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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...

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Autores principales: 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
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Frontiers Media S.A. 2016
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.
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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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