Serum and glucocorticoid-regulated kinase 1: Structure, biological functions, and its inhibitors
Serum and glucocorticoid-regulated kinase 1 (SGK1) is a serine/threonine kinase belonging to the protein kinase A, G, and C (AGC) family. Upon initiation of the phosphoinositide 3-kinase (PI3K) signaling pathway, mammalian target of rapamycin complex 2 (mTORC2) and phosphoinositide-dependent protein...
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| Format: | Article |
| Language: | English |
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Frontiers Media S.A.
2022-11-01
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| Series: | Frontiers in Pharmacology |
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| Online Access: | https://www.frontiersin.org/articles/10.3389/fphar.2022.1036844/full |
| _version_ | 1798018578706857984 |
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| author | Hyunsoo Jang Youngjun Park Youngjun Park Jaebong Jang |
| author_facet | Hyunsoo Jang Youngjun Park Youngjun Park Jaebong Jang |
| author_sort | Hyunsoo Jang |
| collection | DOAJ |
| description | Serum and glucocorticoid-regulated kinase 1 (SGK1) is a serine/threonine kinase belonging to the protein kinase A, G, and C (AGC) family. Upon initiation of the phosphoinositide 3-kinase (PI3K) signaling pathway, mammalian target of rapamycin complex 2 (mTORC2) and phosphoinositide-dependent protein kinase 1 (PDK1) phosphorylate the hydrophobic motif and kinase domain of SGK1, respectively, inducing SGK1 activation. SGK1 modulates essential cellular processes such as proliferation, survival, and apoptosis. Hence, dysregulated SGK1 expression can result in multiple diseases, including hypertension, cancer, autoimmunity, and neurodegenerative disorders. This review provides a current understanding of SGK1, particularly in sodium transport, cancer progression, and autoimmunity. In addition, we summarize the developmental status of SGK1 inhibitors, their structures, and respective potencies evaluated in pre-clinical experimental settings. Collectively, this review highlights the significance of SGK1 and proposes SGK1 inhibitors as potential drugs for treatment of clinically relevant diseases. |
| first_indexed | 2024-04-11T16:26:26Z |
| format | Article |
| id | doaj.art-14fd627ac117442493d172b417c58bb1 |
| institution | Directory Open Access Journal |
| issn | 1663-9812 |
| language | English |
| last_indexed | 2024-04-11T16:26:26Z |
| publishDate | 2022-11-01 |
| publisher | Frontiers Media S.A. |
| record_format | Article |
| series | Frontiers in Pharmacology |
| spelling | doaj.art-14fd627ac117442493d172b417c58bb12022-12-22T04:14:09ZengFrontiers Media S.A.Frontiers in Pharmacology1663-98122022-11-011310.3389/fphar.2022.10368441036844Serum and glucocorticoid-regulated kinase 1: Structure, biological functions, and its inhibitorsHyunsoo Jang0Youngjun Park1Youngjun Park2Jaebong Jang3College of Pharmacy, Korea University, Sejong, South KoreaLaboratory of Immune and Inflammatory Disease, College of Pharmacy, Jeju Research Institute of Pharmaceutical Sciences, Jeju National University, Jeju, South KoreaInterdisciplinary Graduate Program in Advanced Convergence Technology and Science, Jeju National University, Jeju, South KoreaCollege of Pharmacy, Korea University, Sejong, South KoreaSerum and glucocorticoid-regulated kinase 1 (SGK1) is a serine/threonine kinase belonging to the protein kinase A, G, and C (AGC) family. Upon initiation of the phosphoinositide 3-kinase (PI3K) signaling pathway, mammalian target of rapamycin complex 2 (mTORC2) and phosphoinositide-dependent protein kinase 1 (PDK1) phosphorylate the hydrophobic motif and kinase domain of SGK1, respectively, inducing SGK1 activation. SGK1 modulates essential cellular processes such as proliferation, survival, and apoptosis. Hence, dysregulated SGK1 expression can result in multiple diseases, including hypertension, cancer, autoimmunity, and neurodegenerative disorders. This review provides a current understanding of SGK1, particularly in sodium transport, cancer progression, and autoimmunity. In addition, we summarize the developmental status of SGK1 inhibitors, their structures, and respective potencies evaluated in pre-clinical experimental settings. Collectively, this review highlights the significance of SGK1 and proposes SGK1 inhibitors as potential drugs for treatment of clinically relevant diseases.https://www.frontiersin.org/articles/10.3389/fphar.2022.1036844/fullSGK1kinase inhibitorion channelcancerT cell modulation |
| spellingShingle | Hyunsoo Jang Youngjun Park Youngjun Park Jaebong Jang Serum and glucocorticoid-regulated kinase 1: Structure, biological functions, and its inhibitors Frontiers in Pharmacology SGK1 kinase inhibitor ion channel cancer T cell modulation |
| title | Serum and glucocorticoid-regulated kinase 1: Structure, biological functions, and its inhibitors |
| title_full | Serum and glucocorticoid-regulated kinase 1: Structure, biological functions, and its inhibitors |
| title_fullStr | Serum and glucocorticoid-regulated kinase 1: Structure, biological functions, and its inhibitors |
| title_full_unstemmed | Serum and glucocorticoid-regulated kinase 1: Structure, biological functions, and its inhibitors |
| title_short | Serum and glucocorticoid-regulated kinase 1: Structure, biological functions, and its inhibitors |
| title_sort | serum and glucocorticoid regulated kinase 1 structure biological functions and its inhibitors |
| topic | SGK1 kinase inhibitor ion channel cancer T cell modulation |
| url | https://www.frontiersin.org/articles/10.3389/fphar.2022.1036844/full |
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