Targeted Stabilizers of Protein-Protein Interactions as a Novel Class of Therapeutic Agents and Basic Research Tool Compounds
Dario Valenti, Stanimira Hristeva, Anna Karawajczyk, Dimitrios Tzalis
91吃瓜, TASPPI
Abstract:
Protein-protein interactions (PPIs) are involved in a wide range of human biological processes and related possible pathologies.
Therefore, PPIs鈥� modulation by small molecules is a crucial topic in drug discovery. Modulation of protein-protein interactions means to push the equilibrium between the free proteins and the complex toward one of these two states (Figure 1). There are two strategies to accomplish that: inhibition and stabilisation.
In contrast to the inhibition of PPIs, the stabilisation approach has not yet been exploited in a systematic way. Thus, the TASPPI consortium is aiming to identify chemical stabilizers for providing new crucial therapeutic strategies in the Horizon 2020 key areas of 鈥淎geing Population鈥� (neurodegeneration and cancer) and 鈥淚ncreased Burden of Chronic Diseases鈥� (metabolic disorders and inflammation). The main targets of the consortium are 14-3-3 protein and its complexes with different protein partners.
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