Related Experiment Video
Updated: Jan 17, 2026

Network Pharmacology Prediction and Metabolomics Validation of the Mechanism of Fructus Phyllanthi against Hyperlipidemia
Published on: April 7, 2023
[Targets of anti-hyperlipidemia drugs]
Hui Li1, Xian Jing, Xiaolan Deng
1Institute of Clinical Pharmacology, Central South University; Hunan Key Laboratory of Pharmacogenetics, Changsha 410078, China.
Insights
Hyperlipidemia increases cardiovascular disease risk. Targeting key lipid metabolism proteins like NPC1L1 and PCSK9 offers new strategies for developing effective lipid-lowering drugs.
Area of Science:
- Biochemistry
- Pharmacology
- Cardiovascular Medicine
Background:
- Hyperlipidemia is a major risk factor for atherosclerosis and cardiovascular diseases.
- Current lipid-lowering drugs primarily target plasma low-density lipoprotein and high-density lipoprotein levels.
Purpose of the Study:
- To identify key proteins involved in lipid metabolism that serve as targets for anti-hyperlipidemia drugs.
- To explore these proteins as potential targets for novel lipid-lowering drug development.
Main Methods:
- The study focuses on proteins regulating lipid metabolism, including Niemann-Pick C1 like 1 protein (NPC1L1), ACAT, ABCG5/G8, MTP, MAGT, PPAR, FXR, and PCSK9.
- These proteins are identified as crucial in lipid metabolism and as targets for existing and novel anti-hyperlipidemia therapies.
Main Results:
- Several proteins, including NPC1L1, ACAT, ABCG5/G8, MTP, MAGT, PPAR, FXR, and PCSK9, play critical roles in lipid metabolism.
- These proteins are validated targets for current lipid-lowering drugs and serve as evidence for clinical drug selection.
Conclusions:
- The identified lipid metabolism proteins represent crucial targets for anti-hyperlipidemia drug development.
- Targeting these proteins offers a breakthrough approach for creating new and effective lipid-lowering therapies.
Abstract:
Hyperlipidemia is one of the most important risk factors for atherosclerosis, coronary heart disease and other cardiovascular diseases. It is the main effect of lipid-lowering drugs to reduce the plasma low-density lipoprotein or to enhance high-density lipoprotein. Niemann-Pick C1 like 1 protein (NPC1L1), acyl-coenzyme A: cholesterol acyltransferases (ACAT), ATP binding cassette transporter G member 5 and member 8 (ABCG5/G8), microsomal triglyceride transfer protein (MTP), monoacylglycerol acyltransferase, diacylglycerol acyltransferases (MAGT), peroxisome proliferator-activated receptor (PPAR), farnesoid X receptor (FXR), and proprotein convertase subtilisin/kexin type 9 (PCSK9) play key roles in the metabolism of lipid, which are regarded as the targets of anti-hyperlipidemia drugs and evidence for clinic choice of lipid-lowering drugs. These proteins are considered as breakthrough points for new lipid-lowering drug development.
Related Concept Videos
Atherosclerosis III: Management
Coronary Artery Disease IV: Preventive Measures
Lipid-Lowering Drugs: Statins and Miscellaneous Agents
Targets for Drug Action: Overview
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...
Antiplatelet Drugs: Prostaglandin Synthesis, P2Y12 and Glycoprotein IIb/IIIa Inhibitors
Prostaglandin synthesis inhibitors, exemplified by the widely known aspirin, wield their power by irreversibly acetylating...
Oral Hypoglycemic Agents: α-Glucosidase Inhibitors
Acarbose and miglitol are...

