Design, synthesis, and biological evaluation of halogenated N-(2-(4-oxo-1-phenyl-1,3,8-triazaspiro[4.5]decan-8-yl)ethyl)benzamides: discovery of an isoform-selective small molecule phospholipase D2 inhibitor

Design, synthesis, and biological evaluation of halogenated N-(2-(4-oxo-1-phenyl-1,3,8-triazaspiro[4.5]decan-8-yl)ethyl)benzamides: discovery of an isoform-selective small molecule phospholipase D2 inhibitor

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http://www.wikidata.org/entity/Q24635853

Q24635853

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Phospholipase D as a therapeutic target in brain disorders Mammalian phospholipase D physiological and pathological roles Drugs for allosteric sites on receptors Two sites of action for PLD2 inhibitors: The enzyme catalytic center and an allosteric, phosphoinositide biding pocket.The Concise Guide to PHARMACOLOGY 2013/14: enzymes.Phospholipase D in cell signaling: from a myriad of cell functions to cancer growth and metastasis.Phospholipase D facilitates efficient entry of influenza virus, allowing escape from innate immune inhibition 2013 Philip S. Portoghese Medicinal Chemistry Lectureship: drug discovery targeting allosteric sites.Phospholipase D signaling pathways and phosphatidic acid as therapeutic targets in cancer Development of allosteric modulators of GPCRs for treatment of CNS disorders Discovery of desketoraloxifene analogues as inhibitors of mammalian, Pseudomonas aeruginosa, and NAPE phospholipase D enzymes.Phospholipase D mediates nutrient input to mammalian target of rapamycin complex 1 (mTORC1).A novel phosphatidic acid-protein-tyrosine phosphatase D2 axis is essential for ERBB2 signaling in mammary epithelial cells.Phospholipase D2 is involved in the formation of Golgi tubules and ArfGAP1 recruitment Further optimization of the M5 NAM MLPCN probe ML375: tactics and challenges.Phospholipase D: enzymology, functionality, and chemical modulation Human phospholipase D activity transiently regulates pyrimidine biosynthesis in malignant gliomas Comparative lipidomic analysis of mouse and human brain with Alzheimer disease.Label-free detection of G protein-SNARE interactions and screening for small molecule modulators.Lipidomics: when apocrypha becomes canonical.Discovery of a highly selective PLD2 inhibitor (ML395): a new probe with improved physiochemical properties and broad-spectrum antiviral activity against influenza strains Phosphatidic acid and lipid-sensing by mTOR Regulation of phospholipase D activity and phosphatidic acid production after purinergic (P2Y6) receptor stimulation.Sustained PKCβII activity confers oncogenic properties in a phospholipase D- and mTOR-dependent manner.Phospholipase D2 mediates survival signaling through direct regulation of Akt in glioblastoma cells.Phosphatidic acid, phospholipase D and tumorigenesis.Emerging roles of lipid metabolism in cancer metastasis."Molecular switches" on mGluR allosteric ligands that modulate modes of pharmacology.Insights into the PX (phox-homology) domain and SNX (sorting nexin) protein families: structures, functions and roles in disease.Chemical modulation of glycerolipid signaling and metabolic pathways.Targeting phospholipase D in cancer, infection and neurodegenerative disorders.Development of dual PLD1/2 and PLD2 selective inhibitors from a common 1,3,8-Triazaspiro[4.5]decane Core: discovery of Ml298 and Ml299 that decrease invasive migration in U87-MG glioblastoma cells.The influence of polyunsaturated fatty acids on the phospholipase D isoforms trafficking and activity in mast cells.Further evaluation of novel structural modifications to scaffolds that engender PLD isoform selective inhibition.PLD1 rather than PLD2 regulates phorbol-ester-, adhesion-dependent and Fc{gamma}-receptor-stimulated ROS production in neutrophils.Thematic minireview series on phospholipase D and cancer.Phospholipase D and Its Essential Role in Cancer.Clickable Substrate Mimics Enable Imaging of Phospholipase D Activity.Phospholipase D inhibitors reduce human prostate cancer cell proliferation and colony formation.Ex Uno Plura: Differential Labeling of Phospholipid Biosynthetic Pathways with a Single Bioorthogonal Alcohol.

P2860

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P2860

Design, synthesis, and biological evaluation of halogenated N-(2-(4-oxo-1-phenyl-1,3,8-triazaspiro[4.5]decan-8-yl)ethyl)benzamides: discovery of an isoform-selective small molecule phospholipase D2 inhibitor

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http://www.wikidata.org/entity/Q24635853

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2010 nî lūn-bûn

@nan

2010 թուականի Սեպտեմբերին հրատարակուած գիտական յօդուած

@hyw

2010 թվականի սեպտեմբերին հրատարակված գիտական հոդված

@hy

2010年の論文

@ja

2010年論文

@yue

2010年論文

@zh-hant

2010年論文

@zh-hk

2010年論文

@zh-mo

2010年論文

@zh-tw

2010年论文

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