Citation: | HU Yue, XU Jun, LIU Yanhua, WANG Zengtao, HUANG Liming, FANG Jialong, WANG Chen. Advances in lipid-lowering effect of PPARα agonists[J]. Journal of China Pharmaceutical University, 2016, 47(1): 118-124. DOI: 10.11665/j.issn.1000-5048.20160118 |
[1] |
Kersten S.Integrated physiology and systems biology of PPARα[J].Mol Metab,2014,3(4):354-371.
|
[2] |
Zeng ZY,Liao GH,Lu YF,et al.Research progress of PPARα agonists on cardiovascular and cerebrovascular diseases[J].Chin J Med Chem,2014,24(2):147-156.
|
[3] |
Issemann I,Green S.Activation of a member of the steroid hormone receptor superfamily by peroxisome proliferators[J].Nature,1990,347(6294):645-650.
|
[4] |
Gilde AJ,Fruchart JC,Staels B.Peroxisome proliferator-activated receptors at the crossroads of obesity,diabetes,and cardiovascular disease[J].J Am Coll Cardiol,2009,48(9):1-9.
|
[5] |
Esmaeli S,Allameh A,Soleimani M,et al.The role of albumin and PPAR-α in differentiation-dependent change of fatty acid profile during differentiation of mesenchymal stem cells to hepatocyte-like cells[J].Cell Biochem Funct,2014,32(5):410-419.
|
[6] |
Lannutti F,Marrone A,Re N.Prediction of the PPARα agonism of fibrates by combined MM-docking approaches[J].J Mol Graph Model,2011,29:865-875.
|
[7] |
Pawlak M,Lefebvre P,Staels B.Molecular mechanism of PPARα action and its impact on lipid metabolism,inflammation and fibrosis in non-alcoholic fatty liver disease[J].J Hepatol,2015,62(3):1-14.
|
[8] |
Huang J,Das SK,Jha P,et al.The PPARα agonist fenofibrate suppresses B-cell lymphoma in mice by modulating lipid metabolism[J].Biochim Biophys Acta,2013,1831(10):1555-1565.
|
[9] |
Wu C,Jia Y,Lee JH,et al.trans-Caryophyllene is a natural agonistic ligand for peroxisome proliferator-activated receptor-α[J].Bioorg Med Chem Lett,2014,24(14):3168-3174.
|
[10] |
Lee JH,Jun HJ,Hoang MH,et al.Catalposide is a natural agonistic ligand of peroxisome proliferator activated receptor-α[J].Biochem Biophys Res Commun,2012,422(4):568-572.
|
[11] |
Jia Y,Bhuiyan MJ,Jun HJ,et al.Ursolic acid is a PPARα agonist that regulates hepatic lipid metabolism[J].Bioorg Med Chem Lett,2011,21(9):5876-5880.
|
[12] |
Jia Y,Kim JY,Jun HJ,et al.Cyanidin is an agonistic ligand for peroxisome proliferator-activated receptor-alpha reducing hepatic lipid[J].Biochim Biophys Acta,2013,1831(4):698-708.
|
[13] |
Goto T,Takahashi N,Kato S,et al.Bixin activates PPARα and improves obesity-induced abnormalities of carbohydrate and lipid metabolism in mice[J].J Agric Food Chem,2012,60(48):11952-11958.
|
[14] |
Goto T, Kim YI, Funakoshi K, et al. Farnesol, an isoprenoid, improves metabolic abnormalities in mice via both PPARα-dependent and -independent pathways[J].Am J Physiol Endocrinol Metab,2011,301(5):1022-1032.
|
[15] |
Lamers C,Dittrich M,Steri R,et al.Molecular determinants for improved activity at PPARα:structure-activity relationship of pirinixic acid derivatives,docking study and site-directed mutagenesis of PPARα[J].Bioorg Med Chem Lett,2014,24(16):4048-4052.
|
[16] |
Jia Y,Kim JH,Nam B,et al.The dipeptide H-Trp-Arg-OH(WR)Is a PPARα agonist and reduces hepatic lipid accumulation in lipid-loaded H4IIE cells[J].Appl Biochem Biotechnol,2015,175(2):1211-1220.
|
[17] |
Shi GQ,Dropinski JF,Zhang Y,et al.Novel 2,3-dihydrobenzofuran-2-carboxylic acids:highly potent and subtype-selective PPARα agonists with potent hypolipidemic activity[J].J Med Chem,2005,48(17):5589-5599.
