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Cyclotraxin B

Cyclotraxin B
Cyclotraxin B.svg
Clinical data
Other namesCTX-B
ATC code
  • None
Identifiers
CAS Number
PubChem CID
ChemSpider
Chemical and physical data
FormulaC48H73N13O17S3
Molar mass1200.365 g/mol g·mol−1
3D model (JSmol)

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. ^ a b c Cazorla, Maxime; Jouvenceau, Anne; Rose, Christiane; Guilloux, Jean-Philippe; Pilon, Catherine; Dranovsky, Alex; Prémont, Joël (2010). "Cyclotraxin-B, the First Highly Potent and Selective TrkB Inhibitor, Has Anxiolytic Properties in Mice". PLoS ONE. 5 (3): e9777. doi:10.1371/journal.pone.0009777. ISSN 1932-6203. PMC 2841647. PMID 20333308.
  2. ^ a b De Smet, Frederik; Christopoulos, Arthur; Carmeliet, Peter (2014). "Allosteric targeting of receptor tyrosine kinases". Nature Biotechnology. 32 (11): 1113–1120. doi:10.1038/nbt.3028. ISSN 1087-0156.
  3. ^ Growth Factor Receptors—Advances in Research and Application: 2013 Edition. ScholarlyEditions. 21 June 2013. pp. 42–. ISBN 978-1-4816-7619-9.
  4. ^ Advances in Physiology Research and Application: 2011 Edition. ScholarlyEditions. 9 January 2012. pp. 1431–. ISBN 978-1-4649-2075-2.
  5. ^ Constandil, Luis; Goich, Mariela; Hernández, Alejandro; Bourgeais, Laurence; Cazorla, Maxime; Hamon, Michel; Villanueva, Luis; Pelissier, Teresa (2012). "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): 579–589. doi:10.1016/j.jpain.2012.03.008. ISSN 1526-5900.