PMID- 28567459
OWN - NLM
STAT- MEDLINE
DCOM- 20180326
LR  - 20181113
IS  - 1477-0539 (Electronic)
IS  - 1477-0520 (Print)
IS  - 1477-0520 (Linking)
VI  - 15
IP  - 27
DP  - 2017 Jul 21
TI  - Identification of new DNA i-motif binding ligands through a fluorescent 
      intercalator displacement assay.
PG  - 5669-5673
LID - 10.1039/c7ob00710h [doi]
AB  - i-Motifs are quadruplex DNA structures formed from sequences rich in cytosine and 
      held together by intercalated, hemi-protonated cytosine-cytosine base pairs. 
      These sequences are prevalent in gene promoter regions and may play a role in 
      gene transcription. Targeting these structures with ligands could provide a novel 
      way to target genetic disease but there are very few ligands which have been 
      shown to interact with i-motif DNA. Fluorescent intercalator displacement (FID) 
      assays are a simple way to screen ligands against DNA secondary structures. Here 
      we characterise how thiazole orange interacts with i-motif DNA and assess its 
      ability for use in a FID assay. Additionally, we report FID-based ligand 
      screening using thiazole orange against the i-motif forming sequence from the 
      human telomere to reveal new i-motif binding compounds which have the potential 
      for further development.
FAU - Sheng, Qiran
AU  - Sheng Q
AD  - School of Pharmacy, University of East Anglia, Norwich Research Park, Norwich, 
      NR4 7TJ, UK. z.waller@uea.ac.uk.
FAU - Neaverson, Joseph C
AU  - Neaverson JC
AD  - School of Pharmacy, University of East Anglia, Norwich Research Park, Norwich, 
      NR4 7TJ, UK. z.waller@uea.ac.uk.
FAU - Mahmoud, Tasnim
AU  - Mahmoud T
AD  - School of Pharmacy, University of East Anglia, Norwich Research Park, Norwich, 
      NR4 7TJ, UK. z.waller@uea.ac.uk.
FAU - Stevenson, Clare E M
AU  - Stevenson CEM
AD  - Department of Biological Chemistry, John Innes Centre, Norwich Research Park, 
      Norwich, NR4 7UH, UK.
FAU - Matthews, Susan E
AU  - Matthews SE
AUID- ORCID: 0000-0001-8821-0851
AD  - School of Pharmacy, University of East Anglia, Norwich Research Park, Norwich, 
      NR4 7TJ, UK. z.waller@uea.ac.uk.
FAU - Waller, Zoe A E
AU  - Waller ZAE
AUID- ORCID: 0000-0001-8538-0484
AD  - School of Pharmacy, University of East Anglia, Norwich Research Park, Norwich, 
      NR4 7TJ, UK. z.waller@uea.ac.uk and Centre for Molecular and Structural 
      Biochemistry, University of East Anglia, Norwich Research Park, Norwich, NR4 7TJ, 
      UK.
LA  - eng
PT  - Journal Article
DEP - 20170601
PL  - England
TA  - Org Biomol Chem
JT  - Organic & biomolecular chemistry
JID - 101154995
RN  - 0 (Fluorescent Dyes)
RN  - 0 (Intercalating Agents)
RN  - 0 (Ligands)
RN  - 9007-49-2 (DNA)
SB  - IM
MH  - Binding Sites
MH  - DNA/*chemistry
MH  - Fluorescent Dyes/*chemistry
MH  - Intercalating Agents/*chemistry
MH  - Ligands
MH  - Molecular Structure
MH  - Nucleotide Motifs
PMC - PMC5708337
EDAT- 2017/06/02 06:00
MHDA- 2018/03/27 06:00
PMCR- 2017/06/01
CRDT- 2017/06/02 06:00
PHST- 2017/06/02 06:00 [pubmed]
PHST- 2018/03/27 06:00 [medline]
PHST- 2017/06/02 06:00 [entrez]
PHST- 2017/06/01 00:00 [pmc-release]
AID - c7ob00710h [pii]
AID - 10.1039/c7ob00710h [doi]
PST - ppublish
SO  - Org Biomol Chem. 2017 Jul 21;15(27):5669-5673. doi: 10.1039/c7ob00710h. Epub 2017 
      Jun 1.