ADP-ribosylation of rho proteins is inhibited by melittin, mast cell degranulating peptide and compound 48/80.
The amphiphilic agents melittin, mast cell degranulating peptide and compound 48/80 inhibit the ADP-ribosylation of the small GTP-binding proteins rho by Clostridium botulinum exoenzyme C3. Half-maximal and maximal inhibition (greater than 90%) of ADP-ribosylation occurred at about 8 and 25 micrograms/ml for compound 48/80, at 10 and 45 microM for mast cell degranulating peptide and at 15 and 50 microM for melittin, respectively. In addition, these compounds increase the steady state GTP hydrolysis and the association and dissociation rate of GTP-binding of rho proteins through an increase of GDP/GTP exchange. The data suggest that the amphiphilic agents tested interact with small GTP-binding proteins of the rho protein family.
Koch
G
G
Institut für Pharmakologie und Toxikologie, Universität des Saarlandes, Homburg/Saar, Germany.
Habermann
B
B
Mohr
C
C
Just
I
I
Aktories
K
K
D036002:ADP Ribose Transferases / Q000378:metabolism; D000246:Adenosine Diphosphate Ribose / Q000378:metabolism*; D000818:Animals; D001905:Botulinum Toxins; D001921:Brain / Q000378:metabolism; D019204:GTP-Binding Proteins / Q000378:metabolism*; D006153:Guanosine Diphosphate / Q000378:metabolism; D006160:Guanosine Triphosphate / Q000378:metabolism; D008555:Melitten / Q000494:pharmacology*; D010455:Peptides / Q000494:pharmacology*; D013552:Swine; D003189:p-Methoxy-N-methylphenethylamine / Q000494:pharmacology*
D010455:Peptides; D006153:Guanosine Diphosphate; D008555:Melitten; D000246:Adenosine Diphosphate Ribose; C008331:mast cell degranulating peptide; D003189:p-Methoxy-N-methylphenethylamine; D006160:Guanosine Triphosphate; D036002:ADP Ribose Transferases; C063007:exoenzyme C3, Clostridium botulinum; D001905:Botulinum Toxins; D019204:GTP-Binding Proteins