4.5 Review

ANGPTL3: a novel biomarker and promising therapeutic target

Journal

JOURNAL OF DRUG TARGETING
Volume 27, Issue 8, Pages 876-884

Publisher

TAYLOR & FRANCIS LTD
DOI: 10.1080/1061186X.2019.1566342

Keywords

ANGPTL3; signalling pathway; biological feature; biomarkers; therapeutic target

Funding

  1. National Natural Sciences Foundation of China [81270359, 81774130, 81670268]
  2. Key projects of Hunan traditional Chinese Medicine Administration [201614]
  3. Science Foundation for Distinguished Young Scholars of Hunan Province [2018JJ1018]
  4. Hunan Provincial Key Discipline of Pharmaceutical Science

Ask authors/readers for more resources

Angiopoietin-like protein 3 (ANGPTL3) belongs to a multifunctional secreted protein that mainly expresses in the liver, and is regulated by numerous post-translational modifications, including multiple cleavage and glycosylation. Accumulating evidences have revealed that ANGPTL3 plays a critical role in both biological processes, such as lipid metabolism, angiogenesis and haematopoietic function and pathological changes, including atherosclerosis, carcinogenesis, nephrotic syndrome, diabetes, liver diseases and so on. Thus, ANGPTL3 may serve as a potential biomarker in these diseases. Furthermore, ANGPTL3 signalling pathways including LXR/ANGPTL3, thyroid hormone/ANGPTL3, insulin/ANGPTL3 and leptin/ANGPTL3 are also involved in physiological and pathological processes. Some biological ANGPTL3 inhibitors, chemical drugs and traditional Chinese medicine exert beneficial effects by targeting ANGPTL3 directly or indirectly. Therefore, elucidating the effects and underlying mechanisms of ANGPTL3 is essential to develop promising strategies in the diagnosis and treatment of related diseases.

Authors

I am an author on this paper
Click your name to claim this paper and add it to your profile.

Reviews

Primary Rating

4.5
Not enough ratings

Secondary Ratings

Novelty
-
Significance
-
Scientific rigor
-
Rate this paper

Recommended

Article Pharmacology & Pharmacy

Celastrol Attenuates Lipid Accumulation and Stemness of Clear Cell Renal Cell Carcinoma via CAV-1/LOX-1 Pathway

Chan-Juan Zhang, Neng Zhu, Yu-Xiang Wang, Le-Ping Liu, Tan-Jun Zhao, Hong-Tao Wu, Duan-Fang Liao, Li Qin

Summary: The study indicates that celastrol may be a promising active ingredient from traditional Chinese medicine for treating clear cell renal cell carcinoma by inhibiting lipid accumulation and reducing the number of caveolae to slow down tumor growth.

FRONTIERS IN PHARMACOLOGY (2021)

Review Cell Biology

Targeting HDL in tumor microenvironment: New hope for cancer therapy

Tan-Jun Zhao, Neng Zhu, Ya-Ning Shi, Yu-Xiang Wang, Chan-Juan Zhang, Chang-Feng Deng, Duan-Fang Liao, Li Qin

Summary: High-density lipoprotein is closely related to the risk of various cancers and plays a crucial role in tumorigenesis and cancer development by influencing the tumor microenvironment and immune response, suggesting a potential strategy for cancer therapy.

JOURNAL OF CELLULAR PHYSIOLOGY (2021)

Review Oncology

Cholesterol homeostasis and cancer: a new perspective on the low-density lipoprotein receptor

Jia Gu, Neng Zhu, Hong-Fang Li, Tan-Jun Zhao, Chan-Juan Zhang, Duan-Fang Liao, Li Qin

Summary: The dysregulation of LDLR in cancer and its role in cholesterol homeostasis imbalance provides new therapeutic opportunities. LDLR plays a crucial role in cancer progression by modulating cholesterol balance and may serve as a novel target for anti-cancer drug development. The expression and regulation of LDLR vary in different types of cancer, suggesting the importance of personalized treatment approaches.

CELLULAR ONCOLOGY (2022)

Review Pharmacology & Pharmacy

Ezetimibe and Cancer: Is There a Connection?

Jia Gu, Neng Zhu, Hong-Fang Li, Chan-Juan Zhang, Yong-Zhen Gong, Duan-Fang Liao, Li Qin

Summary: High serum cholesterol levels can lead to cancer, but ezetimibe, a drug that reduces cholesterol absorption, has been shown to inhibit cancer development through various mechanisms. There has been debate, but more and more evidence suggests that ezetimibe does not increase the risk of cancer.

