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Recent advances in targeting the "undruggable" proteins: from drug discovery to clinical trials.

ABSTRACT: Undruggable proteins are a class of proteins that are often characterized by large, complex structures or functions that are difficult to interfere with using conventional drug design strategies. Targeting such undruggable targets has been considered also a great opportunity for treatment of human diseases and has attracted substantial efforts in the field of medicine. Therefore, in this review, we focus on the recent development of drug discovery targeting "undruggable" proteins and their application in clinic. To make this review well organized, we discuss the design strategies targeting the undruggable proteins, including covalent regulation, allosteric inhibition, protein-protein/DNA interaction inhibition, targeted proteins regulation, nucleic acid-based approach, immunotherapy and others.

SUBMITTER: Xie X

PROVIDER: S-EPMC10480221 | biostudies-literature | 2023 Sep

REPOSITORIES: biostudies-literature

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Recent advances in targeting the "undruggable" proteins: from drug discovery to clinical trials.

Xie Xin X Yu Tingting T Li Xiang X Zhang Nan N Foster Leonard J LJ Peng Cheng C Huang Wei W He Gu G

Signal transduction and targeted therapy 20230906 1

Undruggable proteins are a class of proteins that are often characterized by large, complex structures or functions that are difficult to interfere with using conventional drug design strategies. Targeting such undruggable targets has been considered also a great opportunity for treatment of human diseases and has attracted substantial efforts in the field of medicine. Therefore, in this review, we focus on the recent development of drug discovery targeting "undruggable" proteins and their appli ...[more]

PMID: 37669923

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