IAM   02674
INSTITUTO ARGENTINO DE MATEMATICA ALBERTO CALDERON
Unidad Ejecutora - UE
artículos
Título:
Drug leads for interactive protein targets with unknown structure
Autor/es:
ARIEL FERNANDEZ; RIDGWAY SCOTT
Revista:
DRUG DISCOVERY TODAY
Editorial:
ELSEVIER SCI LTD
Referencias:
Lugar: Amsterdam; Año: 2016 vol. 21 p. 531 - 535
ISSN:
1359-6446
Resumen:
The disruption of protein?protein interfaces (PPIs) remains a challenge in drug discovery. The problem becomes daunting when the structure of the target protein is unknown and is even further complicated when the interface is susceptible to disruptive phosphorylation. Based solely on protein sequence and information about phosphorylation-susceptible sites within the PPI, a new technology has been developed to identify drug leads to inhibit protein associations. Here we reveal this technology and contrast it with current structure-based technologies for the generation of drug leads.The novel technology is illustrated by a patented invention to treat heart failure. The success of this technology shows that it is possible to generate drug leads in the absence of target structure.