Clinical candidates modulating protein-protein interactions: The fragment-based experience

Dario Valenti, Stanimira Hristeva, Dimitrios Tzalis, and Christian Ottmann

Eur. J. Med. Chem., Apr. 2019, 167, pp 76-95,  DOI: 10.1016/j.ejmech.2019.01.084;

Protein-protein interactions (PPIs) cover a very wide range of biological functions and consequently have become one of the favourite targets for new therapeutic strategies. PPIs are strongly characterised by an intricate and dynamic network of surface interactions occurring between two or more proteins. Because of the complexity of these interactions, many strategies have been applied with the aim to find selective modulators for a specific protein-protein complex. During the last decade, fragment-based approaches have served many drug discovery programs with an impressive increment of contributions, gaining a remarkable role in PPIs modulators’ development. In this review, we detail the successful fragment-to-clinical candidate evolutions related to PPI modulation. An overview on the physico-chemical properties of both fragment hits and lead compounds will be presented together with a statistical analysis of their distribution.

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…


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…