Chemistry:Cyclotraxin B
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Short description: Chemical compound
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| Other names | CTX-B |
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| Formula | C48H73N13O17S3 |
| Molar mass | 1200.37 g·mol−1 |
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Cyclotraxin B (CTX-B) is a small (1200 Da) cyclic peptide and highly potent, selective, non-competitive antagonist or negative allosteric modulator of TrkB (IC50 = 0.30 nM),[1][2] the main receptor of brain-derived neurotrophic factor (BDNF), which itself was derived from BDNF.[1][3] It crosses the blood-brain-barrier with systemic administration and produces anxiolytic-like effects in animals, though notably not antidepressant-like effects.[1][4] The compound has also been found to produce analgesic effects in animal models of neuropathic pain.[5] In addition to TrkB, CTX-B has been found to be an allosteric modulator of VEGFR2, one of the receptors of vascular endothelial growth factor (VEGF).[2]
See also
References
- ↑ 1.0 1.1 1.2 "Cyclotraxin-B, the first highly potent and selective TrkB inhibitor, has anxiolytic properties in mice". PLOS ONE 5 (3): e9777. March 2010. doi:10.1371/journal.pone.0009777. PMID 20333308. Bibcode: 2010PLoSO...5.9777C.
- ↑ 2.0 2.1 "Allosteric targeting of receptor tyrosine kinases". Nature Biotechnology 32 (11): 1113–20. November 2014. doi:10.1038/nbt.3028. PMID 25380447.
- ↑ Growth Factor Receptors—Advances in Research and Application: 2013 Edition. ScholarlyEditions. 21 June 2013. pp. 42–. ISBN 978-1-4816-7619-9. https://books.google.com/books?id=TUMQdWDjquoC&pg=PA42.
- ↑ Advances in Physiology Research and Application: 2011 Edition. ScholarlyEditions. 9 January 2012. pp. 1431–. ISBN 978-1-4649-2075-2. https://books.google.com/books?id=2L3GurwjBK0C&pg=PA1431.
- ↑ "Cyclotraxin-B, a new TrkB antagonist, and glial blockade by propentofylline, equally prevent and reverse cold allodynia induced by BDNF or partial infraorbital nerve constriction in mice". The Journal of Pain 13 (6): 579–89. June 2012. doi:10.1016/j.jpain.2012.03.008. PMID 22560237.
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