“MG132”的意思、由来-开放百科全书

词条

MG132

释义

References

{{Use dmy dates|date=July 2013}}{{more footnotes|date=November 2015}}{{Chembox
| Verifiedfields = changed
| Watchedfields = changed
| verifiedrevid = 446613982
| ImageFile = MG132.svg
| ImageSize = 250px
| IUPACName = Benzyl N-[(2S)-4-methyl-1-[[(2S)-4-methyl-1-[[(2S)-4-methyl-1-oxopentan-2-yl]amino]-1-oxopentan-2-yl]amino]-1-oxopentan-2-yl]carbamate
| OtherNames = N-Benzyloxycarbonyl-L-leucyl-L-leucyl-L-leucinal
Z-Leu-Leu-Leu-al
| Section1 = {{Chembox Identifiers
| CASNo_Ref = {{cascite|correct|??}}
| CASNo = 133407-82-6
| PubChem = 462382
| ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}}
| ChemSpiderID = 406728
| SMILES = CC(C)C[C@@H](C=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)OCc1ccccc1
| StdInChI_Ref = {{stdinchicite|changed|chemspider}}
| StdInChI = 1S/C26H41N3O5/c1-17(2)12-21(15-30)27-24(31)22(13-18(3)4)28-25(32)23(14-19(5)6)29-26(33)34-16-20-10-8-7-9-11-20/h7-11,15,17-19,21-23H,12-14,16H2,1-6H3,(H,27,31)(H,28,32)(H,29,33)/t21-,22-,23-/m0/s1
| StdInChIKey_Ref = {{stdinchicite|changed|chemspider}}
| StdInChIKey = TZYWCYJVHRLUCT-VABKMULXSA-N}}
| Section2 = {{Chembox Properties
| C=26 | H=41 | N=3 | O=5
| Appearance = White solid
| SolubleOther = 100 mM in EtOH and DMSO}}
}}

MG132 is a potent, reversible, and cell-permeable proteasome inhibitor ^[1] (K_i = 4 nM). It belongs to the class of synthetic peptide aldehydes ^[2]. It reduces the degradation of ubiquitin-conjugated proteins in mammalian cells and permeable strains of yeast by the 26S complex without affecting its ATPase or isopeptidase activities. MG132 activates c-Jun N-terminal kinase (JNK1), which initiates apoptosis. MG132 also inhibits NF-κB activation with an IC₅₀ of 3 µM and prevents β-secretase cleavage.

References

1. ^{{cite journal | vauthors = Hayashi M, Saito Y, Kawashima S | title = Calpain activation is essential for membrane fusion of erythrocytes in the presence of exogenous Ca2+. | journal = Biochem Biophys Res Commun | volume = 182 | issue = 2 | pages = 939-946 | date = Jan 31, 1992 | pmid = 1734892}}
2. ^{{cite journal | vauthors = Ito A, Takahashi R, Muira C, Baba Y | title = Synthetic Study of Peptide Aldehydes | journal = Chemical and Pharmaceutical Bulletin | volume = 12 | issue = 23 | pages = 2106-3113 | date = 1975 | pmid = 8987871 | doi = 10.1248/cpb.37.3229 }}

{{cite web | url = http://www.merck-chemicals.com/germany/life-science-research/mg-132/EMD_BIO-474790/p_w_.b.s1LzxMAAAEW02EfVhTm | publisher = merck-chemicals.com | title = MG-132}}

4 : Peptides|Proteasome inhibitors|Aldehydes|Carbamates

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