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SREBP inhibitors: an updated patent review for 2008-present
Zhenyu Peng1, Leyuan Chen2, Manjiang Wang2
1Institute of Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin, China.
Introduction:
Sterol regulatory element-binding proteins (SREBPs) are a family of membrane-binding transcription factors that activate genes encoding enzymes required for cholesterol and unsaturated fatty acid synthesis. Overactivation of SREBP is related to the occurrence and development of diabetes, nonalcoholic fatty liver, tumor, and other diseases. In the past period, many SREBP inhibitors have been found.
Areas Covered:
This manuscript is a patent review of SREBP inhibitors. We searched 2008 to date for all data from the US patent database (https://www.uspto.gov/) and the European patent database (https://www.epo.org/) with 'SREBP' and 'inhibitor' as keywords and analyzed the search results.
Expert Opinion:
Both synthetic and natural SREBP inhibitors have been reported. Despite the lack of cocrystal structure of SREBP inhibitor, the mechanisms of several compounds have been clarified. Importantly, some SREBP inhibitors have been proved to have good activity in preclinical studies. As the characteristics of lipid metabolism reprogramming in cardio-cerebrovascular diseases and tumors are gradually revealed, more and more attention will be focused on SREBP.
Insights
This patent review highlights Sterol Regulatory Element-Binding Protein (SREBP) inhibitors, crucial for managing diseases linked to lipid metabolism. Several SREBP inhibitors show promise in preclinical studies for various conditions.
Area of Science:
- Biochemistry and Molecular Biology
- Medicinal Chemistry
- Drug Discovery
Background:
- Sterol Regulatory Element-Binding Proteins (SREBP) are transcription factors regulating cholesterol and fatty acid synthesis.
- Dysregulation of SREBP is implicated in diseases like diabetes, fatty liver disease, and cancer.
- Developing SREBP inhibitors is a key therapeutic strategy.
Purpose of the Study:
- To review patents on SREBP inhibitors from 2008 to the present.
- To analyze the landscape of SREBP inhibitor development.
- To identify promising SREBP inhibitors for future research.
Main Methods:
- Comprehensive search of US and European patent databases (USPTO, EPO).
- Keywords used: 'SREBP' and 'inhibitor'.
- Analysis of patent data from 2008 to date.
Main Results:
- Numerous synthetic and natural SREBP inhibitors have been patented.
- Mechanisms of action for several inhibitors are understood, despite limited structural data.
- Some SREBP inhibitors demonstrate significant preclinical activity.
Conclusions:
- SREBP inhibitors represent a growing area of pharmaceutical research.
- Potential applications in cardio-cerebrovascular diseases and oncology are increasing.
- Further development of SREBP inhibitors is anticipated due to their therapeutic relevance.
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