A QUANTITATIVE ASSAY TO MEASURE THE RELATIVE DNA-BINDING AFFINITY OF PYRROLO[2,1-C][1,4]BENZODIAZEPINE (PBD) ANTITUMOR ANTIBIOTICS BASED ONTHE INHIBITION OF RESTRICTION-ENDONUCLEASE BAMHI

Authors
PUVVADA MS HARTLEY JA JENKINS TC THURSTON DE
Citation
Ms. Puvvada et al., A QUANTITATIVE ASSAY TO MEASURE THE RELATIVE DNA-BINDING AFFINITY OF PYRROLO[2,1-C][1,4]BENZODIAZEPINE (PBD) ANTITUMOR ANTIBIOTICS BASED ONTHE INHIBITION OF RESTRICTION-ENDONUCLEASE BAMHI, Nucleic acids research, 21(16), 1993, pp. 3671-3675
Citations number
16
Categorie Soggetti
Biology
Journal title
Nucleic acids research → ACNP
ISSN journal
03051048
Volume
21
Issue
16
Year of publication
1993
Pages
3671 - 3675
Database
ISI
SICI code
0305-1048(1993)21:16<3671:AQATMT>2.0.ZU;2-K
Abstract
An assay has been developed (restriction endonuclease digestion assay - RED100) based on inhibition of the restriction endonuclease BamHI th at is capable of quantitative evaluation of the relative DNA-binding a ffinity of pyrrolo[2,1-c][1,4]benzodiazepine (PBD) antitumour antibiot ics. This method provides comparable results to those obtained from th ermal denaturation and ethidium bromide displacement assays but is muc h more sensitive, discriminating between molecules of similar structur e such as DC-81, iso-DC-81 and neothramycin. The results reveal a tren d between relative DNA-binding affinity and in vitro cytotoxicity for the PBDs in two tumour cell lines studied.