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Protein Tyrosine Kinase Panel As a Tool for Anticancer Drug Design
The discovery of the pharmaceutical potential of small molecule inhibitors of oncogenic protein tyrosine kinases is one of the directions in target therapy in oncology. Presently, investigations aiming at developing new therapeutically important inhibitors have to be based on a combination of comput...
Autores principales: | , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
A.I. Gordeyev
2009
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3347529/ https://www.ncbi.nlm.nih.gov/pubmed/22649618 |
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author | Rakitina, T.V. Yudkina, O.V. Smirnova, E.V. Lipkin, A.V. |
author_facet | Rakitina, T.V. Yudkina, O.V. Smirnova, E.V. Lipkin, A.V. |
author_sort | Rakitina, T.V. |
collection | PubMed |
description | The discovery of the pharmaceutical potential of small molecule inhibitors of oncogenic protein tyrosine kinases is one of the directions in target therapy in oncology. Presently, investigations aiming at developing new therapeutically important inhibitors have to be based on a combination of computational and experimental approaches including biochitalicical, cell-based or in silico screening and the study of the three-dimensional structure of the kinase active center, in complex with an inhibitor, using crystallography and X-ray analysis or molecular modeling. This work is an example of a combination of inhibitor experimental search with the computational analysis of the potential mechanism of the inhibitors' action, which allowed to propose the 2-hydroxyphenol group as a scaffold for the design of new tyrosine kinase inhibitors. |
format | Online Article Text |
id | pubmed-3347529 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2009 |
publisher | A.I. Gordeyev |
record_format | MEDLINE/PubMed |
spelling | pubmed-33475292012-05-30 Protein Tyrosine Kinase Panel As a Tool for Anticancer Drug Design Rakitina, T.V. Yudkina, O.V. Smirnova, E.V. Lipkin, A.V. Acta Naturae Research Article The discovery of the pharmaceutical potential of small molecule inhibitors of oncogenic protein tyrosine kinases is one of the directions in target therapy in oncology. Presently, investigations aiming at developing new therapeutically important inhibitors have to be based on a combination of computational and experimental approaches including biochitalicical, cell-based or in silico screening and the study of the three-dimensional structure of the kinase active center, in complex with an inhibitor, using crystallography and X-ray analysis or molecular modeling. This work is an example of a combination of inhibitor experimental search with the computational analysis of the potential mechanism of the inhibitors' action, which allowed to propose the 2-hydroxyphenol group as a scaffold for the design of new tyrosine kinase inhibitors. A.I. Gordeyev 2009-10 /pmc/articles/PMC3347529/ /pubmed/22649618 Text en Copyright © 2009 Park-media Ltd. http://creativecommons.org/licenses/by/2.0/ This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. |
spellingShingle | Research Article Rakitina, T.V. Yudkina, O.V. Smirnova, E.V. Lipkin, A.V. Protein Tyrosine Kinase Panel As a Tool for Anticancer Drug Design |
title | Protein Tyrosine Kinase Panel As a Tool for Anticancer Drug Design |
title_full | Protein Tyrosine Kinase Panel As a Tool for Anticancer Drug Design |
title_fullStr | Protein Tyrosine Kinase Panel As a Tool for Anticancer Drug Design |
title_full_unstemmed | Protein Tyrosine Kinase Panel As a Tool for Anticancer Drug Design |
title_short | Protein Tyrosine Kinase Panel As a Tool for Anticancer Drug Design |
title_sort | protein tyrosine kinase panel as a tool for anticancer drug design |
topic | Research Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3347529/ https://www.ncbi.nlm.nih.gov/pubmed/22649618 |
work_keys_str_mv | AT rakitinatv proteintyrosinekinasepanelasatoolforanticancerdrugdesign AT yudkinaov proteintyrosinekinasepanelasatoolforanticancerdrugdesign AT smirnovaev proteintyrosinekinasepanelasatoolforanticancerdrugdesign AT lipkinav proteintyrosinekinasepanelasatoolforanticancerdrugdesign |