Monoacylglycerol Lipase Inhibitors: Modulators for Lipid Metabolism in Cancer Malignancy, Neurological and Metabolic Disorders

Publication date: Available online 18 October 2019Source: Acta Pharmaceutica Sinica BAuthor(s): Hui Deng, Weimin LiAbstractMonoacylglycerol lipase (MAGL) is a serine hydrolase that plays a crucial role catalysing the hydrolysis of monoglycerides into glycerol and fatty acids. It links the endocannabinoid and eicosanoid systems together by degradation of the abundant endocannabinoid 2-arachidaoylglycerol into arachidonic acid, the precursor of prostaglandins and other inflammatory mediators. MAGL inhibitors have been considered as important agents in many therapeutic fields, including anti-nociceptive, anxiolytic, anti-inflammatory, and even anti-cancer. Currently, ABX-1431, a first-in-class inhibitor of MAGL, is entering clinical phase 2 studies for neurological disorders and other diseases. This review summarizes the diverse (patho)physiological roles of MAGL and will provide an overview on the development of MAGL inhibitors. Although a large number of MAGL inhibitors have been reported, novel inhibitors are still required, particularly reversible ones.Graphical abstractGraphical abstract. Monoacylglycerol lipase (MAGL) plays a crucial role catalyzing the hydrolysis of monoglycerides. MAGL inhibitors have been considered as important agents in many therapeutic fields, including anti-nociceptive, anti-inflammatory and anti-cancer. The diverse (patho)physiological roles of MAGL and a comprehensive overview of reported MAGL inhibitors were summarized in this review.
Source: Acta Pharmaceutica Sinica B - Category: Cancer & Oncology Source Type: research

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CONCLUSIONS: Considering the age group in which rectal prolapse is most commonly seen, and the change in bowel habits, chronic constipation and irritation chronic seen in rectal prolapse may be responsible for the development of rectum cancer, therefore endoscopic screening should not be overlooked in rectal prolapse cases. KEY WORDS: Anorectal emergencies, Colon cancer, Rectal prolapse. PMID: 31723051 [PubMed - in process]
Source: Annali Italiani di Chirurgia - Category: Surgery Tags: Ann Ital Chir Source Type: research
Publication date: Available online 15 November 2019Source: Trends in Food Science &TechnologyAuthor(s): Ryoiti KiyamaAbstractBackgroundGreen tea is produced from the tea plant Camellia sinensis without fermentation, and contains characteristic constituents, which are associated with health-promoting effects such as physiological, immunological, neurological and psychological effects, and protective effects against diseases, such as cancer, cardiovascular diseases and diabetes. Catechins, such as catechin, epicatechin, epigallocatechin, epicatechin-3-O-gallate and epigallocatechin-3-O-gallate, and other green tea consti...
Source: Trends in Food Science and Technology - Category: Food Science Source Type: research
CONCLUSIONS: Both STX3451 and STX2895 provide new approaches for inducing cell death and lowering tumour burden in NF2 as well as in NF1, which both have limited treatment options. PMID: 31730023 [PubMed - in process]
Source: BMC Pharmacology and Toxicology - Category: Drugs & Pharmacology Tags: BMC Pharmacol Toxicol Source Type: research
CONCLUSIONS: The matrices and the questionnaire have a great diagnostic performance which seems interesting for a use as a screening tool for occupational exposures. These results have yet to be confirmed by large-scale studies. PMID: 31727556 [PubMed - as supplied by publisher]
Source: Revue des Maladies Respiratoires - Category: Respiratory Medicine Tags: Rev Mal Respir Source Type: research
The objective of this paper is to synthesise current knowledge on ALK rearrangement and its impact on the management of advanced NSCLC. Several inhibitors of the tyrosine kinase of ALK (crizotinib, ceritinib, alectinib) have been approved as first line therapies in patients with advanced ALK positive NSCLC, which are associated with a better median progression-free survival than conventional chemotherapy. Unfortunately, the emergence of drug resistance leads to tumor progression. In patients with oligoprogressive disease if local ablative therapy can be effected, continuing with the same ALK tyrosine kinase inhibitor is on...
Source: Revue des Maladies Respiratoires - Category: Respiratory Medicine Tags: Rev Mal Respir Source Type: research
Publication date: Available online 15 November 2019Source: Biotechnology ReportsAuthor(s): Pradeep Kumar, Balwant Singh, Vikram Thakur, Abhishek Thakur, Nandita Thakur, Deepak Pandey, Duni ChandAbstractTaxol® (generic name Paclitaxel) is a chemotherapeutic drug, effective against head, neck, breast, lung, bladder, ovary, and cervix cancers. Rising demands in chemotherapy and limited supply of natural taxol have ultimately increased the cost of the drug. Semi synthesis using taxol precursors is not able to meet the global supply and has intensified the need to find alternative ways of taxol production. In the present st...
Source: Biotechnology Reports - Category: Biotechnology Source Type: research
Publication date: Available online 15 November 2019Source: Biosensors and BioelectronicsAuthor(s): Liying Zhao, Huaixia Yang, Xiaoke Zheng, Jinge Li, Lihe Jian, Weisheng Feng, Jinming KongAbstractCytokeratin fragment antigen 21–1 (CYFRA 21–1) DNA is a crucial biomarker closely associated with non-small cell lung cancer. Here, we fabricated a novel electrochemical biosensor for ultrasensitive detection of CYFRA 21–1 DNA via polysaccharide and electrochemically mediated atom transfer radical polymerization (eATRP) dual signal amplification. Specifically, thiolated peptide nucleic acid (PNA) probes at 5&prim...
Source: Biosensors and Bioelectronics - Category: Biotechnology Source Type: research
Authors: Yang JD, Ma L, Zhu Z Abstract We assessed the expression of Serpin Family E Member 1 (SERPINE1) and its prognostic values in gastric adenocarcinoma (GAC) by using the data from TCGA database. The biological functions of SERPINE1 in GAC cells were detected by cell counting Kit-8, colony-forming, Transwell, and wound-healing assays, appropriately. Relative mRNA and protein levels were detected by RT-qPCR and western blot. Bioinformatics analysis indicated that SERPINE1 was significantly up-regulated in GAC tissues compared to normal tissues. High SERPINE1 expression led to a short overall survival and could ...
Source: Journal of Chemotherapy - Category: Cancer & Oncology Tags: J Chemother Source Type: research
Authors: Grothey A, Marshall JL, Bekaii-Saab T PMID: 31730592 [PubMed - in process]
Source: Clinical Advances in Hematology and Oncology - Category: Cancer & Oncology Tags: Clin Adv Hematol Oncol Source Type: research
Authors: Grothey A PMID: 31730591 [PubMed - in process]
Source: Clinical Advances in Hematology and Oncology - Category: Cancer & Oncology Tags: Clin Adv Hematol Oncol Source Type: research
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