Novel Ligands Targeting α4β1 Integrin: Therapeutic Applications and Perspectives
Among the other members of the adhesion molecules' family, α4β1 integrin, a heterodimeric receptor, plays a crucial role in inflammatory diseases, cancer development, metastasis and stem cell mobilization or retention. In many cases, its function in pathogenesis is not yet completely understood...
| Main Authors: | , , , |
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| Format: | Article |
| Language: | English |
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Frontiers Media S.A.
2019-07-01
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| Series: | Frontiers in Chemistry |
| Subjects: | |
| Online Access: | https://www.frontiersin.org/article/10.3389/fchem.2019.00489/full |
| _version_ | 1817978140953149440 |
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| author | Monica Baiula Santi Spampinato Luca Gentilucci Alessandra Tolomelli |
| author_facet | Monica Baiula Santi Spampinato Luca Gentilucci Alessandra Tolomelli |
| author_sort | Monica Baiula |
| collection | DOAJ |
| description | Among the other members of the adhesion molecules' family, α4β1 integrin, a heterodimeric receptor, plays a crucial role in inflammatory diseases, cancer development, metastasis and stem cell mobilization or retention. In many cases, its function in pathogenesis is not yet completely understood and investigations on ligand binding and related stabilization of active/inactive conformations still represent an important goal. For this reason, starting from the highlight of α4β1 functions in human pathologies, we report an overview of synthetic α4β1 integrin ligands under development as potential therapeutic agents. The small molecule library that we have selected represents a collection of lead compounds. These molecules are the object of future refinement in academic and industrial research, in order to achieve a fine tuning of α4β1 integrin regulation for the development of novel agents against pathologies still eluding an effective solution. |
| first_indexed | 2024-04-13T22:26:28Z |
| format | Article |
| id | doaj.art-091caf53eedb4e9184a272f89331c577 |
| institution | Directory Open Access Journal |
| issn | 2296-2646 |
| language | English |
| last_indexed | 2024-04-13T22:26:28Z |
| publishDate | 2019-07-01 |
| publisher | Frontiers Media S.A. |
| record_format | Article |
| series | Frontiers in Chemistry |
| spelling | doaj.art-091caf53eedb4e9184a272f89331c5772022-12-22T02:27:04ZengFrontiers Media S.A.Frontiers in Chemistry2296-26462019-07-01710.3389/fchem.2019.00489472116Novel Ligands Targeting α4β1 Integrin: Therapeutic Applications and PerspectivesMonica Baiula0Santi Spampinato1Luca Gentilucci2Alessandra Tolomelli3Department of Pharmacy and Biotechnology, University of Bologna, Bologna, ItalyDepartment of Pharmacy and Biotechnology, University of Bologna, Bologna, ItalyDepartment of Chemistry “G. Ciamician,” University of Bologna, Bologna, ItalyDepartment of Chemistry “G. Ciamician,” University of Bologna, Bologna, ItalyAmong the other members of the adhesion molecules' family, α4β1 integrin, a heterodimeric receptor, plays a crucial role in inflammatory diseases, cancer development, metastasis and stem cell mobilization or retention. In many cases, its function in pathogenesis is not yet completely understood and investigations on ligand binding and related stabilization of active/inactive conformations still represent an important goal. For this reason, starting from the highlight of α4β1 functions in human pathologies, we report an overview of synthetic α4β1 integrin ligands under development as potential therapeutic agents. The small molecule library that we have selected represents a collection of lead compounds. These molecules are the object of future refinement in academic and industrial research, in order to achieve a fine tuning of α4β1 integrin regulation for the development of novel agents against pathologies still eluding an effective solution.https://www.frontiersin.org/article/10.3389/fchem.2019.00489/fullα4β1 integrinagonistantagonistsmall moleculesinflammatory disorders |
| spellingShingle | Monica Baiula Santi Spampinato Luca Gentilucci Alessandra Tolomelli Novel Ligands Targeting α4β1 Integrin: Therapeutic Applications and Perspectives Frontiers in Chemistry α4β1 integrin agonist antagonist small molecules inflammatory disorders |
| title | Novel Ligands Targeting α4β1 Integrin: Therapeutic Applications and Perspectives |
| title_full | Novel Ligands Targeting α4β1 Integrin: Therapeutic Applications and Perspectives |
| title_fullStr | Novel Ligands Targeting α4β1 Integrin: Therapeutic Applications and Perspectives |
| title_full_unstemmed | Novel Ligands Targeting α4β1 Integrin: Therapeutic Applications and Perspectives |
| title_short | Novel Ligands Targeting α4β1 Integrin: Therapeutic Applications and Perspectives |
| title_sort | novel ligands targeting α4β1 integrin therapeutic applications and perspectives |
| topic | α4β1 integrin agonist antagonist small molecules inflammatory disorders |
| url | https://www.frontiersin.org/article/10.3389/fchem.2019.00489/full |
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