Interaction Studies of Secreted Aspartic Proteases (Saps) from Candida albicans: Application for Drug Discovery

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Backman, Dan,1972-Uppsala universitet,Institutionen för naturvetenskaplig biokemi (författare)

Interaction Studies of Secreted Aspartic Proteases (Saps) from Candida albicans : Application for Drug Discovery

BokEngelska2005

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Uppsala :Acta Universitatis Upsaliensis,2005
53 s.
electronicrdacarrier

Nummerbeteckningar

LIBRIS-ID:oai:DiVA.org:uu-5815
ISBN:9155462634
https://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-5815URI

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Språk:engelska
Sammanfattning på:engelska

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Digital Comprehensive Summaries of Uppsala Dissertations from the Faculty of Science and Technology,1651-6214 ;58

Anmärkningar

This thesis is focused on enzymatic studies of the secreted aspartic proteases (Saps) from Candida albicans as a tool for discovery of anti-candida drugs. C. albicans causes infections in a number of different locations, which differ widely in the protein substrates available and pH. Since C. albicans needs Saps during virulent growth, these enzymes are good targets for drug development.In order to investigate the catalytic characteristics of Saps and their inhibitor affinities, substrate-based kinetic assays were developed. Due to the low sensitivity of these assays, especially at the sub-optimal pH required to mimic the different locations of infections, these assays were not satisfactory. Therefore, a biosensor assay was developed whereby, it was possible to study interaction between Saps and inhibitors without the need to optimise catalytic efficacy. Furthermore, the biosensor assay allowed determination of affinity, as well as the individual association and dissociation rates for inhibitor interactions.Knowledge about substrate specificity, Sap subsite adaptivity, and the pH dependencies of catalytic efficacy has been accumulated. Also, screening of transition-state analogue inhibitors designed for HIV-1 protease has revealed inhibitors with affinity for Saps. Furthermore, the kinetics and pH dependencies of their interaction with Saps have been investigated. One of these inhibitors, BEA-440, displayed a complex interaction with Saps, indicating a conformational change upon binding and a very slow dissociation rate. A time dependent interaction was further supported by inhibition measurements. The structural information obtained affords possibilities for design of new more potent inhibitors that might ultimately become drugs against candidiasis. The strategy to combine substrate specificity studies with inhibitor screening has led to complementary results that generate a framework for further development of potent inhibitors.

Ämnesord och genrebeteckningar

NATURVETENSKAP Biologi Biokemi och molekylärbiologi hsv//swe
NATURAL SCIENCES Biological Sciences Biochemistry and Molecular Biology hsv//eng
Biochemistry
SPR Biosensor
Secreted aspartic proteases
Candida albicans
interaction kinetics
drug discovery
protease inhibitor
Biokemi
Biochemistry
Biokemi

Biuppslag (personer, institutioner, konferenser, titlar ...)

Danielson, Helena (preses)
Tomkinson, Birgitta (preses)
Henriksson, Gunnar,DocentTräkemi, Fiber och polymerteknik, KTH, Stockholm (opponent)
Uppsala universitetInstitutionen för naturvetenskaplig biokemi (creator_code:org_t)

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Av författaren/redakt...: Backman, Dan, 19 ...; Danielson, Helen ...; Tomkinson, Birgi ...; Henriksson, Gunn ...

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NATURVETENSKAP: NATURVETENSKAP; och Biologi; och Biokemi och mole ...

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Av lärosätet: Uppsala universitet

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