Review of Cathepsin K Inhibitor Development and the Potential Role of Phytochemicals
Cathepsin K plays a pivotal role in bone resorption and has emerged as a prominent therapeutic target for treating bone-related diseases such as osteoporosis. Despite significant advances in synthetic inhibitor development, none have achieved FDA approval due to safety and efficacy challenges. This...
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MDPI AG
2024-12-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/30/1/91 |
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| author | Dong Oh Moon |
| author_facet | Dong Oh Moon |
| author_sort | Dong Oh Moon |
| collection | DOAJ |
| description | Cathepsin K plays a pivotal role in bone resorption and has emerged as a prominent therapeutic target for treating bone-related diseases such as osteoporosis. Despite significant advances in synthetic inhibitor development, none have achieved FDA approval due to safety and efficacy challenges. This review highlights the potential of phytochemicals as alternative inhibitors, emphasizing their natural origin, structural diversity, and minimal adverse effects. Key phytochemicals, including AC-5-1, Cycloaltilisin 6, Cycloaltilisin 7, Nicolaioidesin C, and Panduratin A, were examined for their inhibitory activities against cathepsin K. While these compounds exhibit varying IC<sub>50</sub> values, their docking studies revealed significant interactions within Cathepsin K’s active site, particularly involving critical residues such as Cys25 and His162. However, challenges such as lower potency compared to synthetic inhibitors and limited in vivo studies underscore the need for structural optimization and comprehensive preclinical evaluations. This review discusses biological insights, current limitations, and future strategies for advancing phytochemical-based inhibitors toward clinical applications in managing Cathepsin K-associated diseases. |
| format | Article |
| id | doaj-art-ccffd9c3fa3b411994e65b7c83c53210 |
| institution | Kabale University |
| issn | 1420-3049 |
| language | English |
| publishDate | 2024-12-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj-art-ccffd9c3fa3b411994e65b7c83c532102025-01-10T13:18:51ZengMDPI AGMolecules1420-30492024-12-013019110.3390/molecules30010091Review of Cathepsin K Inhibitor Development and the Potential Role of PhytochemicalsDong Oh Moon0Department of Biology Education, Daegu University, 201, Daegudae-ro, Gyeongsan-si 38453, Gyeongsangbuk-do, Republic of KoreaCathepsin K plays a pivotal role in bone resorption and has emerged as a prominent therapeutic target for treating bone-related diseases such as osteoporosis. Despite significant advances in synthetic inhibitor development, none have achieved FDA approval due to safety and efficacy challenges. This review highlights the potential of phytochemicals as alternative inhibitors, emphasizing their natural origin, structural diversity, and minimal adverse effects. Key phytochemicals, including AC-5-1, Cycloaltilisin 6, Cycloaltilisin 7, Nicolaioidesin C, and Panduratin A, were examined for their inhibitory activities against cathepsin K. While these compounds exhibit varying IC<sub>50</sub> values, their docking studies revealed significant interactions within Cathepsin K’s active site, particularly involving critical residues such as Cys25 and His162. However, challenges such as lower potency compared to synthetic inhibitors and limited in vivo studies underscore the need for structural optimization and comprehensive preclinical evaluations. This review discusses biological insights, current limitations, and future strategies for advancing phytochemical-based inhibitors toward clinical applications in managing Cathepsin K-associated diseases.https://www.mdpi.com/1420-3049/30/1/91Cathepsin Kphytochemicalosteoporosisinhibitor |
| spellingShingle | Dong Oh Moon Review of Cathepsin K Inhibitor Development and the Potential Role of Phytochemicals Molecules Cathepsin K phytochemical osteoporosis inhibitor |
| title | Review of Cathepsin K Inhibitor Development and the Potential Role of Phytochemicals |
| title_full | Review of Cathepsin K Inhibitor Development and the Potential Role of Phytochemicals |
| title_fullStr | Review of Cathepsin K Inhibitor Development and the Potential Role of Phytochemicals |
| title_full_unstemmed | Review of Cathepsin K Inhibitor Development and the Potential Role of Phytochemicals |
| title_short | Review of Cathepsin K Inhibitor Development and the Potential Role of Phytochemicals |
| title_sort | review of cathepsin k inhibitor development and the potential role of phytochemicals |
| topic | Cathepsin K phytochemical osteoporosis inhibitor |
| url | https://www.mdpi.com/1420-3049/30/1/91 |
| work_keys_str_mv | AT dongohmoon reviewofcathepsinkinhibitordevelopmentandthepotentialroleofphytochemicals |