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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...
Autores principales: | , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2021
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8659154/ https://www.ncbi.nlm.nih.gov/pubmed/34885993 http://dx.doi.org/10.3390/molecules26237411 |
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author | Tasso, Bruno Spallarossa, Andrea Russo, Eleonora Brullo, Chiara |
author_facet | Tasso, Bruno Spallarossa, Andrea Russo, Eleonora Brullo, Chiara |
author_sort | Tasso, Bruno |
collection | PubMed |
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. |
format | Online Article Text |
id | pubmed-8659154 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-86591542021-12-10 The Development of BTK Inhibitors: A Five-Year Update Tasso, Bruno Spallarossa, Andrea Russo, Eleonora Brullo, Chiara Molecules Review 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. MDPI 2021-12-06 /pmc/articles/PMC8659154/ /pubmed/34885993 http://dx.doi.org/10.3390/molecules26237411 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Review Tasso, Bruno Spallarossa, Andrea Russo, Eleonora Brullo, Chiara The Development of BTK Inhibitors: A Five-Year Update |
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 | Review |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8659154/ https://www.ncbi.nlm.nih.gov/pubmed/34885993 http://dx.doi.org/10.3390/molecules26237411 |
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