Review
Cell Biology
Iason Psilopatis, Kleio Vrettou, Florian Nima Fleckenstein, Stamatios Theocharis
Summary: Preeclampsia is a common hypertensive disorder in pregnancy, and PPARs play a significant role in its pathophysiology. Studies have shown contradictory conclusions regarding PPAR expression in preeclamptic placentae, but PPAR gamma agonists have been identified as a novel and potent anti-preeclamptic treatment option.
Review
Biochemistry & Molecular Biology
Iason Psilopatis, Kleio Vrettou, Constantinos Troungos, Stamatios Theocharis
Summary: Endometrial carcinoma is the most common malignant tumor of the female genital tract in the United States. Peroxisome proliferator-activated receptors (PPARs) are nuclear receptor proteins which regulate gene expression. In our literature review of 27 relevant studies published between 2000 and 2023, it was found that PPAR alpha and PPAR beta/delta isoforms were upregulated in endometrial cancer cells, while PPAR gamma levels were significantly lower. Interestingly, PPAR agonists were found to be potent anti-cancer therapeutic alternatives. Overall, PPARs seem to play a significant role in endometrial cancer.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Review
Biochemistry & Molecular Biology
Weibei Sheng, Qichang Wang, Haotian Qin, Siyang Cao, Yihao Wei, Jian Weng, Fei Yu, Hui Zeng
Summary: Osteoarthritis (OA) is a common degenerative joint disease that is exacerbated by population aging, resulting in a significant economic burden. Current therapies are inadequate, but research on peroxisome proliferator-activated receptors (PPARs) shows promise in slowing OA progression. PPARs have emerged as potential targets for effective OA treatments.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Pharmacology & Pharmacy
Chang Wang, Fei Peng, Bohua Zhong, Ying Shi, Xiaomei Wang, Xueyuan Jin, Junqi Niu
Summary: The study showed that MBT1805 has therapeutic effects on ANIT-induced cholestasis, improving abnormal biochemical indicators, gallbladder enlargement, and histopathological changes. By regulating bile acid synthesis, biotransformation, and transport, MBT1805 helps relieve cholestasis.
FRONTIERS IN PHARMACOLOGY
(2021)
Review
Medicine, General & Internal
Iason Psilopatis, Kleio Vrettou, Eleni Nousiopoulou, Kostas Palamaris, Stamatios Theocharis
Summary: Polycystic ovary syndrome (PCOS) is the most common endocrine disorder in women of reproductive age, causing severe menstrual irregularities, skin conditions, and insulin resistance-associated health problems. Peroxisome proliferator-activated receptors (PPARs) have been investigated for their role in PCOS, but studies have reached contradictory conclusions about PPAR expression in PCOS. However, natural agents have shown promise as alternative treatments for PCOS. Overall, PPARs appear to play a significant role in PCOS.
JOURNAL OF CLINICAL MEDICINE
(2023)
Review
Biochemistry & Molecular Biology
Hiroyuki Miyachi
Summary: Recent progress in understanding the structure and pharmacology of hPPAR gamma has allowed for investigation of various ligands and their effects on biological responses. These ligands serve as valuable tools for studying hPPAR gamma function and potential drugs for hPPAR gamma-related diseases. This review summarizes the medicinal chemistry research on the design, synthesis, and evaluation of hPPAR gamma antagonists based on the induction/inhibition concept of helix 12 (H12) and presents X-ray crystallographic analyses of their unique binding modes.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Review
Biochemistry & Molecular Biology
Yue-Xin Guo, Bo-Ya Wang, Han Gao, Rong-Xuan Hua, Lei Gao, Cheng-Wei He, Ying Wang, Jing-Dong Xu
Summary: This review summarizes the expression profile of PPAR-alpha in the GIT and analyzes its functions in lipid metabolism regulation and pathologic mediation in inflammation. The potential use of PPAR-alpha in treating GIT diseases and the inadequacy of clinical trials in this field are also highlighted.
