Highly Selective Binding and Inhibition of Pyr-His-Pro-NH2 (TRH) Function using a Polypyridinyl Macrocyclic Receptor with an Amphiphilic Cavity.
Chemistry
; 26(43): 9466-9470, 2020 Aug 03.
Article
em En
| MEDLINE
| ID: mdl-32259330
ABSTRACT
Macrocycle, cyclo[4] [(1,3-(4,6)-dimethylbezene)[4](2,6-(3,5)-dimethylpyridine (B4P4), shows highly selective binding affinity with protirelin (Pyr-His-Pro-NH2 ; TRH) among the tested 26 drug or drug adductive substrates. The stable complexation in a 11 manner was fully characterized in solution, gas phase, and solid state study. Furthermore, B4P4 acts as an efficient TRH inhibitor even at [macrocycle][drug] <1300, both in membrane transport and cellar incubation. The current work provides an unprecedented strategy for macrocycles to be efficiently used in drug target therapy.
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Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Piridinas
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Hormônio Liberador de Tireotropina
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Dipeptídeos
Idioma:
En
Ano de publicação:
2020
Tipo de documento:
Article