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Org Biomol Chem ; 18(5): 920-930, 2020 02 07.
Artículo en Inglés | MEDLINE | ID: mdl-31922164

RESUMEN

By choosing pyridostatin (PDS) with high thermal stabilization towards mixed-type G-quadruplexes as the monomer in dimers, three novel polyether-tethered PDS dimers (1a-c) were first synthesized and their interaction with human telomere G-quadruplex dimers (G2T1) was studied. Through the regulation of the linker length in PDS dimers, the dimer with a medium-length polyether linker (1b) showed higher binding selectivity and thermal stabilization (ΔTm = 29.5 °C) towards antiparallel G2T1 over G-quadruplex monomers (G1). Furthermore, the dimer with the longest-length polyether linker (1c) showed higher binding selectivity and thermal stabilization towards mixed-type G2T1 over mixed-type G1, c-kit 1, c-kit 2, c-myc and ds DNA. This work provides new insights into the development of G2T1 binders, especially mixed-type G2T1 binders, which could be promoted by a polymer formed with a mixed-type G-quadruplex binder. In addition, dimer 1c exhibited stronger telomerase inhibition than dimers 1a and 1b.


Asunto(s)
Aminoquinolinas/química , Dimerización , G-Cuádruplex , Ácidos Picolínicos/química , Telómero/metabolismo , Aminoquinolinas/síntesis química , Calorimetría , Dicroismo Circular , Inhibidores Enzimáticos/farmacología , Humanos , Cinética , Ácidos Picolínicos/síntesis química , Telomerasa/antagonistas & inhibidores , Termodinámica
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