FRONTIERS IN MOLECULAR BIOSCIENCES
(2022)
Article
Chemistry, Multidisciplinary
Jie Yang, Xiao Yang, Yi-fei Zhang, Jia-ning Tian, Shi-cheng Fan, Yue Gao, Hui-lin Li, Cheng-hui Cai, Min Huang, Hui-chang Bi
Summary: In this study, it was found that activation of PPARa leads to hepatomegaly in mice, with hepatocyte hypertrophy around the central vein area and hepatocyte proliferation around the portal vein area. The study also revealed that the upregulation of PPARa targets is higher in the central vein area compared to the portal vein area, while the upregulation of proliferation-related proteins mainly occurs in the portal vein area. These findings provide new insights into the understanding of PPARa activation-induced liver enlargement and regeneration.
ACTA PHARMACOLOGICA SINICA
(2023)
Review
Cell Biology
Yaqin Zhao, Huabing Tan, Xiaoyu Zhang, Jing Zhu
Summary: This article summarizes the role of PPARs in the occurrence and development of HCC, as well as their value in the diagnosis, treatment, and prognosis of HCC.
JOURNAL OF CELLULAR AND MOLECULAR MEDICINE
(2023)
Article
Medicine, General & Internal
Marjolein Garsen, Baranca Buijsers, Marloes Sol, Lena Gockeln, Ramon Sonneveld, Toin H. van Kuppevelt, Mark de Graaf, Jacob van den Born, Jan A. A. M. Kamps, Daniel H. van Raalte, Rutger W. van der Meer, Hildo J. Lamb, Jan-Luuk Hillebrands, Ton J. Rabelink, Marissa L. Maciej-Hulme, Guido Krenning, Tom Nijenhuis, Johan van der Vlag
Summary: PPAR y agonists can ameliorate proteinuria by inhibiting the expression of glomerular HPSE, providing a potential mechanism for the renoprotective effects of these drugs.
Article
Biochemistry & Molecular Biology
Xiaoyang Zhu, Qing Liu, Andrew D. Patterson, Arun K. Sharma, Shantu G. Amin, Samuel M. Cohen, Frank J. Gonzalez, Jeffrey M. Peters
Summary: Long-term ligand activation of PPARa in mice causes hepatocarcinogenesis, while hepatocarcinogenesis is diminished in Ppara-null and PPARA-humanized mice. Lipidomic analyses showed elevated levels of hepatic linoleic acid and overall fatty liver in Ppara-null and PPARA-humanized mice. The accumulation of linoleic acid and loss of CD4+ T cells suggest a new role for PPARa in age-associated hepatocarcinogenesis.
Article
Biochemistry & Molecular Biology
Shan Zhang, Yanru You, Yachong Li, Hairui Yuan, Jie Zhou, Lijie Tian, Ying Liu, Baoli Wang, Endong Zhu
Summary: Foxk1 promotes adipocyte differentiation by facilitating nuclear translocation and upregulating the transcriptional activity of the Ppar gamma 2 promoter.
Review
Chemistry, Medicinal
Enrico D'Aniello, Pietro Amodeo, Rosa Maria Vitale
Summary: This review provides an overview of discovery, optimization, and structure-activity relationship studies on PPAR modulators from marine sources, as well as the structural and computational studies that led to their identification and/or elucidation, and rationalization of their mechanisms of action.
Article
Biochemistry & Molecular Biology
Elisabetta Murru, Anna Lisa Muntoni, Claudia Manca, Sonia Aroni, Marco Pistis, Sebastiano Banni, Gianfranca Carta
Summary: The oral medication Fenofibrate (FBR) can reduce body weight, food intake, and liver lipids, and increase hepatic de novo lipogenesis through inducing changes in fatty acid metabolism. This may be achieved by activating the reactions of fatty acid derivatives such as PEA and OEA.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Review
Biochemistry & Molecular Biology
Suvadeep Mal, Ashish Ranjan Dwivedi, Vijay Kumar, Naveen Kumar, Bhupinder Kumar, Vinod Kumar
Summary: PPAR, as a crucial transcription factor, plays a significant role in regulating various disease states, especially in cancer growth and metabolism. However, known PPAR ligands often lead to severe side effects. Therefore, the current focus is on developing novel PPAR ligands with little to no adverse effects.
CURRENT MEDICINAL CHEMISTRY
(2021)