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Activity of the Novel BCR Kinase Inhibitor IQS019 in B-NHL - Couverture souple

Roué, Gael; Esteve-Arenys, Anna

 
9783330090712: Activity of the Novel BCR Kinase Inhibitor IQS019 in B-NHL
Couverture souple
ISBN 10 : 3330090715 ISBN 13 : 9783330090712
Editeur : LAP LAMBERT Academic Publishing, 2017

Synopsis

Chronic lymphocytic leukemia, mantle cell lymphoma, follicular lymphoma and diffuse large B cell lymphoma represent various subtypes of B-cell lymphoid neoplasms with essential differences in cell origin, disease progression, and response to therapy. B-cell receptor (BCR) signaling has recently emerged as a central oncogenic pathway in these models, promoting tumor growth and survival. Here, we describe a new BCR-related kinase inhibitor, IQS019, which interacts with and efficiently prevents the activating phosphorylation of three apical BCR kinases (Syk, Lyn and Btk) in these models. Inhibition of BCR signaling by IQS019 leads to reduced cell proliferation, blockade of cell chemotaxis, and increased caspase-dependent apoptosis. Additionaly, in two different xenotransplant mouse models, treatment with IQS019 results in a remarkable decrease in BCR kinase phosphorylation and mitotic index, reduced tumor burden and tumor cell infiltration into the spleen. Altogether, these results warrant further investigation and clinical development of this novel BCR kinase inhibitor in mature B lymphoid malignancies.

Les informations fournies dans la section « Synopsis » peuvent faire référence à une autre édition de ce titre.

Présentation de l'éditeur

Chronic lymphocytic leukemia, mantle cell lymphoma, follicular lymphoma and diffuse large B cell lymphoma represent various subtypes of B-cell lymphoid neoplasms with essential differences in cell origin, disease progression, and response to therapy. B-cell receptor (BCR) signaling has recently emerged as a central oncogenic pathway in these models, promoting tumor growth and survival. Here, we describe a new BCR-related kinase inhibitor, IQS019, which interacts with and efficiently prevents the activating phosphorylation of three apical BCR kinases (Syk, Lyn and Btk) in these models. Inhibition of BCR signaling by IQS019 leads to reduced cell proliferation, blockade of cell chemotaxis, and increased caspase-dependent apoptosis. Additionaly, in two different xenotransplant mouse models, treatment with IQS019 results in a remarkable decrease in BCR kinase phosphorylation and mitotic index, reduced tumor burden and tumor cell infiltration into the spleen. Altogether, these results warrant further investigation and clinical development of this novel BCR kinase inhibitor in mature B lymphoid malignancies.

Biographie de l'auteur

Gaël Roué received his PhD degree in 2002 at the University of Caen, France. After a first postdoctoral experience in the Pasteur Institute of Paris, he is now leading a team working on the development of new epigenetic, oncogene-, and microenvironment-targeting drugs for aggressive B-cell lymphoma, at the IDIBAPS institute in Barcelona, Spain.

Les informations fournies dans la section « A propos du livre » peuvent faire référence à une autre édition de ce titre.

Éditeur
LAP LAMBERT Academic Publishing
Date d'édition
2017
Langue
anglais
ISBN 10 
3330090715
ISBN 13 
9783330090712
Reliure
Broché
Nombre de pages
64
Coordonnées du fabricant
non disponible
Personne responsable
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