Small molecules targeting glycogen synthase kinase 3 as potential drug candidates for the treatment of retinitis pigmentosa
Retinitis pigmentosa (RP) is an inherited retinal dystrophy that courses with progressive degeneration of retinal tissue and loss of vision. Currently, RP is an unpreventable, incurable condition. We propose glycogen synthase kinase 3 (GSK-3) inhibitors as potential leads for retinal cell neuroprotection, since the retina is also a part of the central nervous system and GSK-3 inhibitors are potent neuroprotectant agents. Using a chemical genetic approach, diverse small molecules with different potency and binding mode to GSK-3 have been used to validate and confirm GSK-3 as a pharmacological target for RP. Moreover, this medicinal chemistry approach has provided new leads for the future disease-modifying treatment of RP.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2017 |
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| Erschienen: |
2017 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:32 |
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| Enthalten in: |
Journal of enzyme inhibition and medicinal chemistry - 32(2017), 1 vom: 24. Dez., Seite 522-526 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Marchena, Miguel [VerfasserIn] |
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| Links: |
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| Themen: |
EC 2.7.11.26 |
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| Anmerkungen: |
Date Completed 23.02.2017 Date Revised 13.11.2018 published: Print Citation Status MEDLINE |
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| doi: |
10.1080/14756366.2016.1265522 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM268261717 |
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| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Retinitis pigmentosa (RP) is an inherited retinal dystrophy that courses with progressive degeneration of retinal tissue and loss of vision. Currently, RP is an unpreventable, incurable condition. We propose glycogen synthase kinase 3 (GSK-3) inhibitors as potential leads for retinal cell neuroprotection, since the retina is also a part of the central nervous system and GSK-3 inhibitors are potent neuroprotectant agents. Using a chemical genetic approach, diverse small molecules with different potency and binding mode to GSK-3 have been used to validate and confirm GSK-3 as a pharmacological target for RP. Moreover, this medicinal chemistry approach has provided new leads for the future disease-modifying treatment of RP | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a GSK-3 inhibitors | |
| 650 | 4 | |a glaucoma | |
| 650 | 4 | |a retinal diseases | |
| 650 | 4 | |a retinitis pigmentosa | |
| 650 | 7 | |a Neuroprotective Agents |2 NLM | |
| 650 | 7 | |a Protein Kinase Inhibitors |2 NLM | |
| 650 | 7 | |a Small Molecule Libraries |2 NLM | |
| 650 | 7 | |a Glycogen Synthase Kinase 3 |2 NLM | |
| 650 | 7 | |a EC 2.7.11.26 |2 NLM | |
| 700 | 1 | |a Villarejo-Zori, Beatriz |e verfasserin |4 aut | |
| 700 | 1 | |a Zaldivar-Diez, Josefa |e verfasserin |4 aut | |
| 700 | 1 | |a Palomo, Valle |e verfasserin |4 aut | |
| 700 | 1 | |a Gil, Carmen |e verfasserin |4 aut | |
| 700 | 1 | |a Hernández-Sánchez, Catalina |e verfasserin |4 aut | |
| 700 | 1 | |a Martínez, Ana |e verfasserin |4 aut | |
| 700 | 1 | |a de la Rosa, Enrique J |e verfasserin |4 aut | |
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