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Protein-protein interaction inhibitors

Lookup NU author(s): Dr Ian HardcastleORCiD



This work is licensed under a Creative Commons Attribution-NonCommercial 4.0 International License (CC BY-NC 4.0).


The study of cellular mechanisms of cancer growth and survival has revealed a complex web of signalling pathways that produce the ‘hallmarks of cancer’. A number of critical cellular signalling nodes have been characterised from which many new drug targets have been proposed. A number of these nodes are regulated by protein-protein interactions, and so present attractive, if challenging, targets for drug discovery. Drug discovery efforts towards three PPI families have resulted in clinically investigated drugs: i.e. Bcl-2 family inhibitors, MDM2-p53 inhibitors and IAP inhibitors. The discovery and optimisation of these drug classes are detailed in this chapter.

Publication metadata

Author(s): Hardcastle IR

Editor(s): Bernstein, PR; Georg, GI; Keller, Th; Kobayashi, T; Lowe, JA; Meanwell, NA; Saxena, AK; Stilz, U; Supuran, CT; Zhang, A

Publication type: Book Chapter

Publication status: Published

Book Title: Topics in Medicinal Chemistry

Year: 2017

Pages: 1-35

Online publication date: 25/07/2017

Acceptance date: 30/06/2017

Publisher: Springer

Place Published: Berlin, Heidelberg


DOI: 10.1007/7355_2017_27