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- W2973889730 endingPage "111703" @default.
- W2973889730 startingPage "111703" @default.
- W2973889730 abstract "Heme oxygenase (HO) enzymes are involved in heme catabolism and several physiological functions. Among the different HO isoforms, HO-2 stands out for its neuroprotective properties and modulatory activity in male reproduction. However, unlike the HO-1 ligands, the potential therapeutic applications of HO-2 inhibitors/activators have not been extensively explored yet. Moreover, the physiological role of HO-2 is still unclear, mostly due to the lack of highly selective HO-2 chemical probes. To boost the interest on this intriguing target, the present review updates the knowledge on the structure-activity relationships of HO-2 inhibitors and activators, as well as their potential therapeutic applications. To the best of our knowledge, among HO-2 inhibitors, clemizole derivatives are the most selective HO-2 inhibitors reported so far (IC50 HO-1 >100 μM, IC50 HO-2 = 3.4 μM), while the HO-2 nonselective inhibitors described herein possess IC50 HO-2 values ≤ 10 μM. Furthermore, the development of HO-2 activators, such as menadione analogues, helped to understand the critical moieties required for HO-2 activation. Recent advances in the potential therapeutic applications of HO-2 inhibitors/activators cover the fields of neurodegenerative, cardiovascular, inflammatory, and reproductive diseases further stimulating the interest towards this target." @default.
- W2973889730 created "2019-09-26" @default.
- W2973889730 creator A5006967238 @default.
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- W2973889730 creator A5076017923 @default.
- W2973889730 creator A5076233600 @default.
- W2973889730 creator A5084855762 @default.
- W2973889730 date "2019-12-01" @default.
- W2973889730 modified "2023-10-10" @default.
- W2973889730 title "Heme Oxygenase-2 (HO-2) as a therapeutic target: Activators and inhibitors" @default.
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