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Cathepsin B and L inhibitors: a patent review (2010 - present)
Yu-Yao Li1, Jing Fang1, Gui-Zhen Ao1
1a College of Pharmaceutical Science , Soochow University , Suzhou , PR China.
Introduction:
Cathepsins play an important role in protein degradation and processing. Aberrant cathepsin B or L is closely associated with many serious diseases such as cancer, osteoporosis and autoimmune disorders. Therefore, development of potent and selective cathepsin B and L inhibitors has aroused much attention in recent years. Although several classes of cathepsin inhibitors are presently available, there are still some problems to solve, such as broad-spectrum inhibition to protease, specially cysteine proteases, which lead to unpredictable side effects in clinical trials. Therefore, it is very necessary to discovery new scaffolds and new application of cathepsin B and L inhibitors for developing therapeutic agents for treating diseases mediated by cathepsin B or L. Areas covered: This updated review summarizes new patents on cathepsin B and L inhibitors from 2010 to present. Expert opinion: The review gives the latest development in the area of inhibitors of cathepsin B and L, which have been considered key therapeutic targets for the development of drugs treating related diseases. This review puts emphasis on the discovery of novel small molecule inhibitors of cathepsin B and L, as well as their new application as new therapeutic agents.
Insights
New patents reveal novel small molecule inhibitors for cathepsin B and L, crucial targets for diseases like cancer. These advancements aim to overcome limitations of current therapies, offering new hope for treating cathepsin-mediated disorders.
Area of Science:
- Biochemistry
- Pharmacology
- Medicinal Chemistry
Background:
- Cathepsins are vital for protein processing; aberrant activity links to cancer, osteoporosis, and autoimmune diseases.
- Current cathepsin inhibitors face challenges like broad-spectrum activity and side effects.
- Developing selective inhibitors for cathepsin B and L is a key research area.
Purpose of the Study:
- To review recent patents (2010-present) on cathepsin B and L inhibitors.
- To highlight novel small molecule inhibitors and their therapeutic applications.
- To address the need for improved cathepsin B and L inhibitors.
Main Methods:
- Patent literature review focusing on cathepsin B and L inhibitors.
- Analysis of novel small molecule scaffolds and their therapeutic potential.
- Summarization of recent advancements in the field.
Main Results:
- Identification of new patent filings for cathepsin B and L inhibitors.
- Emphasis on novel small molecule designs and their applications.
- Discussion of progress in overcoming limitations of existing inhibitors.
Conclusions:
- Recent patents offer promising new cathepsin B and L inhibitors.
- Novel small molecules represent a significant advancement in therapeutic strategies.
- Continued research into selective cathepsin inhibitors is essential for treating associated diseases.
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