Immunology, endocrine & metabolic agents in medicinal chemistry最新文献_第4页

METABOLIC FUNCTIONS OF MYOSTATIN AND GDF11. 肌肉生长抑制素和gdf11的代谢功能。

Immunology, endocrine & metabolic agents in medicinal chemistry Pub Date : 2010-12-01 DOI: 10.2174/187152210793663810

Alexandra C McPherron

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Extracellular Regulation of Myostatin: A Molecular Rheostat for Muscle Mass. 肌生长抑制素的细胞外调控：肌肉质量的分子变阻器。

Immunology, endocrine & metabolic agents in medicinal chemistry Pub Date : 2010-01-01 DOI: 10.2174/187152210793663748

Se-Jin Lee

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Targeting the fatty acid transport proteins (FATP) to understand the mechanisms linking fatty acid transport to metabolism. 以脂肪酸转运蛋白（FATP）为目标，了解脂肪酸转运与代谢的机制。

Immunology, endocrine & metabolic agents in medicinal chemistry Pub Date : 2009-09-01 DOI: 10.2174/187152209788009850

Paul N Black, Angel Sandoval, Elsa Arias-Barrau, Concetta C DiRusso

{"title":"Targeting the fatty acid transport proteins (FATP) to understand the mechanisms linking fatty acid transport to metabolism.","authors":"Paul N Black, Angel Sandoval, Elsa Arias-Barrau, Concetta C DiRusso","doi":"10.2174/187152209788009850","DOIUrl":"10.2174/187152209788009850","url":null,"abstract":"One principal process driving fatty acid transport is vectorial acylation, where fatty acids traverse the membrane concomitant with activation to CoA thioesters. Current evidence is consistent with the proposal that specific fatty acid transport (FATP) isoforms alone or in concert with specific long chain acyl CoA synthetase (Acsl) isoforms function to drive this energy-dependent process. Understanding the details of vectorial acylation is of particular importance as disturbances in lipid metabolism many times leads to elevated levels of circulating free fatty acids, which in turn increases fatty acid internalization and ectopic accumulation of triglycerides. This is associated with changes in fatty acid oxidation rates, accumulation of reactive oxygen species, the synthesis of ceramide and ER stress. The correlation between chronically elevated plasma free fatty acids and triglycerides with the development of obesity, insulin resistance and cardiovascular disease has led to the hypothesis that decreases in pancreatic insulin production, cardiac failure, arrhythmias, and hypertrophy are due to aberrant accumulation of lipids in these tissues. To this end, a detailed understanding of how fatty acids traverse the plasma membrane, become activated and trafficked into downstream metabolic pools and the precise roles provided by the different FATP and Acsl isoforms are especially important questions. We review our current understanding of vectorial acylation and the contributions by specific FATP and Acsl isoforms and the identification of small molecule inhibitors from high throughput screens that inhibit this process and thus provide new insights into the underlying mechanistic basis of this process.","PeriodicalId":88256,"journal":{"name":"Immunology, endocrine & metabolic agents in medicinal chemistry","volume":"9 1 1","pages":"11-17"},"PeriodicalIF":0.0,"publicationDate":"2009-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4665979/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"68024729","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Chemotherapeutic Properties of n-3 Polyunsaturated Fatty Acids - Old Concepts and New Insights. n-3多不饱和脂肪酸的化疗特性-旧概念和新见解。

Immunology, endocrine & metabolic agents in medicinal chemistry Pub Date : 2009-03-01 DOI: 10.2174/187152209788009841

Wooki Kim, David N McMurray, Robert S Chapkin

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Opposing Gatekeepers of Apical Sterol Transport: Niemann-Pick C1-Like 1 (NPC1L1) and ATP-Binding Cassette Transporters G5 and G8 (ABCG5/ABCG8). 顶端甾醇转运的对立守门人：Niemann-Pick C1-Like 1 (NPC1L1) 和 ATP 结合盒转运体 G5 和 G8 (ABCG5/ABCG8)。

Immunology, endocrine & metabolic agents in medicinal chemistry Pub Date : 2009-03-01 DOI: 10.2174/187152209788009797

