Inhibition of ADP-ribosylation of histone H1 by analogs of diadenosine 5',5'''-p1,p4-tetraphosphate

The effects of analogs of diadenosine 5',5'''-p1,p4-tetraphosphate (Ap4A) were examined on the ADP-ribosylation reaction of histone H1 catalysed by purified bovine thymus poly(ADP-ribose)transferase. Among the compounds tested, epsilon Ap4A and ApCH2pppA were shown to be the most...

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Veröffentlicht in:	Molecular and cellular biochemistry 1987-03, Vol.74 (1), p.17-20
Hauptverfasser:	Suzuki, H, Tanaka, Y, Buonamassa, D T, Farina, B, Leone, E
Format:	Artikel
Sprache:	eng
Schlagworte:	Adenine Nucleotides - pharmacology Adenosine Diphosphate Ribose - metabolism Animals Cattle Dinucleoside Phosphates Histones - metabolism Kinetics Poly(ADP-ribose) Polymerase Inhibitors Structure-Activity Relationship Thymus Gland - enzymology
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Zusammenfassung:	The effects of analogs of diadenosine 5',5'''-p1,p4-tetraphosphate (Ap4A) were examined on the ADP-ribosylation reaction of histone H1 catalysed by purified bovine thymus poly(ADP-ribose)transferase. Among the compounds tested, epsilon Ap4A and ApCH2pppA were shown to be the most efficient inhibitors of the enzyme. From kinetic studies of their action, it appears that epsilon Ap4A and ApCH2pppA might be 'mixed type' inhibitors.
ISSN:	0300-8177 1573-4919
DOI:	10.1007/BF00221908