PCSK9 and Hypercholesterolemia: Therapeutic Approach
No Thumbnail
Authors
Obradović, Milan M.Zarić, Božidarka
Sudar-Milovanović, Emina
Ilinčić, Branislava
Stokić, Edita
Perović, Milan
Isenović, Esma R.
Article (Published version)
Metadata
Show full item recordAbstract
Despite the intensive research and progress in modern pharmacotherapy, hypercholesterolemia and related cardiovascular complications remain one of the leading causes of mortality and disability in the modern world. A significant contribution to the treatment of hypercholesterolemia was made by the discovery of proprotein convertase subtilisin/kexin type 9 (PCSK9). This enzyme is responsible for the degradation of the low-density lipoprotein (LDL) receptor (LDLR) found at the surface of the plasma membrane in the liver and directly associated with serum LDL level. Limitations in standard therapy used in the treatment of lipid disorders have led to the development of new drugs, such as an inhibitor of PCSK9. Over the past years, the greatest achievement in discovering the PCSK9 inhibitor was made by designing monoclonal antibodies that disable PCSK9 to bind LDLR and RNA interference to reduce PCSK9 production, but one of the main disadvantages is costeffectiveness. In this review, we wil...l summarize the most recent findings of basic and clinical studies which focus on PCSK9 function, regulation and therapeutic target for the treatment of hypercholesterolemia and associated cardiovascular diseases.
Keywords:
PCSK9 / PCSK9 and hypercholesterolemia / PCSK9 and CVD / PCSK9 therapy / evolocumab / alirocumabSource:
Current Drug Targets, 2018, 19, 9, 1058-1067Funding / projects:
- Hormonal regulation of expression and activity of the nitric oxide synthase and sodium-potassium pump in experimental models of insulin resistance, diabetes and cardiovascular disorders (RS-MESTD-Basic Research (BR or ON)-173033)
DOI: 10.2174/1389450119666171205101401
ISSN: 1389-4501; 1873-5592
PubMed: 29210646
WoS: 000437343200010
Scopus: 2-s2.0-85065074587
Institution/Community
VinčaTY - JOUR AU - Obradović, Milan M. AU - Zarić, Božidarka AU - Sudar-Milovanović, Emina AU - Ilinčić, Branislava AU - Stokić, Edita AU - Perović, Milan AU - Isenović, Esma R. PY - 2018 UR - http://www.eurekaselect.com/158061/article UR - https://vinar.vin.bg.ac.rs/handle/123456789/7916 AB - Despite the intensive research and progress in modern pharmacotherapy, hypercholesterolemia and related cardiovascular complications remain one of the leading causes of mortality and disability in the modern world. A significant contribution to the treatment of hypercholesterolemia was made by the discovery of proprotein convertase subtilisin/kexin type 9 (PCSK9). This enzyme is responsible for the degradation of the low-density lipoprotein (LDL) receptor (LDLR) found at the surface of the plasma membrane in the liver and directly associated with serum LDL level. Limitations in standard therapy used in the treatment of lipid disorders have led to the development of new drugs, such as an inhibitor of PCSK9. Over the past years, the greatest achievement in discovering the PCSK9 inhibitor was made by designing monoclonal antibodies that disable PCSK9 to bind LDLR and RNA interference to reduce PCSK9 production, but one of the main disadvantages is costeffectiveness. In this review, we will summarize the most recent findings of basic and clinical studies which focus on PCSK9 function, regulation and therapeutic target for the treatment of hypercholesterolemia and associated cardiovascular diseases. T2 - Current Drug Targets T1 - PCSK9 and Hypercholesterolemia: Therapeutic Approach VL - 19 IS - 9 SP - 1058 EP - 1067 DO - 10.2174/1389450119666171205101401 ER -
@article{ author = "Obradović, Milan M. and Zarić, Božidarka and Sudar-Milovanović, Emina and Ilinčić, Branislava and Stokić, Edita and Perović, Milan and Isenović, Esma R.", year = "2018", abstract = "Despite the intensive research and progress in modern pharmacotherapy, hypercholesterolemia and related cardiovascular complications remain one of the leading causes of mortality and disability in the modern world. A significant contribution to the treatment of hypercholesterolemia was made by the discovery of proprotein convertase subtilisin/kexin type 9 (PCSK9). This enzyme is responsible for the degradation of the low-density lipoprotein (LDL) receptor (LDLR) found at the surface of the plasma membrane in the liver and directly associated with serum LDL level. Limitations in standard therapy used in the treatment of lipid disorders have led to the development of new drugs, such as an inhibitor of PCSK9. Over the past years, the greatest achievement in discovering the PCSK9 inhibitor was made by designing monoclonal antibodies that disable PCSK9 to bind LDLR and RNA interference to reduce PCSK9 production, but one of the main disadvantages is costeffectiveness. In this review, we will summarize the most recent findings of basic and clinical studies which focus on PCSK9 function, regulation and therapeutic target for the treatment of hypercholesterolemia and associated cardiovascular diseases.", journal = "Current Drug Targets", title = "PCSK9 and Hypercholesterolemia: Therapeutic Approach", volume = "19", number = "9", pages = "1058-1067", doi = "10.2174/1389450119666171205101401" }
Obradović, M. M., Zarić, B., Sudar-Milovanović, E., Ilinčić, B., Stokić, E., Perović, M.,& Isenović, E. R.. (2018). PCSK9 and Hypercholesterolemia: Therapeutic Approach. in Current Drug Targets, 19(9), 1058-1067. https://doi.org/10.2174/1389450119666171205101401
Obradović MM, Zarić B, Sudar-Milovanović E, Ilinčić B, Stokić E, Perović M, Isenović ER. PCSK9 and Hypercholesterolemia: Therapeutic Approach. in Current Drug Targets. 2018;19(9):1058-1067. doi:10.2174/1389450119666171205101401 .
Obradović, Milan M., Zarić, Božidarka, Sudar-Milovanović, Emina, Ilinčić, Branislava, Stokić, Edita, Perović, Milan, Isenović, Esma R., "PCSK9 and Hypercholesterolemia: Therapeutic Approach" in Current Drug Targets, 19, no. 9 (2018):1058-1067, https://doi.org/10.2174/1389450119666171205101401 . .