J Mark Brown, Liqing Yu

{"title":"Opposing Gatekeepers of Apical Sterol Transport: Niemann-Pick C1-Like 1 (NPC1L1) and ATP-Binding Cassette Transporters G5 and G8 (ABCG5/ABCG8).","authors":"J Mark Brown, Liqing Yu","doi":"10.2174/187152209788009797","DOIUrl":"10.2174/187152209788009797","url":null,"abstract":"Cholesterol is essential for the growth and function of all mammalian cells, but abnormally elevated levels of circulating low-density lipoprotein cholesterol (LDL-C) are a major risk factor for the development of atherosclerotic cardiovascular disease (ASCVD). For many years, statin drugs have been used to effectively lower LDL-C, but ASCVD still persists in most of the world. Hence, additional LDL-C lowering is now recommended, and the search for therapeutic strategies that work in synergy with statins has now begun. Intestinal absorption and biliary excretion of cholesterol represent two major pathways and continue to show promise as druggable processes. Importantly, both of these complex physiological pathways are tightly regulated by key proteins located at the apical surface of the small intestine and the liver. One of these proteins, the target of ezetimibe Niemann-Pick C1-Like 1 (NPC1L1), was recently identified to be essential for intestinal cholesterol absorption and protect against excessive biliary sterol loss. In direct opposition of NPC1L1, the heterodimer of ATP-binding cassette transporters G5 and G8 (ABCG5/ABCG8) has been shown to be critical for promoting biliary cholesterol secretion in the liver, and has also been proposed to play a direct role in intestinal disposal of sterols. The purpose of this review is to summarize the current state of knowledge regarding the function of these opposing apical cholesterol transporters, and provide a framework for future studies examining these proteins.","PeriodicalId":88256,"journal":{"name":"Immunology, endocrine & metabolic agents in medicinal chemistry","volume":"9 1","pages":"18-29"},"PeriodicalIF":0.0,"publicationDate":"2009-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2824437/pdf/nihms176868.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"28729569","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Spatial Segregation of Phosphatidylinositol 4,5-Bisphosphate (PIP(2)) Signaling in Immune Cell Functions. 免疫细胞功能中磷脂酰肌醇 4,5-二磷酸（PIP(2)）信号的空间分隔。

Immunology, endocrine & metabolic agents in medicinal chemistry Pub Date : 2008-12-01 DOI: 10.2174/187152208787169233

Corey M Johnson, William Rodgers

引用次数: 0

The Anti-Cancer Effect of A₃ Adenosine Receptor Agonists: A Novel, Targeted Therapy. A3腺苷受体激动剂的抗癌作用:一种新的靶向治疗方法。

Immunology, endocrine & metabolic agents in medicinal chemistry Pub Date : 2007-08-01 DOI: 10.2174/187152207781369878

P Fishman, K A Jacobson, A Ochaion, S Cohen, S Bar-Yehuda

{"title":"The Anti-Cancer Effect of A3 Adenosine Receptor Agonists: A Novel, Targeted Therapy.","authors":"P Fishman, K A Jacobson, A Ochaion, S Cohen, S Bar-Yehuda","doi":"10.2174/187152207781369878","DOIUrl":"10.2174/187152207781369878","url":null,"abstract":"The A3 adenosine receptor (A3AR) is highly expressed in various human solid tumor cells whereas low expression is found in the adjacent normal tissues. Activation of the A3AR with synthetic highly selective agonists, such as IB-MECA, Cl-IB-MECA or LJ529, induces tumor growth inhibition of melanoma, lymphoma, breast, hepatoma, prostate and colon carcinoma cells both in vitro and in vivo. Two molecular events take place upon receptor activation and include: a. receptor internalization and subsequent degradation, followed by decreased receptor mRNA and protein expression level. b. modulation of down-stream signal transduction pathways, including those related to Wnt and NF-κB. Subsequently, the levels of cyclin D1 and c-Myc are decreased leading to tumor growth inhibition. IB-MECA synergizes with chemotherapeutic agents to yield an additive anti-tumor effect and protects against myelotoxicity induced by chemotherapy. Taken together, A3AR agonists may be suggested as a new family of orally bioavailable compounds to be developed as potent inhibitors of malignant diseases.","PeriodicalId":88256,"journal":{"name":"Immunology, endocrine & metabolic agents in medicinal chemistry","volume":"7 ","pages":"298-303"},"PeriodicalIF":0.0,"publicationDate":"2007-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8611655/pdf/nihms-1755964.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39772095","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0