A pyrazolo[3,4-d]pyrimidine compound reduces cell viability and induces apoptosis in different hematological malignancies

Ilaria Laurenzana, Antonella Caivano, Francesco La Rocca, Stefania Trino, Luciana De Luca, Francesca D'Alessio, Silvia Schenone, Geppino Falco, Maurizio Botta, Luigi Del Vecchio, Pellegrino Musto

Research output: Contribution to journalArticle

Abstract

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.

Original languageEnglish
Article number416
JournalFrontiers in Pharmacology
Volume7
DOIs
Publication statusPublished - Nov 7 2016

Fingerprint

pyrazolo(3,4-d)pyrimidine
Hematologic Neoplasms
Cell Survival
Apoptosis
src-Family Kinases
Cell Line
Molecular Targeted Therapy
Neoplasms
Myeloid Cells
United States Food and Drug Administration
Therapeutics
Cell Cycle Checkpoints
Drug Resistance
Pharmaceutical Preparations
Healthy Volunteers
Lymphocytes
Growth

Keywords

  • 4-d]pyrimidine compound
  • Fyn tyrosine kinase
  • Hematological malignancies
  • Pyrazolo[3
  • Src kinase inhibitor
  • Targeted therapies

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)

Cite this

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.

In: Frontiers in Pharmacology, Vol. 7, 416, 07.11.2016.

Research output: Contribution to journalArticle

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