Design, Synthesis and Evaluation of AdSS Bisubstrate Inhibitors.
ChemMedChem
; 15(23): 2269-2272, 2020 12 03.
Article
de En
| MEDLINE
| ID: mdl-32779344
ABSTRACT
Many cancers lack the expression of methylthioadenosine phosphorylase (MTAP). These cancers require adenylosuccinate synthetase (AdSS) for nucleic acid synthesis. By inhibiting adenylosuccinate synthetase, we potentially have a new therapeutic agent. Bisubstrate inhibitors were synthesized and evaluated against purified AdSS. The best activity was obtained with adenosine bearing a four-carbon linker that connects the N-formyl-N-hydroxy moiety to the 6-position of the purine nucleoside.
Mots clés
Texte intégral:
1
Collection:
01-internacional
Base de données:
MEDLINE
Sujet principal:
Nucléoside purique
/
Conception de médicament
/
Antienzymes
Limites:
Humans
Langue:
En
Journal:
ChemMedChem
Sujet du journal:
FARMACOLOGIA
/
QUIMICA
Année:
2020
Type de document:
Article
Pays d'affiliation:
États-Unis d'Amérique