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Protein WISDOM: A Workbench for In silico De novo Design of BioMolecules
Published on: July 25, 2013
ADAM17 as a promising therapeutic target: from structural basis to inhibitor discovery in human diseases
Lisa Liu1, Erkang Tian1, Shuqi Quan1
1State Key Laboratory of Oral Diseases, National Center for Stomatology, National Clinical Research Center for Oral Diseases, Department of Orthodontics, West China Hospital of Stomatology, Sichuan University, Chengdu, China.
Abstract:
A disintegrin and metalloproteinase 17 (ADAM17) is a transmembrane protease that regulates diverse physiological processes by shedding membrane-bound proteins, including cytokines, their receptors, and adhesion molecules. A mounting body of evidence has emerged linking ADAM17 to the pathogenesis of various diseases, including inflammation, cancer, cardiovascular and neurodegenerative diseases, highlighting its potential as a therapeutic target. This review offers a comprehensive overview of the molecular structure and biological functions of ADAM17, emphasizing its role in human diseases and therapeutic strategies that target ADAM17 activity. Recent advances in the development of ADAM17-targeting agents, including small-molecule inhibitors, monoclonal antibodies, and endogenous regulatory proteins, are discussed with a focus on the structural basis of their activity, with the aim of informing and guiding future drug discovery efforts.
Insights
A disintegrin and metalloproteinase 17 (ADAM17) is a key protease involved in various diseases. This review details ADAM17
Area of Science:
- Biochemistry
- Molecular Biology
- Pathophysiology
Background:
- ADAM17 is a transmembrane protease crucial for shedding membrane proteins.
- ADAM17 plays a role in physiological processes and disease pathogenesis.
- Evidence links ADAM17 to inflammation, cancer, and cardiovascular/neurodegenerative diseases.
Purpose of the Study:
- To provide a comprehensive overview of ADAM17.
- To emphasize ADAM17's role in human diseases.
- To discuss therapeutic strategies targeting ADAM17.
Main Methods:
- Literature review of ADAM17's molecular structure and function.
- Analysis of ADAM17's involvement in disease pathogenesis.
- Review of current and emerging ADAM17-targeting therapeutic agents.
Main Results:
- ADAM17's structure and function are detailed.
- ADAM17's implication in various disease states is highlighted.
- Advances in small-molecule inhibitors, monoclonal antibodies, and regulatory proteins targeting ADAM17 are presented.
Conclusions:
- ADAM17 is a significant therapeutic target for multiple diseases.
- Understanding ADAM17 structure is key for developing effective inhibitors.
- This review guides future drug discovery efforts for ADAM17-related conditions.
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