|
[18] |
Desai RC, Metzger E, Santini C, et al. Design and synthesis of potent and subtype-selective PPARα agonists[J].Bioorg Med Chem Lett,2006,16(6):1673-1678.
|
[19] |
Fruchart JC.Selective peroxisome proliferator-activated receptor α modulators(SPPARMα):the next generation of peroxisome proliferator-activated receptor α-agonists[J].Cardiovasc Diabetol.,2013,12(82):2-8.
|
[20] |
Liu ZM,Hu M,Chan P,et al.Early investigational drugs targeting PPAR-α for the treatment of metabolic disease[J].Expert Opin Investig Drugs,2015,24(5):611-621.
|
[21] |
Sahebkar A, Chew GT, Watts GF. New peroxisome proliferator-activated receptor agonists:potential treatments for atherogenic dyslipidemia and non-alcoholic fatty liver disease[J].Expert Opin Pharmacother,2014,15(4):493-503.
|
[22] |
Brown PJ,Stuart LW,Hurley KP,et al.Identification of a subtype selective human PPARalpha agonist through parallel-array synthesis[J].Bioorg Med Chem Lett,2001,11(9):1225-1227.
|
[23] |
Solingapuram Sai KK,Kil KE,Tu Z,et al.Synthesis,radiolabeling and initial in vivo evaluation of[11C]KSM-01 for imaging PPARα receptors[J].Bioorg Med Chem Lett,2012,22(19):6233-6236.
|
[24] |
Matthews JM,Chen X,Cryan E,et al.Design and synthesis of indane-ureido-thioisobutyric acids:a novel class of PPARα agonists[J].Bioorg Med Chem Lett,2007,17(24):6773-6778.
|
[25] |
Miyachi H, Nomura M, Tanase T, et al. Design,synthesis and evaluation of substituted phenylpropanoic acid derivatives as peroxisome proliferator-activated receptor(PPAR)activators:novel human PPARα-selective activators[J].Bioorg Med Chem Lett,2002,12(1):77-80.
|
[26] |
Sierra ML,Beneton V,Boullay AB,et al.Substituted 2-[(4-aminomethyl)phenoxy]-2-methylpropionic acid PPARalpha agonists.1.Discovery of a novel series of potent HDLc raising agents[J].J Med Chem,2007,50(4):685-695.
|
[27] |
Faucher N,Martres P,Laroze A,et al.Design,synthesis and evaluation of trifluoromethane sulfonamide derivatives as new potent and selective peroxisome proliferator-activated receptor alpha agonists[J].Bioorg Med Chem Lett,2008,18(2):710-715.
|
[28] |
Ban S,Kasuga J,Nakagome I,et al.Structure-based design,synthesis,and nonalcoholic steatohepatitis(NASH)-preventive effect of phenylpropanoic acid peroxisome proliferator-activated receptor(PPAR)α-selective agonists[J].Bioorg Med Chem,2011,19:3183-3191.
|
[29] |
Wagner JD,Shadoan MK,Zhang L,et al.A selective peroxisome proliferator-activated receptor alpha agonist,CP-900691,improves plasma lipids,lipoproteins,and glycemic control in diabetic monkeys[J].J Pharmacol Exp Ther,2010,333(3):844-853.
|
[30] |
Askari B,Wietecha T,Hudkins KL,et al.Effects of CP-900691,a novel peroxisome proliferator-activated receptor α,agonist on diabetic nephropathy in the BTBR ob/ob mouse[J].Lab Invest,2014,94(8):851-862.
|
[31] |
Aoki T,Asaki T,Hamamoto T,et al.Discovery of a novel class of 1,3-dioxane-2-carboxylic acid derivatives as subtype-selective peroxisome proliferator-activated receptor alpha(PPARalpha)agonists[J].Bioorg Med Chem Lett,2008,18(6):2128-2132.
|
[32] |
Asaki T,Aoki T,Hamamoto T,et al.Structure-activity studies on 1,3-dioxane-2-carboxylic acid derivatives,a novel class of subtype-selective peroxisome proliferator-activated receptor alpha(PPARalpha)agonists[J].Bioorg Med Chem,2008,16(2):981-994.
|
[33] |
Nomura M,Yumoto K,Shinozaki T,et al.Discovery of cyclic amine-substituted benzoic acids as PPARα agonists[J].Bioorg Med Chem Lett,2012,22(1):334-338.
|
[34] |
Schäfer HL,Linz W,Falk E,et al,AVE8134,a novel potent PPARα agonist,improves lipid profile and glucose metabolism in dyslipidemic mice and type 2 diabetic rats[J].Acta Pharmacol Sin,2012 33(1):82-90.
