Large-scale screening of i-motif binding compounds in the silkworm, Bombyx mori.
Biochem Biophys Res Commun
; 589: 9-15, 2022 01 22.
Article
in En
| MEDLINE
| ID: mdl-34883288
ABSTRACT
DNA secondary structure i-motif involves in gene transcription and considered as a novel target for cancer gene therapy. I-motif-binding compounds can either stabilize or destroy the structure, resulting in change in target gene transcription. In this study, a large-scale screening of binding compounds was conducted using the i-motif structure of BmPOUM2, a transcription factor in silkworm, Bombyx mori. Surface plasmon resonance imaging (SPRi) high-throughput binding screening of 3642 compounds found 60 compounds with an binding affinity Kd of 10-7-10-6 M. SPRi and circular dichroism (CD) double screening demonstrated that the BmPOUM2 i-motif structure bound the compounds IF1, IF3, IF4, IF6 and IF7 with Kd of 10-7 M, and the compounds IF2 and tetrakis (4-N-methylpyridyl) porphine (TMPyP4) with a Kd of 10-8 M. Interestingly, IF2, IF3, IF4, IF6 and IF7 promoted the binding of the i-motif-binding protein BmILF with the i-motif structure, whereas TMPyP4 inhibited the binding. This study provided a list of compounds that have potential applications in functional analysis of i-motif structure and in pesticide and drug development through gene transcription regulation by i-motif structure.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Bombyx
/
High-Throughput Screening Assays
/
Nucleotide Motifs
Type of study:
Diagnostic_studies
/
Screening_studies
Limits:
Animals
Language:
En
Journal:
Biochem Biophys Res Commun
Year:
2022
Type:
Article
Affiliation country:
China