Publication

Improved Angiostatic Activity of Dasatinib by Modulation with Hydrophobic Chains

Paul Joseph Dyson, Patrycja Nowak-Sliwinska, Catherine Marie Amélie Clavel, Emilia Paunescu
2015
Journal Articles

Abstract

Dasatinib is an orally active nonselective tyrosine kinase inhibitor used to treat certain types of adult leukemia. By inhibiting PDGFR-beta and SFKs in both tumor cells and tumor associated endothelial cells, dasatinib inhibits tumor growth and angiogenesis. Herein, dasatinib derivatives modified with hydrophobic chains were prepared and evaluated for their in vitro antiproliferative selectivity and their in vivo antiangiogenic activity. For one of the derivatives, modified with a long perfluorinated chain, a significant enhancement in antiangiogenic activity was observed. Combined, these results suggest a possible generic route to modulate the angiostatic activity of drugs.

Official source

https://infoscience.epfl.ch/entities/publication/45f42155-203b-49f1-9a6b-a139cabb7bc6

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Paul Joseph Dyson, Patrycja Nowak-Sliwinska, Catherine Marie Amélie Clavel, Emilia Paunescu
2015
Journal Articles

Abstract

Official source

https://infoscience.epfl.ch/entities/publication/45f42155-203b-49f1-9a6b-a139cabb7bc6

About this result

Related concepts (25)

Neoplasm

A neoplasm (ˈniː.oʊˌplæzəm,_ˈniː.ə-) is a type of abnormal and excessive growth of tissue. The process that occurs to form or produce a neoplasm is called neoplasia. The growth of a neoplasm is uncoordinated with that of the normal surrounding tissue, and persists in growing abnormally, even if the original trigger is removed. This abnormal growth usually forms a mass, when it may be called a tumour or tumor. ICD-10 classifies neoplasms into four main groups: benign neoplasms, in situ neoplasms, malignant neoplasms, and neoplasms of uncertain or unknown behavior.

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Tumor antigen

Tumor antigen is an antigenic substance produced in tumor cells, i.e., it triggers an immune response in the host. Tumor antigens are useful tumor markers in identifying tumor cells with diagnostic tests and are potential candidates for use in cancer therapy. The field of cancer immunology studies such topics. Normal proteins in the body are not antigenic because of self-tolerance, a process in which self-reacting cytotoxic T lymphocytes (CTLs) and autoantibody-producing B lymphocytes are culled "centrally" in primary lymphatic tissue (BM) and "peripherally" in secondary lymphatic tissue (mostly thymus for T-cells and spleen/lymph nodes for B cells).

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