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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...

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Detalles Bibliográficos
Autores principales: Tasso, Bruno, Spallarossa, Andrea, Russo, Eleonora, Brullo, Chiara
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
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.
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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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