PE 22-28

PE 22-28
Identifiers
	IUPAC name (2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(2-aminoacetyl)amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]acetyl]amino]-4-methylpentanoyl]amino]-5-(diaminomethylideneamino)pentanoic acid;
CAS Number	1801959-12-5;
PubChem CID	165437303;
ChemSpider	128942433;
Chemical and physical data
Formula	C35H56N12O9
Molar mass	788.908 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES OC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CN)C(C)C)CO)Cc1c[NH]c2ccccc21)CCCCN)CCCNC(N)=N;
	InChI InChI=1S/C35H55N11O9/c1-18(2)12-24(31(51)43-23(34(54)55)10-7-11-39-35(37)38)42-28(49)16-41-30(50)25(13-20-15-40-22-9-6-5-8-21(20)22)44-32(52)26(17-47)45-33(53)29(19(3)4)46-27(48)14-36/h5-6,8-9,15,18-19,23-26,29,40,47H,7,10-14,16-17,36H2,1-4H3,(H,41,50)(H,42,49)(H,43,51)(H,44,52)(H,45,53)(H,46,48)(H,54,55)(H4,37,38,39)/t23-,24-,25-,26-,29-/m0/s1; Key:CMNBQRXBBJQIOA-YIHYGEMESA-N;

PE 22-28 is a heptapeptide with the sequence GVSWGLR or Gly–Val–Ser–Trp–Gly–Leu–Arg. It is a fragment of the endogenous TREK-1 antagonist spadin, and is the smallest fragment identified which shows similar TREK-1 inhibitory activity to spadin itself. It has been investigated as a potential antidepressant.^[1]

References

^ Djillani A, Pietri M, Moreno S, Heurteaux C, Mazella J, Borsotto M (2017). "Shortened Spadin Analogs Display Better TREK-1 Inhibition, In Vivo Stability and Antidepressant Activity". Frontiers in Pharmacology. 8 643. doi:10.3389/fphar.2017.00643. PMC 5601071. PMID 28955242.

[1] Djillani A, Pietri M, Moreno S, Heurteaux C, Mazella J, Borsotto M (2017). "Shortened Spadin Analogs Display Better TREK-1 Inhibition, In Vivo Stability and Antidepressant Activity". Frontiers in Pharmacology. 8 643. doi:10.3389/fphar.2017.00643. PMC 5601071. PMID 28955242.

[1]

See also

References