PCSK9 Inhibition: From Current Advances to Evolving Future
Proprotein convertase subtilisin/kexin type 9 (PCSK9) is a secretory serine protease synthesized primarily by the liver. It mainly promotes the degradation of low-density lipoprotein receptor (LDL-R) by binding LDL-R, reducing low-density lipoprotein cholesterol (LDL-C) clearance. In addition to reg...
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| Format: | Article |
| Language: | English |
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MDPI AG
2022-09-01
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| Series: | Cells |
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| Online Access: | https://www.mdpi.com/2073-4409/11/19/2972 |
| _version_ | 1797480042947674112 |
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| author | Chunping Liu Jing Chen Huiqi Chen Tong Zhang Dongyue He Qiyuan Luo Jiaxin Chi Zebin Hong Yizhong Liao Shihui Zhang Qizhe Wu Huan Cen Guangzhong Chen Jinxin Li Lei Wang |
| author_facet | Chunping Liu Jing Chen Huiqi Chen Tong Zhang Dongyue He Qiyuan Luo Jiaxin Chi Zebin Hong Yizhong Liao Shihui Zhang Qizhe Wu Huan Cen Guangzhong Chen Jinxin Li Lei Wang |
| author_sort | Chunping Liu |
| collection | DOAJ |
| description | Proprotein convertase subtilisin/kexin type 9 (PCSK9) is a secretory serine protease synthesized primarily by the liver. It mainly promotes the degradation of low-density lipoprotein receptor (LDL-R) by binding LDL-R, reducing low-density lipoprotein cholesterol (LDL-C) clearance. In addition to regulating LDL-R, PCSK9 inhibitors can also bind Toll-like receptors (TLRs), scavenger receptor B (SR-B/CD36), low-density lipoprotein receptor-related protein 1 (LRP1), apolipoprotein E receptor-2 (ApoER2) and very-low-density lipoprotein receptor (VLDL-R) reducing the lipoprotein concentration and slowing thrombosis. In addition to cardiovascular diseases, PCSK9 is also used in pancreatic cancer, sepsis, and Parkinson’s disease. Currently marketed PCSK9 inhibitors include alirocumab, evolocumab, and inclisiran, as well as small molecules, nucleic acid drugs, and vaccines under development. This review systematically summarized the application, preclinical studies, safety, mechanism of action, and latest research progress of PCSK9 inhibitors, aiming to provide ideas for the drug research and development and the clinical application of PCSK9 in cardiovascular diseases and expand its application in other diseases. |
| first_indexed | 2024-03-09T21:54:27Z |
| format | Article |
| id | doaj.art-1b4b517f094847f48edf4dd4a7035645 |
| institution | Directory Open Access Journal |
| issn | 2073-4409 |
| language | English |
| last_indexed | 2024-03-09T21:54:27Z |
| publishDate | 2022-09-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Cells |
| spelling | doaj.art-1b4b517f094847f48edf4dd4a70356452023-11-23T20:00:24ZengMDPI AGCells2073-44092022-09-011119297210.3390/cells11192972PCSK9 Inhibition: From Current Advances to Evolving FutureChunping Liu0Jing Chen1Huiqi Chen2Tong Zhang3Dongyue He4Qiyuan Luo5Jiaxin Chi6Zebin Hong7Yizhong Liao8Shihui Zhang9Qizhe Wu10Huan Cen11Guangzhong Chen12Jinxin Li13Lei Wang14State Key Laboratory of Dampness Syndrome of Chinese Medicine, The Second Affiliated Hospital of Guangzhou University of Chinese Medicine, Guangzhou 510080, ChinaSchool of Biotechnology and Health Sciences, Wuyi University, Jiangmen 529020, ChinaState Key Laboratory of Dampness Syndrome of Chinese Medicine, The Second Affiliated Hospital of Guangzhou University of Chinese Medicine, Guangzhou 510080, ChinaState Key Laboratory of Dampness Syndrome of Chinese Medicine, The Second Affiliated Hospital of Guangzhou University of Chinese Medicine, Guangzhou 510080, ChinaState Key Laboratory of Dampness Syndrome of Chinese Medicine, The Second Affiliated Hospital of Guangzhou University of Chinese Medicine, Guangzhou 