Biomaterial Database

Phosphatidylinositol kinase of bovine adrenal chromaffin granules. Modulation by hydrophilic and amphiphilic cations. 1988

E S Husebye, and T Flatmark

Department of Biochemistry, University of Bergen, Norway.

The effects of hydrophilic and amphiphilic cations on the activity of phosphatidylinositol (PI) kinase (EC 2.7.1.67) of chromaffin granule ghosts were investigated. The cations studied can be divided into two groups, i.e. (i) compounds with a biphasic response (stimulation and inhibition), and (ii) those with a selective stimulatory effect on the enzyme activity. The cationic amphiphile trifluoperazine belongs to the first group, and stimulated the enzyme activity, maximal at 80 microM (2-fold), with a progressive inhibition at higher concentrations. This biphasic response was shared by a number of structurally related cationic amphiphiles, i.e. the tricyclic antidepressants, imipramine and desipramine, the phenothiazine, chlorpromazine, the miconazole derivative, calmidazolium, the beta-adrenergic agonist, propranolol, compound 48/80, as well as by the hydrophilic cations neomycin and poly-L-lysine. On the other hand, a pure stimulatory effect was observed with the amphiphilic polypeptide mastoparan and the polycationic compound spermidine, whereas ACTH1-39 and ACTH1-24 (peptides structurally related to mastoparan) revealed a slight inhibitory effect. We conclude that all the cations tested including Mg2+, stimulate PI kinase activity rather unspecifically by binding of the positively charged groups to a membrane component, probably the PI kinase itself. This site is different from that mediating the specific inhibition by calcium (Husebye ES and Flatmark T, Biochim Biophys Acta 968: 261-265, 1988). The inhibitory effect of cationic amphiphiles is correlated to their lipid solubility, and represents a perturbation of the membrane structure, but not a solubilization of enzyme or phosphoinositide from the membrane. The inhibitory effect of hydrophilic cations is due to complexation of ATP.

UI	MeSH Term	Description	Entries
D008274	Magnesium	A metallic element that has the atomic symbol Mg, atomic number 12, and atomic weight 24.31. It is important for the activity of many enzymes, especially those involved in OXIDATIVE PHOSPHORYLATION.
D009355	Neomycin	Aminoglycoside antibiotic complex produced by Streptomyces fradiae. It is composed of neomycins A, B, and C, and acts by inhibiting translation during protein synthesis.	Fradiomycin Sulfate,Neomycin Palmitate,Neomycin Sulfate
D010455	Peptides	Members of the class of compounds composed of AMINO ACIDS joined together by peptide bonds between adjacent amino acids into linear, branched or cyclical structures. OLIGOPEPTIDES are composed of approximately 2-12 amino acids. Polypeptides are composed of approximately 13 or more amino acids. PROTEINS are considered to be larger versions of peptides that can form into complex structures such as ENZYMES and RECEPTORS.	Peptide,Polypeptide,Polypeptides
D010716	Phosphatidylinositols	Derivatives of phosphatidic acids in which the phosphoric acid is bound in ester linkage to the hexahydroxy alcohol, myo-inositol. Complete hydrolysis yields 1 mole of glycerol, phosphoric acid, myo-inositol, and 2 moles of fatty acids.	Inositide Phospholipid,Inositol Phosphoglyceride,Inositol Phosphoglycerides,Inositol Phospholipid,Phosphoinositide,Phosphoinositides,PtdIns,Inositide Phospholipids,Inositol Phospholipids,Phosphatidyl Inositol,Phosphatidylinositol,Inositol, Phosphatidyl,Phosphoglyceride, Inositol,Phosphoglycerides, Inositol,Phospholipid, Inositide,Phospholipid, Inositol,Phospholipids, Inositide,Phospholipids, Inositol
D010770	Phosphotransferases	A rather large group of enzymes comprising not only those transferring phosphate but also diphosphate, nucleotidyl residues, and others. These have also been subdivided according to the acceptor group. (From Enzyme Nomenclature, 1992) EC 2.7.	Kinases,Phosphotransferase,Phosphotransferases, ATP,Transphosphorylase,Transphosphorylases,Kinase,ATP Phosphotransferases
D011073	Polyamines	Amine compounds that consist of carbon chains or rings containing two or more primary amino groups.	Polyamine
D011107	Polylysine	A peptide which is a homopolymer of lysine.	Epsilon-Polylysine,Poly-(Alpha-L-Lysine),Epsilon Polylysine
D002412	Cations	Positively charged atoms, radicals or groups of atoms which travel to the cathode or negative pole during electrolysis.	Cation
D002417	Cattle	Domesticated bovine animals of the genus Bos, usually kept on a farm or ranch and used for the production of meat or dairy products or for heavy labor.	Beef Cow,Bos grunniens,Bos indicus,Bos indicus Cattle,Bos taurus,Cow,Cow, Domestic,Dairy Cow,Holstein Cow,Indicine Cattle,Taurine Cattle,Taurus Cattle,Yak,Zebu,Beef Cows,Bos indicus Cattles,Cattle, Bos indicus,Cattle, Indicine,Cattle, Taurine,Cattle, Taurus,Cattles, Bos indicus,Cattles, Indicine,Cattles, Taurine,Cattles, Taurus,Cow, Beef,Cow, Dairy,Cow, Holstein,Cows,Dairy Cows,Domestic Cow,Domestic Cows,Indicine Cattles,Taurine Cattles,Taurus Cattles,Yaks,Zebus
D002837	Chromaffin Granules	Organelles in CHROMAFFIN CELLS located in the adrenal glands and various other organs. These granules are the site of the synthesis, storage, metabolism, and secretion of EPINEPHRINE and NOREPINEPHRINE.	Chromaffin Granule,Granule, Chromaffin