Related Experiment Video
Updated: Aug 2, 2025
A High-Throughput Luciferase Assay to Evaluate Proteolysis of the Single-Turnover Protease PCSK9
Published on: August 28, 2018
The evolving landscape of PCSK9 inhibition in cancer
1Department of Molecular, Cellular and Biomedical Sciences, Sophie Davis School of Biomedical Education, City University of New York School of Medicine, New York, NY, 10031, USA.
Abstract:
Cancer is a disease with a significant global burden in terms of premature mortality, loss of productivity, healthcare expenditures, and impact on mental health. Recent decades have seen numerous advances in cancer research and treatment options. Recently, a new role of cholesterol-lowering PCSK9 inhibitor therapy has come to light in the context of cancer. PCSK9 is an enzyme that induces the degradation of low-density lipoprotein receptors (LDLRs), which are responsible for clearing cholesterol from the serum. Thus, PCSK9 inhibition is currently used to treat hypercholesterolemia, as it can upregulate LDLRs and enable cholesterol reduction through these receptors. The cholesterol-lowering effects of PCSK9 inhibitors have been suggested as a potential mechanism to combat cancer, as cancer cells have been found to increasingly rely on cholesterol for their growth needs. Additionally, PCSK9 inhibition has demonstrated the potential to induce cancer cell apoptosis through several pathways, increase the efficacy of a class of existing anticancer therapies, and boost the host immune response to cancer. A role in managing cancer- or cancer treatment-related development of dyslipidemia and life-threatening sepsis has also been suggested. This review examines the current evidence regarding the effects of PCSK9 inhibition in the context of different cancers and cancer-associated complications.
Insights
PCSK9 inhibitors, used for lowering cholesterol, show promise in cancer treatment by reducing cancer cell cholesterol and inducing apoptosis. This therapy may also enhance existing cancer treatments and boost immune response.
Area of Science:
- Oncology
- Cardiovascular Pharmacology
- Biochemistry
Background:
- Cancer represents a significant global health burden, driving research into novel therapeutic strategies.
- Cholesterol metabolism plays a crucial role in cancer cell proliferation and survival.
- Proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors are established therapies for hypercholesterolemia.
Purpose of the Study:
- To review the emerging evidence on the role of PCSK9 inhibition in cancer.
- To explore the multifaceted effects of PCSK9 inhibitors beyond cholesterol reduction in oncological contexts.
- To examine the potential of PCSK9 inhibition in managing cancer-associated complications.
Main Methods:
- Comprehensive literature review of preclinical and clinical studies.
- Analysis of research investigating PCSK9's role in cholesterol homeostasis and cancer biology.
- Evaluation of studies on PCSK9 inhibition's impact on cancer cell apoptosis, treatment efficacy, and immune response.
Main Results:
- PCSK9 inhibition reduces serum cholesterol by upregulating low-density lipoprotein receptors (LDLRs).
- Cancer cells exhibit increased reliance on cholesterol, making cholesterol-lowering strategies a potential therapeutic avenue.
- PCSK9 inhibition demonstrates potential to induce cancer cell apoptosis, enhance existing anticancer therapies, and modulate the immune response.
Conclusions:
- PCSK9 inhibition presents a novel therapeutic strategy with potential anticancer effects.
- Beyond lipid-lowering, PCSK9 inhibition may directly impact cancer progression and treatment outcomes.
- Further research is warranted to elucidate the full potential of PCSK9 inhibitors in oncology and manage treatment-related side effects like dyslipidemia.
More Related Videos
Related Concept Videos
02:34Inhibition of Cdk Activity
02:57Targeted Cancer Therapies
There are several types of targeted therapies against...
02:50Combination Therapies and Personalized Medicine
The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...
03:03mTOR Signaling and Cancer Progression
The mTOR pathway or the...
01:05Cancer-Critical Genes II: Tumor Suppressor Genes
When the function of certain critical genes, especially those involved in cell cycle regulation and cell growth signaling cascades, gets disrupted, it upsets the cell cycle progression. Such cells with unchecked cell cycles start proliferating uncontrollably and eventually develop into tumors.
Such genes that act...