First Demonstration of Positive Allosteric-like Modulation at the Human Wild Type Translocator Protein (TSPO).
J Med Chem
; 58(21): 8743-9, 2015 Nov 12.
Article
en En
| MEDLINE
| ID: mdl-26461041
ABSTRACT
We show that changing the number and position of nitrogen atoms in the heteroatomic core of a pyrazolopyrimidine acetamide is sufficient to induce complex binding to wild type human TSPO. Only compounds with this complex binding profile lacked intrinsic effect on glioblastoma proliferation but positively modulated the antiproliferative effects of a synthetic TSPO ligand. To the best of our knowledge this is the first demonstration of allosteric-like interaction at the wild type human TSPO.
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Pirimidinas
/
Receptores de GABA
/
Proliferación Celular
/
Acetamidas
/
Antineoplásicos
Límite:
Humans
Idioma:
En
Revista:
J Med Chem
Asunto de la revista:
QUIMICA
Año:
2015
Tipo del documento:
Article