4-甲基环己胺

Amino Acids 42(2-3) , 619-26, (2012)

Polyamines spermidine and spermine are known to be required for mammalian cell proliferation and for embryonic development. Alpha-difluoromethylornithine (DFMO), an inhibitor of ornithine decarboxylase (ODC) a limiting enzyme of polyamine biosynthesis, deplet...

J. Med. Chem. 51 , 2777-86, (2008)

Seven novel binders, binding in the active site of Plasmodium falciparum spermidine synthase, were identified by structure-based virtual screening. The binding of these compounds was experimentally verified by NMR techniques. Spermidine synthase, an enzyme in...

Biochem. Pharmacol. 45(9) , 1897-903, (1993)

Several inhibitors of aminopropyltransferases, developed recently in this laboratory, were tested for their specificity by measuring their effects on six enzyme activities related to polyamine biosynthesis and interconversion. Two of them, trans-4-methylcyclo...

Cancer Prev. Res. (Phila.) 3(2) , 140-7, (2010)

The oncogenic transcription factor c-Myc (Myc) is frequently overexpressed in human cancers. Myc is known to induce or repress a large set of genes involved in cell growth and proliferation, explaining the selection for mutations in cancer that deregulate Myc...

J. Biochem. 117(2) , 339-45, (1995)

The effects of a potent spermidine synthase inhibitor, trans-4-methylcyclohexylamine (4MCHA), and a spermine synthase inhibitor, N-(3-aminopropyl)cyclohexylamine (APCHA), on polyamine biosynthesis and cell growth have been studied in rat hepatoma cells (HTC c...

J. Biochem. 117(4) , 824-9, (1995)

The inhibitory effect on cell growth of a combination of alpha-difluoromethylornithine (DFMO) and an inhibitor of aminopropyl transferase was examined. N-(3-aminopropyl)cyclohexylamine (APCHA) and trans-4-methylcyclohexylamine (4MCHA) were used as inhibitors ...

Biol. Pharm. Bull. 30(10) , 1943-6, (2007)

A sensitive method for the determination of polyamines in mammalian cells was described using electrospray ionization and time-of-flight mass spectrometer. This method was 50-fold more sensitive than the previous method using ionspray ionization and quadrupol...

J. Chromatogr. B. Analyt. Technol. Biomed. Life Sci. 845(1) , 80-3, (2007)

An assay for spermidine synthase (SPDS) activity in rat liver has been developed using micellar electrokinetic chromatography (MEKC) with laser-induced fluorescence (LIF) detection to enable the discovery of SPDS inhibitors. The assay was established by estim...

Biol. Pharm. Bull. 27(9) , 1327-32, (2004)

Homology modeling and inhibitory studies using substrate analogs were undertaken to construct a possible three-dimensional structure, including the putrescine-binding site, of rat spermidine synthase based on its primary sequence. Of the ten cysteine residues...

Biol. Pharm. Bull. 28(4) , 569-73, (2005)

In rat tissues, a decrease in spermidine, accompanied by an increase in spermine was induced by the oral administration (once daily for either 1 week or 1 month) of trans-4-methylcyclohexylamine (4MCHA), a spermidine synthase inhibitor. This is similar to the...