TMC-95A, a reversible proteasome inhibitor, induces neurite outgrowth in PC12 cells

Masayuki Inoue; Haifeng Zhai; Hayato Sakazaki; Hidetomo Furuyama; Yoshiyasu Fukuyama; Masahiro Hirama

doi:10.1016/j.bmcl.2003.11.043

TMC-95A, a reversible proteasome inhibitor, induces neurite outgrowth in PC12 cells

Bioorg Med Chem Lett. 2004 Feb 9;14(3):663-5. doi: 10.1016/j.bmcl.2003.11.043.

Authors

Masayuki Inoue¹, Haifeng Zhai, Hayato Sakazaki, Hidetomo Furuyama, Yoshiyasu Fukuyama, Masahiro Hirama

Affiliation

¹ Department of Chemistry, Graduate School of Science, Tohoku University, Sendai 980-8578, Japan. [email protected]

PMID: 14741264
DOI: 10.1016/j.bmcl.2003.11.043

Abstract

TMC-95A has been characterized as a potent proteasome inhibitor that binds to enzymes non-covalently at low nanomolar concentrations. Herein, the neuritogenic activity of TMC-95A in PC12 rat pheochromocytoma cells is reported for the first time. TMC-95A induced a positive neurite initiation of PC12 cells at concentration ranging from 1 to 20 microM.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Ascomycota / chemistry*
Cysteine Endopeptidases / drug effects*
Molecular Structure
Multienzyme Complexes / drug effects*
Neurites / drug effects*
Neurites / physiology
PC12 Cells
Peptides, Cyclic / isolation & purification
Peptides, Cyclic / pharmacology*
Protease Inhibitors / isolation & purification
Protease Inhibitors / pharmacology*
Proteasome Endopeptidase Complex
Rats

Substances

Multienzyme Complexes
Peptides, Cyclic
Protease Inhibitors
TMC-95A
Cysteine Endopeptidases
Proteasome Endopeptidase Complex