title: A Pyrazolo[3,4-d]pyrimidine Compound Reduces Cell Viability and Induces Apoptosis in Different Hematological Malignancies.
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.
authors.affiliation: Laboratory of Preclinical and Translational Research, IRCCS - Referral Cancer Center of Basilicata (CROB), Rionero in Vulture Potenza, Italy.
authors.forename: Ilaria
authors.initials: I
authors.lastname: Laurenzana
authors.affiliation: Laboratory of Preclinical and Translational Research, IRCCS - Referral Cancer Center of Basilicata (CROB), Rionero in Vulture Potenza, Italy.
authors.forename: Antonella
authors.initials: A
authors.lastname: Caivano
authors.affiliation: Laboratory of Preclinical and Translational Research, IRCCS - Referral Cancer Center of Basilicata (CROB), Rionero in Vulture Potenza, Italy.
authors.forename: Francesco
authors.initials: F
authors.lastname: La Rocca
authors.affiliation: Laboratory of Preclinical and Translational Research, IRCCS - Referral Cancer Center of Basilicata (CROB), Rionero in Vulture Potenza, Italy.
authors.forename: Stefania
authors.initials: S
authors.lastname: Trino
authors.affiliation: Laboratory of Preclinical and Translational Research, IRCCS - Referral Cancer Center of Basilicata (CROB), Rionero in Vulture Potenza, Italy.
authors.forename: Luciana
authors.initials: L
authors.lastname: De Luca
authors.affiliation: Biotecnologie Avanzate s.c.a.r.l., CEINGE Napoli, Italy.
authors.forename: Francesca
authors.initials: F
authors.lastname: D'Alessio
authors.affiliation: Department of Pharmacy, University of Genoa Genoa, Italy.
authors.forename: Silvia
authors.initials: S
authors.lastname: Schenone
authors.affiliation: Department of Biology, University of Naples Federico II Naples, Italy.
authors.forename: Geppino
authors.initials: G
authors.lastname: Falco
authors.affiliation: Department of Biotechnology, Chemistry and Pharmacy, University of Siena Siena, Italy.
authors.forename: Maurizio
authors.initials: M
authors.lastname: Botta
authors.affiliation: Biotecnologie Avanzate s.c.a.r.l., CEINGENapoli, Italy; Department of Molecular Medicine and Medical Biotechnologies, University of Naples Federico IINaples, Italy.
authors.forename: Luigi
authors.initials: L
authors.lastname: Del Vecchio
authors.affiliation: Scientific Direction, IRCCS - Referral Cancer Center of Basilicata (CROB), Rionero in Vulture Potenza, Italy.
authors.forename: Pellegrino
authors.initials: P
authors.lastname: Musto
keywords: 4-d]pyrimidine compound; Fyn tyrosine kinase; Src kinase inhibitor; hematological malignancies; pyrazolo[3; targeted therapies