Anthraquinone-peptides as inhibitors of AP-1 transcription factor.
Peptide-1-[N-[2-succinamidylethyl]amino]anthraquinones containing five seven amino acid residues including the KCR motif important in AP-1 protein binding to DNA have been synthesised as potential transcription factor inhibitors. These anthraquinone-peptides showed DNA intercalative binding and inhibition of AP-1 protein binding to its DNA consensus sequence.
Ijaz
T
T
School of Pharmacy & Pharmaceutical Sciences, De Montfort University, UK.
Tran
P
P
Ruparelia
K C
KC
Teesdale-Spittle
P H
PH
Orr
S
S
Patterson
L H
LH
D020816:Amino Acid Motifs; D000880:Anthraquinones / Q000138:chemical synthesis / Q000494:pharmacology*; D001665:Binding Sites; D020650:Combinatorial Chemistry Techniques; D016384:Consensus Sequence; D004247:DNA / Q000378:metabolism; D004586:Electrophoresis; D006801:Humans; D007364:Intercalating Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D010446:Peptide Fragments / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology*; D011485:Protein Binding / Q000187:drug effects; D013329:Structure-Activity Relationship; D013696:Temperature; D018808:Transcription Factor AP-1 / Q000037:antagonists & inhibitors*
D000880:Anthraquinones; D007364:Intercalating Agents; D010446:Peptide Fragments; D018808:Transcription Factor AP-1; D004247:DNA