FRONTIERS IN PHARMACOLOGY (2022)

Review Oncology

Present Status, Challenges, and Prospects of Dihydromyricetin in the Battle against Cancer

Jiajun Wu, Zuowei Xiao, Hongfang Li, Neng Zhu, Jia Gu, Wenmao Wang, Chao Liu, Wei Wang, Li Qin

Summary: Dihydromyricetin (DHM), a natural flavonoid compound extracted from Ampelopsis grossedentata, has attracted attention due to its multiple beneficial activities and anticancer effects. DHM inhibits the progression of various cancers through various mechanisms, such as antiangiogenesis, antiproliferation, apoptosis, and inhibition of invasion and migration. In addition, DHM can regulate multiple signaling pathways involved in cancer development, including mTOR, noncoding RNA-mediated signaling, PI3K/Akt pathway, NF-kappa B, p53, and ER stress-driven signaling. DHM also has a remarkable ability to reverse drug resistance when used in combination with other drugs. However, the low bioavailability of DHM limits its potential applications, which can be improved through structural modification and exploration of novel dosage forms.

CANCERS (2022)

Article Biochemistry & Molecular Biology

Wnt5a/Ror2 promotes vascular smooth muscle cells proliferation via activating PKC

Yaning Shi, Hongfang Li, Jia Gu, Yongzhen Gong, Xuejiao Xie, Duanfang Liao, Li Qin

Summary: Wnt5a promotes the proliferation of VSMCs by activating PKC through binding with Ror2. The expression of Wnt5a protein increased significantly in VSMCs stimulated by 10% serum in a time-dependent manner. Overexpression of Wnt5a accelerated the proliferation rate of VSMCs, while knockdown of Wnt5a reversed this effect. Wnt5a up-regulated the expression of Ror2 by binding to it. Furthermore, Wnt5a induced the expression of PKC in VSMCs, and knockdown of Wnt5a or Ror2 inhibited PKC phosphorylation.

FOLIA HISTOCHEMICA ET CYTOBIOLOGICA (2022)

Review Cell & Tissue Engineering

The lipid rafts in cancer stem cell: a target to eradicate cancer

Shuo Zhang, Neng Zhu, Hong Fang Li, Jia Gu, Chan Juan Zhang, Duan Fang Liao, Li Qin

Summary: Cancer stem cells (CSCs) are a subpopulation of cancer cells with stem cell properties, and lipid rafts play a crucial role in CSCs, making them promising therapeutic targets for cancer treatment.

STEM CELL RESEARCH & THERAPY (2022)

Review Endocrinology & Metabolism

New dawn for cancer cell death: Emerging role of lipid metabolism

Chanjuan Zhang, Neng Zhu, Hongfang Li, Yongzhen Gong, Jia Gu, Yaning Shi, Duanfang Liao, Wei Wang, Aiguo Dai, Li Qin

Summary: This review summarizes the emerging concepts of lipid metabolic reprogramming in cancer, including pathways like lipid uptake and trafficking, de novo synthesis, esterification, fatty acid synthesis, and oxidation. Cancer cells continuously adapt their metabolism to the changing environment, with lipid metabolism interacting bidirectionally with epigenetic modifying enzymes to regulate cancer cell death. Lipids in the tumor microenvironment play unique roles beyond metabolic needs, and targeting lipid metabolism could be a potential therapeutic strategy for improving cancer patient treatment efficacy and survival.

MOLECULAR METABOLISM (2022)

Article Chemistry, Analytical

GSH-specific fluorescent probe for sensing, bioimaging, rapid screening of natural inhibitor Celastrol and ccRCC theranostics

Chanjuan Zhang, Yan Qin, Changfeng Deng, Neng Zhu, Yaning Shi, Wei Wang, Li Qin

Summary: An off-on fluorescent probe (NBD-P) has been developed for detecting and visualizing intracellular glutathione (GSH) which can distinguish cancer tissues from normal tissues. This study also establishes a rapid drug screening method using NBD-P and identifies a natural GSH inhibitor from Tripterygium wilfordii Hook F. Additionally, insights into fluorescence probes for GSH inhibitors and cancer diagnosis, as well as the anti-cancer effects of Traditional Chinese Medicine (TCM), are provided.

