Intrinsically Fluorescent Anti-Cancer Drugs
At present, about one-third of the total protein targets in the pharmaceutical research sector are kinase-based. While kinases have been attractive targets to combat many diseases, including cancer, selective kinase inhibition has been challenging, because of the high degree of structural homology i...
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| Format: | Article |
| Language: | English |
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MDPI AG
2022-07-01
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| Series: | Biology |
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| Online Access: | https://www.mdpi.com/2079-7737/11/8/1135 |
| _version_ | 1797439421418569728 |
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| author | Md. Lutful Kabir Feng Wang Andrew H. A. Clayton |
| author_facet | Md. Lutful Kabir Feng Wang Andrew H. A. Clayton |
| author_sort | Md. Lutful Kabir |
| collection | DOAJ |
| description | At present, about one-third of the total protein targets in the pharmaceutical research sector are kinase-based. While kinases have been attractive targets to combat many diseases, including cancer, selective kinase inhibition has been challenging, because of the high degree of structural homology in the active site where many kinase inhibitors bind. Despite efficacy as cancer drugs, kinase inhibitors can exhibit limited target specificity and rationalizing their target profiles in the context of precise molecular mechanisms or rearrangements is a major challenge for the field. Spectroscopic approaches such as infrared, Raman, NMR and fluorescence have the potential to provide significant insights into drug-target and drug-non-target interactions because of sensitivity to molecular environment. This review places a spotlight on the significance of fluorescence for extracting information related to structural properties, discovery of hidden conformers in solution and in target-bound state, binding properties (e.g., location of binding sites, hydrogen-bonding, hydrophobicity), kinetics as well as dynamics of kinase inhibitors. It is concluded that the information gleaned from an understanding of the intrinsic fluorescence from these classes of drugs may aid in the development of future drugs with improved side-effects and less disease resistance. |
| first_indexed | 2024-03-09T11:52:39Z |
| format | Article |
| id | doaj.art-96a713b9c4e94e3f917c8f69e9d8db3d |
| institution | Directory Open Access Journal |
| issn | 2079-7737 |
| language | English |
| last_indexed | 2024-03-09T11:52:39Z |
| publishDate | 2022-07-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Biology |
| spelling | doaj.art-96a713b9c4e94e3f917c8f69e9d8db3d2023-11-30T23:12:59ZengMDPI AGBiology2079-77372022-07-01118113510.3390/biology11081135Intrinsically Fluorescent Anti-Cancer DrugsMd. Lutful Kabir0Feng Wang1Andrew H. A. Clayton2Optical Sciences Centre, Department of Physics and Astronomy, School of Science, Computing and Engineering Technologies, Swinburne University of Technology, Melbourne, VIC 3122, AustraliaDepartment of Chemistry and Biotechnology, School of Science, Computing and Engineering Technologies, Swinburne University of Technology, Melbourne, VIC 3122, AustraliaOptical Sciences Centre, Department of Physics and Astronomy, School of Science, Computing and Engineering Technologies, Swinburne University of Technology, Melbourne, VIC 3122, AustraliaAt present, about one-third of the total protein targets in the pharmaceutical research sector are kinase-based. While kinases have been attractive targets to combat many diseases, including cancer, selective kinase inhibition has been challenging, because of the high degree of structural homology in the active site where many kinase inhibitors bind. Despite efficacy as cancer drugs, kinase inhibitors can exhibit limited target specificity and rationalizing their target profiles in the context of precise molecular mechanisms or rearrangements is a major challenge for the field. Spectroscopic approaches such as infrared, Raman, NMR and fluorescence have the potential to provide significant insights into drug-target and drug-non-target interactions because of sensitivity to molecular environment. This review places a spotlight on the significance of fluorescence for extracting information related to structural properties, discovery of hidden conformers in solution and in target-bound state, binding properties (e.g., location of binding sites, hydrogen-bonding, hydrophobicity), kinetics as well as dynamics of kinase inhibitors. It is concluded that the information gleaned from an understanding of the intrinsic fluorescence from these classes of drugs may aid in the development of future drugs with improved side-effects and less disease resistance.https://www.mdpi.com/2079-7737/11/8/1135canceranti-cancer drugstyrosine kinasetyrosine kinase inhibitorsfluorescence |
| spellingShingle | Md. Lutful Kabir Feng Wang Andrew H. A. Clayton Intrinsically Fluorescent Anti-Cancer Drugs Biology cancer anti-cancer drugs tyrosine kinase tyrosine kinase inhibitors fluorescence |
| title | Intrinsically Fluorescent Anti-Cancer Drugs |
| title_full | Intrinsically Fluorescent Anti-Cancer Drugs |
| title_fullStr | Intrinsically Fluorescent Anti-Cancer Drugs |
| title_full_unstemmed | Intrinsically Fluorescent Anti-Cancer Drugs |
| title_short | Intrinsically Fluorescent Anti-Cancer Drugs |
| title_sort | intrinsically fluorescent anti cancer drugs |
| topic | cancer anti-cancer drugs tyrosine kinase tyrosine kinase inhibitors fluorescence |
| url | https://www.mdpi.com/2079-7737/11/8/1135 |
| work_keys_str_mv | AT mdlutfulkabir intrinsicallyfluorescentanticancerdrugs AT fengwang intrinsicallyfluorescentanticancerdrugs AT andrewhaclayton intrinsicallyfluorescentanticancerdrugs |