Cathepsin B and L inhibitors: a patent review (2010 - present)

ABSTRACT

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.

KEYWORDS:

• Cathepsin B inhibitors
• cathepsin L inhibitors
• selectivity
• updated review

Article highlights

• Cathepsin B or L may be one of the most attractive proteases to be used as the targets for new therapeutic agents.

• A comprehensive summary of new developments in the field of cathepsin B and L inhibition is reported through discussion of patents from 2010 to present.

• New scaffolds from small molecules library, natural products as well as reasonable drug design may contribute greatly in the field of drug discovery.

• Novel use of some known cathepsin B or L inhibitors, and cathepsin B or L inhibition of some known compounds may broaden their application in clinics. This box summarizes the key points contained in the article.

Declaration of interest

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

Additional information

Funding

This research was funded by Science and Technology Program from Suzhou City (Grant No: SYS201317) and PAPD (A Project funded by the Priority Academic Program Development of Jiangsu Higher Education Institutions).