Chemistry:SAFit2
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| Formula | C46H62N2O10 |
| Molar mass | 802.99 g·mol−1 |
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SAFit2 is a drug which acts as a potent and selective inhibitor of the signalling factor FK506 binding protein 51 (FKBP51), which is involved in the downstream response to glucocorticoid release in the body.[1] Since elevated glucocorticoid levels are a characteristic marker of chronic stress, blocking glucocorticoid signalling pathways using SAFit2 has been shown to counteract many of the associated symptoms such as obesity,[2][3] chronic pain,[4][5] depression and anxiety,[6][7] and addiction.[8][9] While SAFit2 itself is a relatively large molecule and is unlikely to have suitable properties to be developed for medical use, it has demonstrated that inhibition of FKBP51 may be a useful therapeutic approach for alleviating consequences of long-term chronic stress and pain.
See also
References
- ↑ "Selective inhibitors of the FK506-binding protein 51 by induced fit". Nature Chemical Biology 11 (1): 33–7. January 2015. doi:10.1038/nchembio.1699. PMID 25436518.
- ↑ "Stress-responsive FKBP51 regulates AKT2-AS160 signaling and metabolic function". Nature Communications 8 (1): 1725. November 2017. doi:10.1038/s41467-017-01783-y. PMID 29170369. Bibcode: 2017NatCo...8.1725B.
- ↑ "Focus on FKBP51: A molecular link between stress and metabolic disorders". Molecular Metabolism 29: 170–181. November 2019. doi:10.1016/j.molmet.2019.09.003. PMID 31668388.
- ↑ "The stress regulator FKBP51 drives chronic pain by modulating spinal glucocorticoid signaling". Science Translational Medicine 8 (325): 325ra19. February 2016. doi:10.1126/scitranslmed.aab3376. PMID 26865567.
- ↑ "The stress regulator FKBP51: a novel and promising druggable target for the treatment of persistent pain states across sexes". Pain 159 (7): 1224–1234. July 2018. doi:10.1097/j.pain.0000000000001204. PMID 29533388.
- ↑ "Pharmacological Inhibition of the Psychiatric Risk Factor FKBP51 Has Anxiolytic Properties". The Journal of Neuroscience 35 (24): 9007–16. June 2015. doi:10.1523/JNEUROSCI.4024-14.2015. PMID 26085626.
- ↑ "Pharmacological Modulation of the Psychiatric Risk Factor FKBP51 Alters Efficiency of Common Antidepressant Drugs". Frontiers in Behavioral Neuroscience 12: 262. 2018. doi:10.3389/fnbeh.2018.00262. PMID 30483074.
- ↑ "The selective FKBP51 inhibitor SAFit2 reduces alcohol consumption and reinstatement of conditioned alcohol effects in mice". Addiction Biology 25 (3): e12758. May 2020. doi:10.1111/adb.12758. PMID 31173432.
- ↑ "Targeting the Glucocorticoid Receptor Reduces Binge-Like Drinking in High Drinking in the Dark (HDID-1) Mice". Alcoholism: Clinical and Experimental Research 44 (5): 1025–1036. March 2020. doi:10.1111/acer.14318. PMID 32154593.
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