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Biological Evaluation of Serine Protease Inhibitors and Inducers of Protein Degradation

dc.contributor.advisorGütschow, Michael
dc.contributor.authorMangold, Martin
dc.date.accessioned2020-10-02T10:06:27Z
dc.date.available2020-10-02T10:06:27Z
dc.date.issued02.10.2020
dc.identifier.urihttp://hdl.handle.net/20.500.11811/8639
dc.description.abstractSerine proteases represent the largest group of enzymes of the human degradome. As such, they are valuable targets for the development of new drugs, due to their involvement in several diseases. Over the course of this work, a library of 73 compounds was evaluated as inhibitors of selected serine proteases. This way, several inhibitors of the enzyme matriptase-2, an important regulator of iron homeostasis, and thrombin were discovered. Some of these were established further for the use as activity-based probes in additional experiments. In a different approach, a test system for the evaluation of protein degradation inducing molecules (PROTACs) was conceptualized and established. Targeted protein degradation represents a promising new therapeutic option for the treatment of previously undruggable diseases.en
dc.language.isoeng
dc.rightsIn Copyright
dc.rights.urihttp://rightsstatements.org/vocab/InC/1.0/
dc.subjectInhibitors
dc.subjectactivity-based drugs
dc.subjectmatriptase-2
dc.subjectinduced protein degradation
dc.subject.ddc500 Naturwissenschaften
dc.titleBiological Evaluation of Serine Protease Inhibitors and Inducers of Protein Degradation
dc.typeDissertation oder Habilitation
dc.publisher.nameUniversitäts- und Landesbibliothek Bonn
dc.publisher.locationBonn
dc.rights.accessRightsopenAccess
dc.identifier.urnhttps://nbn-resolving.org/urn:nbn:de:hbz:5-59752
ulbbn.pubtypeErstveröffentlichung
ulbbnediss.affiliation.nameRheinische Friedrich-Wilhelms-Universität Bonn
ulbbnediss.affiliation.locationBonn
ulbbnediss.thesis.levelDissertation
ulbbnediss.dissID5975
ulbbnediss.date.accepted2020-09-10
ulbbnediss.instituteMathematisch-Naturwissenschaftliche Fakultät : Fachgruppe Pharmazie / Pharmazeutisches Institut
ulbbnediss.fakultaetMathematisch-Naturwissenschaftliche Fakultät
dc.contributor.coRefereeSchiedel, Anke


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