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Bruton’s Tyrosine Kinase Inhibitors (BTKIs): Review of Preclinical Studies and Evaluation of Clinical Trials

In the last few decades, there has been a growing interest in Bruton’s tyrosine kinase (BTK) and the compounds that target it. BTK is a downstream mediator of the B-cell receptor (BCR) signaling pathway and affects B-cell proliferation and differentiation. Evidence demonstrating the expression of BT...

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Autores principales: Rozkiewicz, Dariusz, Hermanowicz, Justyna Magdalena, Kwiatkowska, Iwona, Krupa, Anna, Pawlak, Dariusz
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10005125/
https://www.ncbi.nlm.nih.gov/pubmed/36903645
http://dx.doi.org/10.3390/molecules28052400
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author Rozkiewicz, Dariusz
Hermanowicz, Justyna Magdalena
Kwiatkowska, Iwona
Krupa, Anna
Pawlak, Dariusz
author_facet Rozkiewicz, Dariusz
Hermanowicz, Justyna Magdalena
Kwiatkowska, Iwona
Krupa, Anna
Pawlak, Dariusz
author_sort Rozkiewicz, Dariusz
collection PubMed
description In the last few decades, there has been a growing interest in Bruton’s tyrosine kinase (BTK) and the compounds that target it. BTK is a downstream mediator of the B-cell receptor (BCR) signaling pathway and affects B-cell proliferation and differentiation. Evidence demonstrating the expression of BTK on the majority of hematological cells has led to the hypothesis that BTK inhibitors (BTKIs) such as ibrutinib can be an effective treatment for leukemias and lymphomas. However, a growing body of experimental and clinical data has demonstrated the significance of BTK, not just in B-cell malignancies, but also in solid tumors, such as breast, ovarian, colorectal, and prostate cancers. In addition, enhanced BTK activity is correlated with autoimmune disease. This gave rise to the hypothesis that BTK inhibitors can be beneficial in the therapy of rheumatoid arthritis (RA), systemic lupus erythematosus (SLE), multiple sclerosis (MS), Sjögren’s syndrome (SS), allergies, and asthma. In this review article, we summarize the most recent findings regarding this kinase as well as the most advanced BTK inhibitors that have been developed to date and their clinical applications mainly in cancer and chronic inflammatory disease patients.
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spelling pubmed-100051252023-03-11 Bruton’s Tyrosine Kinase Inhibitors (BTKIs): Review of Preclinical Studies and Evaluation of Clinical Trials Rozkiewicz, Dariusz Hermanowicz, Justyna Magdalena Kwiatkowska, Iwona Krupa, Anna Pawlak, Dariusz Molecules Review In the last few decades, there has been a growing interest in Bruton’s tyrosine kinase (BTK) and the compounds that target it. BTK is a downstream mediator of the B-cell receptor (BCR) signaling pathway and affects B-cell proliferation and differentiation. Evidence demonstrating the expression of BTK on the majority of hematological cells has led to the hypothesis that BTK inhibitors (BTKIs) such as ibrutinib can be an effective treatment for leukemias and lymphomas. However, a growing body of experimental and clinical data has demonstrated the significance of BTK, not just in B-cell malignancies, but also in solid tumors, such as breast, ovarian, colorectal, and prostate cancers. In addition, enhanced BTK activity is correlated with autoimmune disease. This gave rise to the hypothesis that BTK inhibitors can be beneficial in the therapy of rheumatoid arthritis (RA), systemic lupus erythematosus (SLE), multiple sclerosis (MS), Sjögren’s syndrome (SS), allergies, and asthma. In this review article, we summarize the most recent findings regarding this kinase as well as the most advanced BTK inhibitors that have been developed to date and their clinical applications mainly in cancer and chronic inflammatory disease patients. MDPI 2023-03-06 /pmc/articles/PMC10005125/ /pubmed/36903645 http://dx.doi.org/10.3390/molecules28052400 Text en © 2023 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
Rozkiewicz, Dariusz
Hermanowicz, Justyna Magdalena
Kwiatkowska, Iwona
Krupa, Anna
Pawlak, Dariusz
Bruton’s Tyrosine Kinase Inhibitors (BTKIs): Review of Preclinical Studies and Evaluation of Clinical Trials
title Bruton’s Tyrosine Kinase Inhibitors (BTKIs): Review of Preclinical Studies and Evaluation of Clinical Trials
title_full Bruton’s Tyrosine Kinase Inhibitors (BTKIs): Review of Preclinical Studies and Evaluation of Clinical Trials
title_fullStr Bruton’s Tyrosine Kinase Inhibitors (BTKIs): Review of Preclinical Studies and Evaluation of Clinical Trials
title_full_unstemmed Bruton’s Tyrosine Kinase Inhibitors (BTKIs): Review of Preclinical Studies and Evaluation of Clinical Trials
title_short Bruton’s Tyrosine Kinase Inhibitors (BTKIs): Review of Preclinical Studies and Evaluation of Clinical Trials
title_sort bruton’s tyrosine kinase inhibitors (btkis): review of preclinical studies and evaluation of clinical trials
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10005125/
https://www.ncbi.nlm.nih.gov/pubmed/36903645
http://dx.doi.org/10.3390/molecules28052400
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