Anaplastic Lymphoma Kinase (ALK) is a receptor tyrosine kinase that belongs to the Insulin receptor subfamily involved as full length receptor in neural development. Even if the expression of ALK protein is down-regulated in the adults, the ALK full length is expressed in different types of tumors. Moreover, chromosomal rearrangements, involving the alk gene, can occur leading the formation of different ALK fusion proteins characterized by the kinase domain of ALK fused to several partners that determine cellular localization. Structural investigation and characterization of the ALK kinase domain in absence of its crystal structure constituted the basis of development of ALK small molecule inhibitors. Here, we described normal function of the ALK receptor and its role in tumors; formation of the constitutively activated ALK fusion proteins and we reported an update of developed small molecule inhibitors of the ALK kinase activity.

Tartari, C., Scapozza, L., & GAMBACORTI PASSERINI, C. (2011). The ALK gene, an attractive target for inhibitor development. CURRENT TOPICS IN MEDICINAL CHEMISTRY, 11(11), 1406-1419 [10.2174/156802611795589593].

The ALK gene, an attractive target for inhibitor development

TARTARI, CARMEN GIULIA;GAMBACORTI PASSERINI, CARLO
2011

Abstract

Anaplastic Lymphoma Kinase (ALK) is a receptor tyrosine kinase that belongs to the Insulin receptor subfamily involved as full length receptor in neural development. Even if the expression of ALK protein is down-regulated in the adults, the ALK full length is expressed in different types of tumors. Moreover, chromosomal rearrangements, involving the alk gene, can occur leading the formation of different ALK fusion proteins characterized by the kinase domain of ALK fused to several partners that determine cellular localization. Structural investigation and characterization of the ALK kinase domain in absence of its crystal structure constituted the basis of development of ALK small molecule inhibitors. Here, we described normal function of the ALK receptor and its role in tumors; formation of the constitutively activated ALK fusion proteins and we reported an update of developed small molecule inhibitors of the ALK kinase activity.
Articolo in rivista - Articolo scientifico
Cell signaling, PKA, cAMP, multi-targeting, disease, pharmacological treatment, intracellular signaling pathway components, spatiotemporal regulation, asthma, chronic obstructive pulmonary disease, COPD, cAMP pathway
English
1406
1419
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Tartari, C., Scapozza, L., & GAMBACORTI PASSERINI, C. (2011). The ALK gene, an attractive target for inhibitor development. CURRENT TOPICS IN MEDICINAL CHEMISTRY, 11(11), 1406-1419 [10.2174/156802611795589593].
Tartari, C; Scapozza, L; GAMBACORTI PASSERINI, C
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/10281/28613
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