|
[35] |
Xu Y,Mayhugnd D,Saeed A,et al.Design and synthesis of a potent and selective triazolone-based peroxisome prolife-rator-activated receptor α agonist[J].J Med Chem,2003,46(24):5121-5124.
|
[36] |
Khera AV,Millar JS,Ruotolo G,et al.Potent peroxisome proliferator-activated receptor-α agonist treatment increases cholesterol efflux capacity in humans with the metabolic syndrome[J].Eur Heart J,2015,25(6):291-295.
|
[37] |
Mizuno CS, Ma G, Khan S, et al. Design, synthesis, biological evaluation and docking studies of pterostilbene analogs inside PPAR[J].Bioorg Med Chem,2008,16(7):3800-3808.
|
[38] |
Sauerberg P,Mogensen JP,Jeppesen L,et al.Design of potent PPARalpha agonists[J].Bioorg Med Chem Lett,2007,17(11):3198-3202.
|
[39] |
Pingali H,Jain M,Shah S,et al.Design and synthesis of novel bis-oximinoalkanoic acids as potent PPARalpha agonists[J].Bioorg Med Chem Lett,2010,20(3):1156-1161.
|
[1] | CAI Xu, WU Xiaoqian, HAN Lingfei, FENG Feng, QU Wei, LIU Wenyuan. Research progress on natural products regulating osteogenic differentiation[J]. Journal of China Pharmaceutical University, 2025, 56(1): 10-21. DOI: 10.11665/j.issn.1000-5048.2024101003 |
[2] | LU Lixue, WANG Yonghui. Progress in discovery of RORγt inverse agonists for the treatment of autoimmune diseases[J]. Journal of China Pharmaceutical University, 2024, 55(1): 87-102. DOI: 10.11665/j.issn.1000-5048.2023121303 |
[3] | LU Zhipeng, XU Qinglong, CHEN Panpan, QIN Yajuan, TANG Lijun, LI Tingyou. Research progress of radioprobes targeting fibroblast activating protein[J]. Journal of China Pharmaceutical University, 2022, 53(6): 651-662. DOI: 10.11665/j.issn.1000-5048.20220603 |
[4] | YANG Qian, CHEN Nannan, YOU Qidong, XU Xiaoli. Research progress on stimulator of interferon genes (STING) agonists[J]. Journal of China Pharmaceutical University, 2022, 53(3): 253-263. DOI: 10.11665/j.issn.1000-5048.20220301 |
[5] | JI Liyang, HAO Jing, WANG Guocheng, XIE Weijia. Research progress on stimulator of interferon genes agonists for cancer immunotherapy[J]. Journal of China Pharmaceutical University, 2020, 51(1): 1-9. DOI: 10.11665/j.issn.1000-5048.20200101 |
[6] | WANG Chen, XU Jun, LIU Yanhua, WANG Zengtao, HU Yue, TIAN Taiping, YI Mengjuan. Research progress on functionalized graphene oxide as drug carriers[J]. Journal of China Pharmaceutical University, 2017, 48(1): 117-124. DOI: 10.11665/j.issn.1000-5048.20170118 |
[7] | ZHANG Danfeng, JIAO Yu, LIU Yong, ZHANG Yanmin, ZHANG Zhimin, LU Tao. Progress of small molecule anti-tumor covalent drugs[J]. Journal of China Pharmaceutical University, 2017, 48(1): 1-7. DOI: 10.11665/j.issn.1000-5048.20170101 |
[8] | HU Yue, CHEN Zhou, LUO Xiaoxing, XUE Xiaoyan. Research progress of 1, 2-dilinoleyloxy-3-dimethylaminopropane-based cationic lipid nanoparticle[J]. Journal of China Pharmaceutical University, 2016, 47(1): 112-117. DOI: 10.11665/j.issn.1000-5048.20160117 |
[9] | ZHANG Jinghui, WANG Yajing, HU Rong. Roles of Moesin in tumor progression[J]. Journal of China Pharmaceutical University, 2015, 46(3): 371-375. DOI: 10.11665/j.issn.1000-5048.20150319 |
[10] | ZHANG Qian, CHEN Cen, YANG Fengqing, XIA Zhining. Mechanism of agonist-induced platelet activation and research progress of anti-platelet drugs[J]. Journal of China Pharmaceutical University, 2014, 45(6): 632-648. DOI: 10.11665/j.issn.1000-5048.20140604 |