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The crystal and molecular structure of the anticancer drug actinomycin D—some explanations for its unusual properties
Author(s) -
Ginell Stephan,
Lessinger Leslie,
Berman Helen M.
Publication year - 1988
Publication title -
biopolymers
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.556
H-Index - 125
eISSN - 1097-0282
pISSN - 0006-3525
DOI - 10.1002/bip.360270511
Subject(s) - chemistry , molecule , dimer , hydrogen bond , stereochemistry , ring (chemistry) , crystal structure , crystallography , dna , peptide , torsion (gastropod) , netropsin , anticancer drug , drug , biochemistry , organic chemistry , minor groove , medicine , surgery , psychology , psychiatry
The crystal structure of the antitumor antibiotic actinomycin D has been determined by the methods of x‐ray crystallography. There are three independent molecules in the asymmetric unit. Two of the molecules form a hydrogen‐bonded dimer. The peptides within all three molecules have very similar conformations. The greatest conformational variability in the drug molecules occurs in the torsion angles of the bonds connecting the phenoxazone ring to the peptide rings. The results of this analysis has allowed us to explain the unusual physical properties of ActD as well as to provide an explanation for the thermodynamics of its interactions with DNA.