Correlation between Membrane Permeability and the Intracellular Degradation Activity of Proteolysis-Targeting Chimeras
Proteolysis-targeting chimeras (PROTACs) have attracted attention as an innovative drug modality that induces the selective degradation of target proteins. This technology shows higher activity than conventional inhibitors and holds great potential in the field of drug discovery. Optimization of the...
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| Published in | Chemical & pharmaceutical bulletin Vol. 72; no. 11; pp. 961 - 965 |
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| Main Authors | , , , |
| Format | Journal Article |
| Language | English |
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Japan
The Pharmaceutical Society of Japan
14.11.2024
Japan Science and Technology Agency |
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| Online Access | Get full text |
| ISSN | 0009-2363 1347-5223 1347-5223 |
| DOI | 10.1248/cpb.c24-00615 |
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| Abstract | Proteolysis-targeting chimeras (PROTACs) have attracted attention as an innovative drug modality that induces the selective degradation of target proteins. This technology shows higher activity than conventional inhibitors and holds great potential in the field of drug discovery. Optimization of the linker is essential for PROTACs to achieve sufficient activity, particularly with regard to cell membrane permeability. However, the correlation between membrane permeability and the activity of PROTACs has not been fully explored. To address this, we established a new molecular design approach to remove the linker and optimize PROTAC structure. These PROTAC compound groups were used to analyze the correlation between membrane permeability and activity using LC-tandem mass spectrometry (LC-MS/MS). Results revealed that the degradation activity of PROTACs fluctuates with increasing membrane permeability and changes in response to linker optimization, while sufficient proteolytic activity can be retained. These findings demonstrate the importance of considering the balance between membrane permeability and activity in PROTAC design and provide a new strategy for developing more effective PROTACs. |
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| AbstractList | Proteolysis-targeting chimeras (PROTACs) have attracted attention as an innovative drug modality that induces the selective degradation of target proteins. This technology shows higher activity than conventional inhibitors and holds great potential in the field of drug discovery. Optimization of the linker is essential for PROTACs to achieve sufficient activity, particularly with regard to cell membrane permeability. However, the correlation between membrane permeability and the activity of PROTACs has not been fully explored. To address this, we established a new molecular design approach to remove the linker and optimize PROTAC structure. These PROTAC compound groups were used to analyze the correlation between membrane permeability and activity using LC-tandem mass spectrometry (LC-MS/MS). Results revealed that the degradation activity of PROTACs fluctuates with increasing membrane permeability and changes in response to linker optimization, while sufficient proteolytic activity can be retained. These findings demonstrate the importance of considering the balance between membrane permeability and activity in PROTAC design and provide a new strategy for developing more effective PROTACs. Proteolysis-targeting chimeras (PROTACs) have attracted attention as an innovative drug modality that induces the selective degradation of target proteins. This technology shows higher activity than conventional inhibitors and holds great potential in the field of drug discovery. Optimization of the linker is essential for PROTACs to achieve sufficient activity, particularly with regard to cell membrane permeability. However, the correlation between membrane permeability and the activity of PROTACs has not been fully explored. To address this, we established a new molecular design approach to remove the linker and optimize PROTAC structure. These PROTAC compound groups were used to analyze the correlation between membrane permeability and activity using LC-tandem mass spectrometry (LC-MS/MS). Results revealed that the degradation activity of PROTACs fluctuates with increasing membrane permeability and changes in response to linker optimization, while sufficient proteolytic activity can be retained. These findings demonstrate the importance of considering the balance between membrane permeability and activity in PROTAC design and provide a new strategy for developing more effective PROTACs.Proteolysis-targeting chimeras (PROTACs) have attracted attention as an innovative drug modality that induces the selective degradation of target proteins. This technology shows higher activity than conventional inhibitors and holds great potential in the field of drug discovery. Optimization of the linker is essential for PROTACs to achieve sufficient activity, particularly with regard to cell membrane permeability. However, the correlation between membrane permeability and the activity of PROTACs has not been fully explored. To address this, we established a new molecular design approach to remove the linker and optimize PROTAC structure. These PROTAC compound groups were used to analyze the correlation between membrane permeability and activity using LC-tandem mass spectrometry (LC-MS/MS). Results revealed that the degradation activity of PROTACs fluctuates with increasing membrane permeability and changes in response to linker optimization, while sufficient proteolytic activity can be retained. These findings demonstrate the importance of considering the balance between membrane permeability and activity in PROTAC design and provide a new strategy for developing more effective PROTACs. |
| ArticleNumber | c24-00615 |
| Author | Yokoo, Hidetomo Demizu, Yosuke Osawa, Hinata Saito, Kosuke |
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| Cites_doi | 10.1039/C0MB00074D 10.1021/acs.jmedchem.1c01496 10.1073/pnas.141230798 10.1021/acschembio.9b00972 10.1126/science.287.5460.2013 10.1016/S0021-9258(18)61429-2 10.3390/cells8060619 10.1016/j.bmcl.2008.07.114 10.3390/bioengineering9120766 10.1021/acs.jmedchem.6b01781 10.1021/acs.jmedchem.1c01206 10.1039/D2MD00284A 10.1186/s12943-022-01707-5 10.1021/acs.jmedchem.8b01631 10.2353/ajpath.2009.080709 10.1021/acsmedchemlett.0c00605 10.1016/j.ejmech.2022.114821 10.1021/acs.jmedchem.2c00877 10.1016/0005-2760(79)90198-X 10.1016/j.bmc.2023.117259 10.1039/D2CS00220E 10.1016/S0167-4838(00)00161-8 10.3390/molecules27061977 10.1016/j.ab.2008.08.012 10.1021/jacs.2c05499 |
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| Copyright | 2024 Author(s) Published by The Pharmaceutical Society of Japan 2024. This work is published under https://creativecommons.org/licenses/by-nc/4.0/ (the “License”). Notwithstanding the ProQuest Terms and Conditions, you may use this content in accordance with the terms of the License. |
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| Keywords | degradation activity LC-tandem mass spectrometry (LC-MS/MS) linker optimization membrane permeability proteolysis-targeting chimera |
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| SubjectTerms | Cell Membrane Permeability - drug effects Cell membranes Chimeras Chromatography, Liquid Correlation Degradation degradation activity Design optimization Humans LC-tandem mass spectrometry (LC-MS/MS) linker optimization Mass spectrometry Mass spectroscopy Membrane permeability Molecular Structure Permeability Proteolysis Proteolysis - drug effects proteolysis-targeting chimera Tandem Mass Spectrometry |
| Title | Correlation between Membrane Permeability and the Intracellular Degradation Activity of Proteolysis-Targeting Chimeras |
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