Unknown

Dataset Information

0

Triostin a derived cyclopeptide as architectural template for the alignment of four recognition units.


ABSTRACT: The DNA bisintercalator triostin A is structurally based on a disulfide-bridged depsipeptide scaffold that provides preorganization of two quinoxaline units in 10.5 Å distance. Triostin A analogues are synthesized with nucleobase recognition units replacing the quinoxalines and containing two additional recognition units in between. Thus, four nucleobase recognition units are organized on a rigid template, well suited for DNA double strand interactions. The new tetra-nucleobase binders are synthesized as aza-TANDEM derivatives lacking the N-methylation of triostin A and based on a cyclopeptide backbone. Synthesis of two tetra-nucleobase aza-TANDEM derivatives is established, DNA interaction analyzed by microscale thermophoresis, cytotoxic activity studied and a nucleobase sequence dependent self-aggregation investigated by mass spectrometry.

PROVIDER: S-EPMC4232271 | BioStudies |

REPOSITORIES: biostudies

Similar Datasets

| S-EPMC3102191 | BioStudies
1998-01-01 | S-EPMC1219111 | BioStudies
1983-01-01 | S-EPMC1154398 | BioStudies
1978-01-01 | S-EPMC1185755 | BioStudies
1985-01-01 | S-EPMC1144661 | BioStudies
2009-01-01 | S-EPMC2733282 | BioStudies
| S-EPMC7199197 | BioStudies
| S-EPMC2631397 | BioStudies
| S-EPMC7057376 | BioStudies
| S-EPMC5934746 | BioStudies