ANALYTICA CHIMICA ACTA (2023)

Review Medicine, Research & Experimental

Celastrol: The new dawn in the treatment of vascular remodeling diseases

Jun-Lan Tan, Jian Yi, Xian-Ya Cao, Fei-Ying Wang, Si-Lin Xie, Ling-Ling Zhou, Li Qin, Ai-Guo Dai

Summary: There is increasing evidence that abnormal vascular remodeling plays a role in cardiovascular diseases (CVDs), making it a potential target for prevention and treatment. Celastrol, an active ingredient of the Chinese herb Tripterygium wilfordii Hook F, has shown promise in improving vascular remodeling through various mechanisms. It has been proven to ameliorate inflammation, hyperproliferation, and migration of vascular smooth muscle cells, as well as other factors involved in vascular remodeling. Celastrol has also demonstrated positive effects in treating hypertension, atherosclerosis, and pulmonary artery hypertension.

BIOMEDICINE & PHARMACOTHERAPY (2023)

Review Cell Biology

Resistin-like molecules: a marker, mediator and therapeutic target for multiple diseases

Yaning Shi, Neng Zhu, Yun Qiu, Junlan Tan, Feiying Wang, Li Qin, Aiguo Dai

Summary: RELMs are highly cysteine-rich proteins, including RELM alpha, RELM beta, Resistin, and RELM gamma, which exhibit significant differences in structure, distribution, and function. The expression of RELMs is regulated by various signaling molecules, such as IL-4, IL-13, and their receptors. RELMs proteins are involved in a wide range of physiological and pathological processes, and participate in the progression of numerous diseases. Meanwhile, RELMs can serve as biomarkers, risk predictors, and therapeutic targets for these diseases, providing novel targets or strategies for their treatment and prevention.

CELL COMMUNICATION AND SIGNALING (2023)

Article Biochemistry & Molecular Biology

In Vitro Anti-Influenza A Virus H1N1 Effect of Sesquiterpene-Rich Extracts of Carpesium abrotanoides

Li Li, Shenghui Yang, Dilu Chen, Zhihuang Wu, Meijun Zhang, Fang Yang, Li Qin, Xiaojiang Zhou

Summary: This study evaluated the anti-influenza A virus H1N1 potential of sesquiterpene-targeted fractions derived from Carpesium abrotanoides for the first time. The results indicated that SECA showed significant protective effects on MDCK cells infected with influenza A virus (H1N1).

MOLECULES (2022)

Article Biochemistry & Molecular Biology

An ultrasensitive GSH-specific fluorescent probe unveils celastrol-induced ccRCC ferroptosis

Hongfang Li, Changfeng Deng, Neng Zhu, Chanjuan Zhang, Qing Zeng, Li Qin

Summary: In this study, a stable and highly selective fluorescent probe AR was designed and synthesized for real-time monitoring of intracellular glutathione (GSH) levels and fluorescence imaging. The probe can track changes in GSH levels and fluorescence imaging, aiding in early diagnosis of diseases and evaluating the effects of cell death-inducing drugs. Furthermore, the probe was able to observe a significant decrease in GSH levels during the treatment of clear cell renal cell carcinoma (ccRCC) with celastrol-induced ferroptosis. These findings provide a novel strategy for celastrol targeting ferroptosis in ccRCC treatment and the application of fluorescent probes in understanding the mechanism of CeT in ccRCC treatment.

BIOORGANIC CHEMISTRY (2023)

Review Biochemistry & Molecular Biology

A Lipid Perspective on Regulated Pyroptosis

Yun Qiu, Ya-Ning Shi, Neng Zhu, Shuo Zhang, Chan-Juan Zhang, Jia Gu, Peng He, Ai-Guo Dai, Li Qin

Summary: Pyroptosis is a pro-inflammatory cell death caused by Gasdermin (GSMD) family-mediated membrane pore formation and cell lysis. It leads to the release of inflammatory factors and inflammation in multiple tissues, impacting various metabolic disorders. Lipid metabolism plays a significant role in pyroptosis, as bioactive lipid molecules act as triggers and regulators of pyroptosis. Understanding the relationship between lipid molecules, such as cholesterol and fatty acids, and pyroptosis during metabolic processes can provide insights into disease pathogenesis and aid in developing effective strategies.

INTERNATIONAL JOURNAL OF BIOLOGICAL SCIENCES (2023)

Article Geriatrics & Gerontology

Crosstalk between Lipid Rafts and Aging: New Frontiers for Delaying Aging

Shuo Zhang, Neng Zhu, Jia Gu, Hong-Fang Li, Yun Qiu, Duan-Fang Liao, Li Qin

Summary: With the global population rapidly aging, delaying aging has become a hot research topic. Lipid rafts (LRs), which are microdomains in the plasma membrane containing sphingolipids and cholesterol, have been found to have an interesting interplay with aging. The components of LRs are altered with aging, and LRs strongly influence the aging process. Therefore, targeting LRs is a promising strategy for delaying aging.

AGING AND DISEASE (2022)

No Data Available