Biological Evaluation of Serine Protease Inhibitors and Inducers of Protein Degradation
Biological Evaluation of Serine Protease Inhibitors and Inducers of Protein Degradation
View/Type of Scholarly Publication
DissertationDate of Exam
10.09.2020Date of Publication
02.10.2020Advisor
Gütschow, MichaelCo-Referee
Schiedel, AnkeMetadata
Show full item record
Citable Links 
Abstract
Serine 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.
Subjects
Inhibitors, activity-based drugs, matriptase-2, induced protein degradation
Classification (DDC)
500 NaturwissenschaftenMangold, Martin: Biological Evaluation of Serine Protease Inhibitors and Inducers of Protein Degradation. - Bonn, 2020. - Dissertation, Rheinische Friedrich-Wilhelms-Universität Bonn.
Online-Ausgabe in bonndoc: https://nbn-resolving.org/urn:nbn:de:hbz:5-59752
Online-Ausgabe in bonndoc: https://nbn-resolving.org/urn:nbn:de:hbz:5-59752
@phdthesis{handle:20.500.11811/8639,
urn: https://nbn-resolving.org/urn:nbn:de:hbz:5-59752,
author = {{Martin Mangold}},
title = {Biological Evaluation of Serine Protease Inhibitors and Inducers of Protein Degradation},
school = {Rheinische Friedrich-Wilhelms-Universität Bonn},
year = 2020,
month = oct,
note = {Serine 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.},
url = {https://hdl.handle.net/20.500.11811/8639}
}
urn: https://nbn-resolving.org/urn:nbn:de:hbz:5-59752,
author = {{Martin Mangold}},
title = {Biological Evaluation of Serine Protease Inhibitors and Inducers of Protein Degradation},
school = {Rheinische Friedrich-Wilhelms-Universität Bonn},
year = 2020,
month = oct,
note = {Serine 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.},
url = {https://hdl.handle.net/20.500.11811/8639}
}
The following license files are associated with this item:
