Cyclotraxin B
- None
- (3S,6R,11R,17S,20S,23S,26S,32S,35S)-6-amino-20-(4-aminobutyl)-3-(2-amino-2-oxoethyl)-17-(2-carboxyethyl)-23-[(1R)-1-hydroxyethyl]-26-[(4-hydroxyphenyl)methyl]-32-(2-methylsulfanylethyl)-2,5,13,16,19,22,25,28,31,34-decaoxo-8,9-dithia-1,4,12,15,18,21,24,27,30,33-decazabicyclo[33.3.0]octatriacontane-11-carboxylic acid
- 1203586-72-4
- 90489002
- 29785020
- DTXSID501045820
- Interactive image
- CC(C1C(=O)NC(C(=O)NC(C(=O)NCC(=O)NC(CSSCC(C(=O)NC(C(=O)N2CCCC2C(=O)NC(C(=O)NCC(=O)NC(C(=O)N1)CC3=CC=C(C=C3)O)CCSC)CC(=O)N)N)C(=O)O)CCC(=O)O)CCCCN)O
- InChI=1S/C48H73N13O17S3/c1-24(62)39-46(75)58-28(6-3-4-15-49)43(72)56-29(12-13-38(67)68)41(70)52-21-37(66)55-33(48(77)78)23-81-80-22-27(50)40(69)59-32(19-35(51)64)47(76)61-16-5-7-34(61)45(74)57-30(14-17-79-2)42(71)53-20-36(65)54-31(44(73)60-39)18-25-8-10-26(63)11-9-25/h8-11,24,27-34,39,62-63H,3-7,12-23,49-50H2,1-2H3,(H2,51,64)(H,52,70)(H,53,71)(H,54,65)(H,55,66)(H,56,72)(H,57,74)(H,58,75)(H,59,69)(H,60,73)(H,67,68)(H,77,78)/t24-,27+,28+,29+,30+,31+,32+,33+,34+,39+/m1/s1
- Key:JLBMMJHZUYBFGX-ZHTCEXBHSA-N
Cyclotraxin B (CTX-B) is a small (1200 Da) cyclic peptide and highly potent (IC50 = 0.30 nM), selective, and non-competitive antagonist or negative allosteric modulator of TrkB, the main receptor of brain-derived neurotrophic factor (BDNF).[1][2] CTX-B was originally developed by Cazorla M. and colleagues at Université Paris and Inserm in 2010, mimicking a specific structural loop in BDNF known for its functional selectivity.[1][3] Cyclotraxin-B's name originates from Cyclic trk inhibitor B.[1]
CTX-B 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
- ^ a b c d Cazorla M, Jouvenceau A, Rose C, Guilloux JP, Pilon C, Dranovsky A, Prémont J (March 2010). "Cyclotraxin-B, the first highly potent and selective TrkB inhibitor, has anxiolytic properties in mice". PLOS ONE. 5 (3): e9777. Bibcode:2010PLoSO...5.9777C. doi:10.1371/journal.pone.0009777. PMC 2841647. PMID 20333308.
- ^ a b De Smet F, Christopoulos A, Carmeliet P (November 2014). "Allosteric targeting of receptor tyrosine kinases". Nature Biotechnology. 32 (11): 1113–20. doi:10.1038/nbt.3028. PMID 25380447. S2CID 12609911.
- ^ Growth Factor Receptors—Advances in Research and Application: 2013 Edition. ScholarlyEditions. 21 June 2013. pp. 42–. ISBN 978-1-4816-7619-9.
- ^ Advances in Physiology Research and Application: 2011 Edition. ScholarlyEditions. 9 January 2012. pp. 1431–. ISBN 978-1-4649-2075-2.
- ^ Constandil L, Goich M, Hernández A, Bourgeais L, Cazorla M, Hamon M, et al. (June 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): 579–89. doi:10.1016/j.jpain.2012.03.008. hdl:10533/130454. PMID 22560237.
- v
- t
- e
- Agonists: Angiopoietin 1
- Angiopoietin 4
- Antagonists: Angiopoietin 2
- Angiopoietin 3
- Kinase inhibitors: Altiratinib
- CE-245677
- Rebastinib
- Antibodies: Evinacumab (against angiopoietin 3)
- Nesvacumab (against angiopoietin 2)
EGF (ErbB1/HER1) |
|
---|---|
ErbB2/HER2 |
|
ErbB3/HER3 |
|
ErbB4/HER4 |
|
FGFR1 | |
---|---|
FGFR2 |
|
FGFR3 | |
FGFR4 | |
Unsorted |
|
- Agonists: Fosgonimeton
- Hepatocyte growth factor
- Potentiators: Dihexa (PNB-0408)
- Kinase inhibitors: Altiratinib
- AM7
- AMG-458
- Amuvatinib
- BMS-777607
- Cabozantinib
- Capmatinib
- Crizotinib
- Foretinib
- Golvatinib
- INCB28060
- JNJ-38877605
- K252a
- MK-2461
- PF-04217903
- PF-2341066
- PHA-665752
- SU-11274
- Tivantinib
- Volitinib
- Antibodies: Emibetuzumab
- Ficlatuzumab
- Flanvotumab
- Onartuzumab
- Rilotumumab
- Telisotuzumab
- Telisotuzumab vedotin
IGF-1 |
|
---|---|
IGF-2 |
|
Others |
- Antagonists: ALE-0540
- Dexamethasone
- EVT-901 (SAR-127963)
- Testosterone
- Antibodies: Against NGF: ABT-110 (PG110)
- ASP-6294
- Fasinumab
- Frunevetmab
- Fulranumab
- MEDI-578
- Ranevetmab
- Tanezumab
- Aptamers: Against NGF: RBM-004
- Decoy receptors: LEVI-04 (p75NTR-Fc)
- Agonists: Becaplermin
- Platelet-derived growth factor (A, B, C, D)
- Kinase inhibitors: Agerafenib
- Avapritinib
- Axitinib
- Crenolanib
- Imatinib
- Lenvatinib
- Masitinib
- Motesanib
- Nintedanib
- Pazopanib
- Radotinib
- Quizartinib
- Ripretinib
- Sunitinib
- Sorafenib
- Toceranib
- Antibodies: Olaratumab
- Ramucirumab
- Tovetumab
GFRα1 |
|
---|---|
GFRα2 |
|
GFRα3 |
|
GFRα4 |
|
Unsorted |
|
- See here instead.
TrkA |
|
---|---|
TrkB |
|
TrkC |
|
- Agonists: Placental growth factor (PGF)
- Ripretinib
- Telbermin
- VEGF (A, B, C, D (FIGF))
- Allosteric modulators: Cyclotraxin B
- Kinase inhibitors: Agerafenib
- Altiratinib
- Axitinib
- Cabozantinib
- Cediranib
- Fruquintinib
- Lapatinib
- Lenvatinib
- Motesanib
- Nintedanib
- Pazopanib
- Pegaptanib
- Rebastinib
- Regorafenib
- Semaxanib
- Sorafenib
- Sunitinib
- Toceranib
- Tivozanib
- Vandetanib
- WHI-P 154
- Antibodies: Alacizumab pegol
- Bevacizumab
- Icrucumab
- Ramucirumab
- Ranibizumab
- Decoy receptors: Aflibercept
- Additional growth factors: Adrenomedullin
- Colony-stimulating factors (see here instead)
- Connective tissue growth factor (CTGF)
- Ephrins (A1, A2, A3, A4, A5, B1, B2, B3)
- Erythropoietin (see here instead)
- Glucose-6-phosphate isomerase (GPI; PGI, PHI, AMF)
- Glia maturation factor (GMF)
- Hepatoma-derived growth factor (HDGF)
- Interleukins/T-cell growth factors (see here instead)
- Leukemia inhibitory factor (LIF)
- Macrophage-stimulating protein (MSP; HLP, HGFLP)
- Midkine (NEGF2)
- Migration-stimulating factor (MSF; PRG4)
- Oncomodulin
- Pituitary adenylate cyclase-activating peptide (PACAP)
- Pleiotrophin
- Renalase
- Thrombopoietin (see here instead)
- Wnt signaling proteins
- Additional growth factor receptor modulators: Cerebrolysin (neurotrophin mixture)
This article about an anxiolytic is a stub. You can help Wikipedia by expanding it. |
- v
- t
- e