The Development of BTK Inhibitors: A Five-Year Update
Bruton’s tyrosine kinase (BTK) represented, in the past ten years, an important target for the development of new therapeutic agents that could be useful for cancer and autoimmune disorders. To date, five compounds, able to block BTK in an irreversible manner, have been launched in the market, where...
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| Format: | Article |
| Language: | English |
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MDPI AG
2021-12-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/26/23/7411 |
| _version_ | 1797507386679754752 |
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| author | Bruno Tasso Andrea Spallarossa Eleonora Russo Chiara Brullo |
| author_facet | Bruno Tasso Andrea Spallarossa Eleonora Russo Chiara Brullo |
| author_sort | Bruno Tasso |
| collection | DOAJ |
| description | Bruton’s tyrosine kinase (BTK) represented, in the past ten years, an important target for the development of new therapeutic agents that could be useful for cancer and autoimmune disorders. To date, five compounds, able to block BTK in an irreversible manner, have been launched in the market, whereas many reversible BTK inhibitors (BTKIs), with reduced side effects that are more useful for long-term administration in autoimmune disorders, are under clinical investigation. Despite the presence in the literature of many articles and reviews, studies on BTK function and BTKIs are of great interest for pharmaceutical companies as well as academia. This review is focused on compounds that have appeared in the literature from 2017 that are able to block BTK in an irreversible or reversible manner; also, new promising tunable irreversible inhibitors, as well as PROTAC molecules, have been reported. This summary could improve the knowledge of the chemical diversity of BTKIs and provide information for future studies, particularly from the medicinal chemistry point of view. Data reported here are collected from different databases (Scifinder, Web of Science, Scopus, Google Scholar, and Pubmed) using “BTK” and “BTK inhibitors” as keywords. |
| first_indexed | 2024-03-10T04:47:45Z |
| format | Article |
| id | doaj.art-cca83abbb6004b0a831aeb3cc80dbcca |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-10T04:47:45Z |
| publishDate | 2021-12-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-cca83abbb6004b0a831aeb3cc80dbcca2023-11-23T02:52:09ZengMDPI AGMolecules1420-30492021-12-012623741110.3390/molecules26237411The Development of BTK Inhibitors: A Five-Year UpdateBruno Tasso0Andrea Spallarossa1Eleonora Russo2Chiara Brullo3Department of Pharmacy, University of Genova, Viale Benedetto XV 3, 16132 Genova, ItalyDepartment of Pharmacy, University of Genova, Viale Benedetto XV 3, 16132 Genova, ItalyDepartment of Pharmacy, University of Genova, Viale Benedetto XV 3, 16132 Genova, ItalyDepartment of Pharmacy, University of Genova, Viale Benedetto XV 3, 16132 Genova, ItalyBruton’s tyrosine kinase (BTK) represented, in the past ten years, an important target for the development of new therapeutic agents that could be useful for cancer and autoimmune disorders. To date, five compounds, able to block BTK in an irreversible manner, have been launched in the market, whereas many reversible BTK inhibitors (BTKIs), with reduced side effects that are more useful for long-term administration in autoimmune disorders, are under clinical investigation. Despite the presence in the literature of many articles and reviews, studies on BTK function and BTKIs are of great interest for pharmaceutical companies as well as academia. This review is focused on compounds that have appeared in the literature from 2017 that are able to block BTK in an irreversible or reversible manner; also, new promising tunable irreversible inhibitors, as well as PROTAC molecules, have been reported. This summary could improve the knowledge of the chemical diversity of BTKIs and provide information for future studies, particularly from the medicinal chemistry point of view. Data reported here are collected from different databases (Scifinder, Web of Science, Scopus, Google Scholar, and Pubmed) using “BTK” and “BTK inhibitors” as keywords.https://www.mdpi.com/1420-3049/26/23/7411Bruton’s kinase(ir)reversible inhibitorsB-cell malignanciesautoimmune diseasesmedicinal chemistrysmall molecules |
| spellingShingle | Bruno Tasso Andrea Spallarossa Eleonora Russo Chiara Brullo The Development of BTK Inhibitors: A Five-Year Update Molecules Bruton’s kinase (ir)reversible inhibitors B-cell malignancies autoimmune diseases medicinal chemistry small molecules |
| title | The Development of BTK Inhibitors: A Five-Year Update |
| title_full | The Development of BTK Inhibitors: A Five-Year Update |
| title_fullStr | The Development of BTK Inhibitors: A Five-Year Update |
| title_full_unstemmed | The Development of BTK Inhibitors: A Five-Year Update |
| title_short | The Development of BTK Inhibitors: A Five-Year Update |
| title_sort | development of btk inhibitors a five year update |
| topic | Bruton’s kinase (ir)reversible inhibitors B-cell malignancies autoimmune diseases medicinal chemistry small molecules |
| url | https://www.mdpi.com/1420-3049/26/23/7411 |
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