Development of novel macrocyclic small molecules that target CTG trinucleotide repeats.
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ABSTRACT:
SUBMITTER: Serrano JF
PROVIDER: S-EPMC6592636 | biostudies-literature | 2019 Jul
REPOSITORIES: biostudies-literature
Publications
Development of novel macrocyclic small molecules that target CTG trinucleotide repeats.
Serrano Julio F JF Lee JuYeon J Daniel Curet L L Hagler Lauren D LD Bonson Sarah E SE Schuster Emma J EJ Zimmerman Steven C SC
Bioorganic & medicinal chemistry 20190514 13
We describe the molecular design, synthesis, and investigation of a series of acridine-triaminotriazine macrocycles that selectively bind to CTG trinucleotide repeats in DNA with minimal nonspecific binding. The limited conformational flexibility enforces the stacking of the triaminotriazine and acridine units. Isothermal titration calorimetry studies and Job plot analyses revealed that the ligands bound to d(CTG) mismatched sites. The acridine and triaminotriazine units were shown to intramolec ...[more]
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