Protein Information

Name Leu 2
Synonyms 1B4; Leu2; BCMSUN; DLB 2; DLB2; DLEU 2; DLEU2; Deleted in lymphocytic leukemia 2…

Compound Information

Name OCH
CAS 2,3,4,4,5,5,6,6-octachloro-2-cyclohexen-1-one

Reference List

PubMed Abstract RScore(About this table)
12162713 Wu J, Yoon SH, Wu WM, Bodor N: Synthesis and biological evaluations of brain-targeted chemical delivery systems of [Nva2]-TRH. J Pharm Pharmacol. 2002 Jul;54(7):945-50.

The fully packaged DHT-Pro-Pro-Gln-Nva-Pro-Gly-OCh produced robust antagonism, reducing sleeping time from 89 min to 48 min, similar to the Leu2-analogue (49 min).
82(1,1,1,2) Details
10882017 Yoon SH, Wu J, Wu WM, Prokai L, Bodor N: Brain-targeted chemical delivery of [Leu2, Pip3]-TRH: synthesis and biological evaluation. Bioorg Med Chem. 2000 May;8(5):1059-63.

Sequential metabolism of the obtained 'packaged' chemical delivery system, (CDS), DHT-Pro-Pro-Gln-Leu-Pip-OCh, should yield a 'locked-in' precursor following the oxidative conversion of the dihydrotrigonellyl (DHT) to the trigonellyl (T+) moiety, followed by removal of the cholesteryl function and cleavage of the T+-Pro-Pro by prolyl endopeptidase.
4(0,0,0,4) Details
11972752 Ouyang H, Vander Velde DG, Borchardt RT, Siahaan TJ: Synthesis and conformational analysis of a coumarinic acid-based cyclic prodrug of an opioid peptide with modified sensitivity to esterase-catalyzed bioconversion. J Pept Res. 2002 Apr;59(4):183-95.


Briefly, phenacyl-protected 3-(2-hydroxyphenyl)-propynoic acid 17 was coupled with Boc-d-Leu-OCH (2) I 5 to give the intermediate 18, which was further elaborated and conjugated with tetrapeptide 4 to give linear precursor 2.
1(0,0,0,1) Details