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A Pyrazolo[3,4-d]pyrimidine Compound Reduces Cell Viability and Induces Apoptosis in Different Hematological Malignancies
Molecular targeted therapies are based upon drugs acting on tumors by interfering with specific targets involved in growth and spread of cancer. Many targeted therapies were approved by Food and Drug Administration as standard treatment, others were introduced into preclinical or clinical studies on...
Autores principales: | , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Frontiers Media S.A.
2016
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5098387/ https://www.ncbi.nlm.nih.gov/pubmed/27872592 http://dx.doi.org/10.3389/fphar.2016.00416 |
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author | Laurenzana, Ilaria Caivano, Antonella La Rocca, Francesco Trino, Stefania De Luca, Luciana D’Alessio, Francesca Schenone, Silvia Falco, Geppino Botta, Maurizio Del Vecchio, Luigi Musto, Pellegrino |
author_facet | Laurenzana, Ilaria Caivano, Antonella La Rocca, Francesco Trino, Stefania De Luca, Luciana D’Alessio, Francesca Schenone, Silvia Falco, Geppino Botta, Maurizio Del Vecchio, Luigi Musto, Pellegrino |
author_sort | Laurenzana, Ilaria |
collection | PubMed |
description | Molecular targeted therapies are based upon drugs acting on tumors by interfering with specific targets involved in growth and spread of cancer. Many targeted therapies were approved by Food and Drug Administration as standard treatment, others were introduced into preclinical or clinical studies on hematological malignancies (HMs). The development of drug-resistance in some HMs and the lack of effective treatments in other ones emphasized the need for searching new molecular targets and therapeutic agents. The aim of this study was to evaluate the effects of 4c pyrazolo[3,4-d]pyrimidine compound, a Src inhibitor, on lymphoid and myeloid neoplasms. Here, we demonstrated its ability to reduce cell viability, induce apoptosis and cell cycle arrest in lymphoid cell lines such as Jurkat, SKMM1, Derl-2/7, and myeloid cell lines, such as Jurl-MK1. Moreover, we reported a high expression of a Src kinase, Fyn, in these cell lines compared to healthy subjects. This study was a starting point to investigate 4c pyrazolo[3,4-d]pyrimidine compound as a drug for HMs and Src kinases as its potential molecular targets. |
format | Online Article Text |
id | pubmed-5098387 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2016 |
publisher | Frontiers Media S.A. |
record_format | MEDLINE/PubMed |
spelling | pubmed-50983872016-11-21 A Pyrazolo[3,4-d]pyrimidine Compound Reduces Cell Viability and Induces Apoptosis in Different Hematological Malignancies Laurenzana, Ilaria Caivano, Antonella La Rocca, Francesco Trino, Stefania De Luca, Luciana D’Alessio, Francesca Schenone, Silvia Falco, Geppino Botta, Maurizio Del Vecchio, Luigi Musto, Pellegrino Front Pharmacol Pharmacology Molecular targeted therapies are based upon drugs acting on tumors by interfering with specific targets involved in growth and spread of cancer. Many targeted therapies were approved by Food and Drug Administration as standard treatment, others were introduced into preclinical or clinical studies on hematological malignancies (HMs). The development of drug-resistance in some HMs and the lack of effective treatments in other ones emphasized the need for searching new molecular targets and therapeutic agents. The aim of this study was to evaluate the effects of 4c pyrazolo[3,4-d]pyrimidine compound, a Src inhibitor, on lymphoid and myeloid neoplasms. Here, we demonstrated its ability to reduce cell viability, induce apoptosis and cell cycle arrest in lymphoid cell lines such as Jurkat, SKMM1, Derl-2/7, and myeloid cell lines, such as Jurl-MK1. Moreover, we reported a high expression of a Src kinase, Fyn, in these cell lines compared to healthy subjects. This study was a starting point to investigate 4c pyrazolo[3,4-d]pyrimidine compound as a drug for HMs and Src kinases as its potential molecular targets. Frontiers Media S.A. 2016-11-07 /pmc/articles/PMC5098387/ /pubmed/27872592 http://dx.doi.org/10.3389/fphar.2016.00416 Text en Copyright © 2016 Laurenzana, Caivano, La Rocca, Trino, De Luca, D’Alessio, Schenone, Falco, Botta, Del Vecchio and Musto. http://creativecommons.org/licenses/by/4.0/ This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) or licensor are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms. |
spellingShingle | Pharmacology Laurenzana, Ilaria Caivano, Antonella La Rocca, Francesco Trino, Stefania De Luca, Luciana D’Alessio, Francesca Schenone, Silvia Falco, Geppino Botta, Maurizio Del Vecchio, Luigi Musto, Pellegrino A Pyrazolo[3,4-d]pyrimidine Compound Reduces Cell Viability and Induces Apoptosis in Different Hematological Malignancies |
title | A Pyrazolo[3,4-d]pyrimidine Compound Reduces Cell Viability and Induces Apoptosis in Different Hematological Malignancies |
title_full | A Pyrazolo[3,4-d]pyrimidine Compound Reduces Cell Viability and Induces Apoptosis in Different Hematological Malignancies |
title_fullStr | A Pyrazolo[3,4-d]pyrimidine Compound Reduces Cell Viability and Induces Apoptosis in Different Hematological Malignancies |
title_full_unstemmed | A Pyrazolo[3,4-d]pyrimidine Compound Reduces Cell Viability and Induces Apoptosis in Different Hematological Malignancies |
title_short | A Pyrazolo[3,4-d]pyrimidine Compound Reduces Cell Viability and Induces Apoptosis in Different Hematological Malignancies |
title_sort | pyrazolo[3,4-d]pyrimidine compound reduces cell viability and induces apoptosis in different hematological malignancies |
topic | Pharmacology |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5098387/ https://www.ncbi.nlm.nih.gov/pubmed/27872592 http://dx.doi.org/10.3389/fphar.2016.00416 |
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