Stabilization of protein-protein interactions by small molecules.

Giordanetto F, Schäfer A, Ottmann C.

Drug Discovery Today. 2014 Aug 28. pii: S1359-6446(14)00332-8. doi: 10.1016/j.drudis.2014.08.005.

Abstract:
Protein–protein interactions (PPIs) are implicated in every disease and mastering the ability to influence PPIs with small molecules would considerably enlarge the druggable genome. Whereas inhibition of PPIs has repeatedly been shown to work successfully, targeted stabilization of PPIs is underrepresented in the literature. This is all the more surprising because natural products like FK506, rapamycin, brefeldin, forskolin and fusicoccin confer their physiological activity by stabilizing specific PPIs. However, recently a number of very interesting synthetic molecules have been reported from drug discovery projects that indeed achieve their desired activities by stabilizing either homo- or hetero-oligomeric complexes of their target proteins.

Want to know more about this publication?

Contact our scientists

medicinal chemistry

Drug Discovery

We are running our own state-of-the-art Drug Discovery Chemistry facilities in Germany with the option for process research chemistry, upscaling, kilolab production…

performance chemicals

Material Science

We create performance chemicals to enhance new materials, plastics, coatings, dyes & inks, cosmetics, flavors and many more research and industrial applications…

startseite-firstbanner

Looks interesting?

As a leading contract research organization in discovery chemistry and custom synthesis, Taros provides comprehensive solutions to meet our clients’ needs from diverse branches and applications

Our experienced chemists practice a pragmatic culture and customer-centric approach in order to exceed project expectations, despite challenges, bridging very narrow timelines. They are trained to consider economic, safety and ecological boundaries and conditions laid out for all stages of the project, starting from the development of synthetic routes to…