Inhibition of carbonic anhydrase IX targets primary tumors, metastases, and cancer stem cells : Three for the price of one
© 2018 Wiley Periodicals, Inc..
Human carbonic anhydrase (CA) IX is a tumor-associated protein, since it is scarcely present in normal tissues, but highly overexpressed in a large number of solid tumors, where it actively contributes to survival and metastatic spread of tumor cells. Due to these features, the characterization of its biochemical, structural, and functional features for drug design purposes has been extensively carried out, with consequent development of several highly selective small molecule inhibitors and monoclonal antibodies to be used for different purposes. Aim of this review is to provide a comprehensive state-of-the-art of studies performed on this enzyme, regarding structural, functional, and biomedical aspects, as well as the development of molecules with diagnostic and therapeutic applications for cancer treatment. A brief description of additional pharmacologic applications for CA IX inhibition in other diseases, such as arthritis and ischemia, is also provided.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2018 |
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| Erschienen: |
2018 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:38 |
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| Enthalten in: |
Medicinal research reviews - 38(2018), 6 vom: 10. Sept., Seite 1799-1836 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Supuran, Claudiu T [VerfasserIn] |
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| Links: |
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| Anmerkungen: |
Date Completed 08.02.2019 Date Revised 15.02.2019 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1002/med.21497 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM282845135 |
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| 520 | |a © 2018 Wiley Periodicals, Inc. | ||
| 520 | |a Human carbonic anhydrase (CA) IX is a tumor-associated protein, since it is scarcely present in normal tissues, but highly overexpressed in a large number of solid tumors, where it actively contributes to survival and metastatic spread of tumor cells. Due to these features, the characterization of its biochemical, structural, and functional features for drug design purposes has been extensively carried out, with consequent development of several highly selective small molecule inhibitors and monoclonal antibodies to be used for different purposes. Aim of this review is to provide a comprehensive state-of-the-art of studies performed on this enzyme, regarding structural, functional, and biomedical aspects, as well as the development of molecules with diagnostic and therapeutic applications for cancer treatment. A brief description of additional pharmacologic applications for CA IX inhibition in other diseases, such as arthritis and ischemia, is also provided | ||
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| 700 | 1 | |a De Simone, Giuseppina |e verfasserin |4 aut | |
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