510080, ChinaHealth Science Center, Shenzhen University, Shenzhen 518060, ChinaState Key Laboratory of Dampness Syndrome of Chinese Medicine, The Second Affiliated Hospital of Guangzhou University of Chinese Medicine, Guangzhou 510080, ChinaState Key Laboratory of Dampness Syndrome of Chinese Medicine, The Second Affiliated Hospital of Guangzhou University of Chinese Medicine, Guangzhou 510080, ChinaState Key Laboratory of Dampness Syndrome of Chinese Medicine, The Second Affiliated Hospital of Guangzhou University of Chinese Medicine, Guangzhou 510080, ChinaState Key Laboratory of Dampness Syndrome of Chinese Medicine, The Second Affiliated Hospital of Guangzhou University of Chinese Medicine, Guangzhou 510080, ChinaDepartment of Neurosurgery, Institute of Neuroscience, Guangdong Provincial People’s Hospital, Guangdong Academy of Medical Sciences, Guangzhou 510080, ChinaState Key Laboratory of Dampness Syndrome of Chinese Medicine, The Second Affiliated Hospital of Guangzhou University of Chinese Medicine, Guangzhou 510080, ChinaDepartment of Neurosurgery, Institute of Neuroscience, Guangdong Provincial People’s Hospital, Guangdong Academy of Medical Sciences, Guangzhou 510080, ChinaState Key Laboratory of Dampness Syndrome of Chinese Medicine, The Second Affiliated Hospital of Guangzhou University of Chinese Medicine, Guangzhou 510080, ChinaState Key Laboratory of Dampness Syndrome of Chinese Medicine, The Second Affiliated Hospital of Guangzhou University of Chinese Medicine, Guangzhou 510080, ChinaProprotein convertase subtilisin/kexin type 9 (PCSK9) is a secretory serine protease synthesized primarily by the liver. It mainly promotes the degradation of low-density lipoprotein receptor (LDL-R) by binding LDL-R, reducing low-density lipoprotein cholesterol (LDL-C) clearance. In addition to regulating LDL-R, PCSK9 inhibitors can also bind Toll-like receptors (TLRs), scavenger receptor B (SR-B/CD36), low-density lipoprotein receptor-related protein 1 (LRP1), apolipoprotein E receptor-2 (ApoER2) and very-low-density lipoprotein receptor (VLDL-R) reducing the lipoprotein concentration and slowing thrombosis. In addition to cardiovascular diseases, PCSK9 is also used in pancreatic cancer, sepsis, and Parkinson’s disease. Currently marketed PCSK9 inhibitors include alirocumab, evolocumab, and inclisiran, as well as small molecules, nucleic acid drugs, and vaccines under development. This review systematically summarized the application, preclinical studies, safety, mechanism of action, and latest research progress of PCSK9 inhibitors, aiming to provide ideas for the drug research and development and the clinical application of PCSK9 in cardiovascular diseases and expand its application in other diseases.https://www.mdpi.com/2073-4409/11/19/2972cardiovascular diseasePCSK9 inhibitorsclinical applicationssecurityresearch status |
| spellingShingle | Chunping Liu Jing Chen Huiqi Chen Tong Zhang Dongyue He Qiyuan Luo Jiaxin Chi Zebin Hong Yizhong Liao Shihui Zhang Qizhe Wu Huan Cen Guangzhong Chen Jinxin Li Lei Wang PCSK9 Inhibition: From Current Advances to Evolving Future Cells cardiovascular disease PCSK9 inhibitors clinical applications security research status |
| title | PCSK9 Inhibition: From Current Advances to Evolving Future |
| title_full | PCSK9 Inhibition: From Current Advances to Evolving Future |
| title_fullStr | PCSK9 Inhibition: From Current Advances to Evolving Future |
| title_full_unstemmed | PCSK9 Inhibition: From Current Advances to Evolving Future |
| title_short | PCSK9 Inhibition: From Current Advances to Evolving Future |
| title_sort | pcsk9 inhibition from current advances to evolving future |
| topic | cardiovascular disease PCSK9 inhibitors clinical applications security research status |
| url | https://www.mdpi.com/2073-4409/11/19/2972 |
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