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dc.contributor.authorFasano, M
dc.contributor.authorDella Corte, C
dc.contributor.authorCalifano, Raffaele
dc.contributor.authorCapuano, A
dc.contributor.authorTroiani, T
dc.contributor.authorMartinelli, E
dc.contributor.authorCiardiello, F
dc.contributor.authorMorgillo, F
dc.date.accessioned2014-07-14T15:06:35Z
dc.date.available2014-07-14T15:06:35Z
dc.date.issued2014-06
dc.identifier.citationType III or allosteric kinase inhibitors for the treatment of non-small cell lung cancer. 2014, 23 (6):809-21 Expert Opin Investig Drugsen
dc.identifier.issn1744-7658
dc.identifier.pmid24673358
dc.identifier.doi10.1517/13543784.2014.902934
dc.identifier.urihttp://hdl.handle.net/10541/322889
dc.description.abstractIn recent times, there has been much interest in the development of pharmacological kinase inhibitors that treat NSCLC. Furthermore, treatment options have been guided by the development of a wide panel of synthetic small molecule kinase inhibitors. Most of the molecules developed belong to the type I class of inhibitors that target the ATP-binding site in its active conformation. The high sequence similarity in the ATP-binding site among members of the kinase families often results in low selectivity and additional toxicities. Also, second mutations in the ATP-binding site, such as threonine to methionine at position 790, have been described as a mechanism of resistance to ATP-competitive kinase inhibitors. For these reasons, alternative drug development approaches targeting sites other than the ATP cleft are being pursued. The class III or allosteric inhibitors, which bind outside the ATP-binding site, have been shown to negatively modulate kinase activity.
dc.language.isoenen
dc.rightsArchived with thanks to Expert opinion on investigational drugsen
dc.titleType III or allosteric kinase inhibitors for the treatment of non-small cell lung cancer.en
dc.typeArticleen
dc.contributor.departmentSecond University of Naples, Medical Oncology, Department of Experimental and Internal Medicine "F. Magrassi e A. Lanzara" , Via S. Pansini 5, 80131 Napoli , Italia +39 081 5666745 ; +39 081 5666732 ;en
dc.identifier.journalExpert Opinion on Investigational Drugsen
html.description.abstractIn recent times, there has been much interest in the development of pharmacological kinase inhibitors that treat NSCLC. Furthermore, treatment options have been guided by the development of a wide panel of synthetic small molecule kinase inhibitors. Most of the molecules developed belong to the type I class of inhibitors that target the ATP-binding site in its active conformation. The high sequence similarity in the ATP-binding site among members of the kinase families often results in low selectivity and additional toxicities. Also, second mutations in the ATP-binding site, such as threonine to methionine at position 790, have been described as a mechanism of resistance to ATP-competitive kinase inhibitors. For these reasons, alternative drug development approaches targeting sites other than the ATP cleft are being pursued. The class III or allosteric inhibitors, which bind outside the ATP-binding site, have been shown to negatively modulate kinase activity.


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