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FAKULTY OF SCIENCE AND TECHNOLOGY DEPARTMENT OF CHEMISTRY Development of novel renin inhibitors and interaction of antimicrobial and cytotoxic peptides with plasma proteins A drug discovery study Annfrid Sivertsen A dissertation for the degree of Philosophiae Doctor April 2013

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Page 1: Development of novel renin inhibitors and interaction of

FAKULTY OF SCIENCE AND TECHNOLOGY DEPARTMENT OF CHEMISTRY

Development of novel renin inhibitors and interaction of antimicrobial and cytotoxic peptides with plasma proteins A drug discovery study

Annfrid Sivertsen

A dissertation for the degree of Philosophiae Doctor April 2013

Page 2: Development of novel renin inhibitors and interaction of
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FAKULTY OF SCIENCE AND TECHNOLOGY DEPARTMENT OF CHEMISTRY

Development of novel renin inhibitors and interaction of antimicrobial and cytotoxic peptides with plasma proteins A drug discovery study

Annfrid Sivertsen

A dissertation for the degree of Philosophiae Doctor April 2013

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N-terminaldomain

C-terminal domain

Connecting interdomain

Flap

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>

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μ

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°

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Domain I

Domain III

Domain II

Drug site I Drug site II

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N-terminal

C-terminal

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Figure 14. The figure shows the comparison of the phenotype F1*S and A of AGP, in a) for phenotype

F1*S and in b) for phenotype A respectively. Both the pattern of polar residues and shape of the

binding pocket are altered, with the binding site of phenotype A lacking sub-pocket III due to changes

in side chain conformations of sub-site III residues. The binding site is located in the middle of the

figures, with the binding site section viewed to the right for closer inspection. The electrostatic surface

potential is shown for both phenotypes. Reprint from Nishi et al. 2011 [149], with permission from the

American Society for Biochemistry and Molecular Biology.

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°

°

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μ μ

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μ

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μ

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μ μ

μ

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Paper I

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Paper II

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Paper III

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Paper IV

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ISBN xxx-xx-xxxx-xxx-x


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