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Syk inhibitors in clinical development for hematological malignancies
Spleen tyrosine kinase (Syk) is a cytosolic non-receptor protein tyrosine kinase (PTK) and is mainly expressed in hematopoietic cells. Syk was recognized as a critical element in the B-cell receptor signaling pathway. Syk is also a key component in signal transduction from other immune receptors lik...
Autores principales: | , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
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BioMed Central
2017
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5534090/ https://www.ncbi.nlm.nih.gov/pubmed/28754125 http://dx.doi.org/10.1186/s13045-017-0512-1 |
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author | Liu, Delong Mamorska-Dyga, Aleksandra |
author_facet | Liu, Delong Mamorska-Dyga, Aleksandra |
author_sort | Liu, Delong |
collection | PubMed |
description | Spleen tyrosine kinase (Syk) is a cytosolic non-receptor protein tyrosine kinase (PTK) and is mainly expressed in hematopoietic cells. Syk was recognized as a critical element in the B-cell receptor signaling pathway. Syk is also a key component in signal transduction from other immune receptors like Fc receptors and adhesion receptors. Several oral Syk inhibitors including fostamatinib (R788), entospletinib (GS-9973), cerdulatinib (PRT062070), and TAK-659 are being assessed in clinical trials. The second generation compound, entospletinib, showed promising results in clinical trials against B-cell malignancies, mainly chronic lymphoid leukemia. Syk inhibitors are being evaluated in combination regimens in multiple malignancies. |
format | Online Article Text |
id | pubmed-5534090 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2017 |
publisher | BioMed Central |
record_format | MEDLINE/PubMed |
spelling | pubmed-55340902017-08-03 Syk inhibitors in clinical development for hematological malignancies Liu, Delong Mamorska-Dyga, Aleksandra J Hematol Oncol Review Spleen tyrosine kinase (Syk) is a cytosolic non-receptor protein tyrosine kinase (PTK) and is mainly expressed in hematopoietic cells. Syk was recognized as a critical element in the B-cell receptor signaling pathway. Syk is also a key component in signal transduction from other immune receptors like Fc receptors and adhesion receptors. Several oral Syk inhibitors including fostamatinib (R788), entospletinib (GS-9973), cerdulatinib (PRT062070), and TAK-659 are being assessed in clinical trials. The second generation compound, entospletinib, showed promising results in clinical trials against B-cell malignancies, mainly chronic lymphoid leukemia. Syk inhibitors are being evaluated in combination regimens in multiple malignancies. BioMed Central 2017-07-28 /pmc/articles/PMC5534090/ /pubmed/28754125 http://dx.doi.org/10.1186/s13045-017-0512-1 Text en © The Author(s). 2017 Open AccessThis article is distributed under the terms of the Creative Commons Attribution 4.0 International License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The Creative Commons Public Domain Dedication waiver (http://creativecommons.org/publicdomain/zero/1.0/) applies to the data made available in this article, unless otherwise stated. |
spellingShingle | Review Liu, Delong Mamorska-Dyga, Aleksandra Syk inhibitors in clinical development for hematological malignancies |
title | Syk inhibitors in clinical development for hematological malignancies |
title_full | Syk inhibitors in clinical development for hematological malignancies |
title_fullStr | Syk inhibitors in clinical development for hematological malignancies |
title_full_unstemmed | Syk inhibitors in clinical development for hematological malignancies |
title_short | Syk inhibitors in clinical development for hematological malignancies |
title_sort | syk inhibitors in clinical development for hematological malignancies |
topic | Review |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5534090/ https://www.ncbi.nlm.nih.gov/pubmed/28754125 http://dx.doi.org/10.1186/s13045-017-0512-1 |
work_keys_str_mv | AT liudelong sykinhibitorsinclinicaldevelopmentforhematologicalmalignancies AT mamorskadygaaleksandra sykinhibitorsinclinicaldevelopmentforhematologicalmalignancies |