of WHV particles in serum was followed by DNA polymerase assay. No effect on WHV production could be seen during 2 weeks' treatment. No change of the in vitro sensitivity to PFA of the WHV DNA polymerase was seen. These results indicate that the WHV associated DNA polymerase has no role in the production of viral particles.
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  • Result 1-10 of 118
Type of publication
journal article (92)
conference paper (22)
research review (2)
book chapter (2)
Type of content
peer-reviewed (82)
other academic/artistic (35)
pop. science, debate, etc. (1)
Author/Editor
Oberg, K (38)
OBERG, B (32)
Eriksson, B (26)
Zhang, H. (11)
VRANG, L (11)
JOHANSSON, NG (9)
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UNGE, T (9)
Larsson, H (6)
Rickert, M (6)
Tiensuu Janson, E (6)
Gahrton, G (6)
Oberg, AS (6)
Bjorkholm, M (6)
LIND, P (6)
NOREEN, R (6)
SAHLBERG, C (6)
Lichtenstein, P. (6)
Almqvist, C (5)
Larsson, T (5)
Larsson, C (5)
HOGBERG, M (5)
Weber, G. (4)
Stridsberg, M (4)
Wang, S (4)
Schiöth, Helgi B. (4)
Arver, Stefan (4)
Jokinen, Jussi (4)
Ljungman, P (4)
Oberg, Kjell (4)
Chatzittofis, Andrea ... (4)
Paul, C (4)
Turesson, I (3)
Tidefelt, U (3)
Lonnqvist, B (3)
AHGREN, C (3)
CANTRELL, AS (3)
JASKUNAS, SR (3)
JORDAN, CL (3)
KINNICK, MD (3)
MORIN, JM (3)
MUESING, MA (3)
Bjurling, P (3)
Ahlstrom, H (3)
Langstrom, B (3)
Harmenberg, J (3)
UTTER, G (3)
Samuelsson, B (3)
LILIEMARK, J (3)
GRUBER, A (3)
Åkerström, Göran (3)
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Karolinska Institutet (62)
Uppsala University (50)
Umeå University (6)
Lund University (6)
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Swedish (1)
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Medical and Health Sciences (14)
Natural sciences (4)
Engineering and Technology (3)
Social Sciences (1)

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