Literature DB >> 11229777

Pyrrolidine inhibitors of human cytosolic phospholipase A2. Part 2: synthesis of potent and crystallized 4-triphenylmethylthio derivative 'pyrrophenone'.

K Seno1, T Okuno, K Nishi, Y Murakami, K Yamada, S Nakamoto, T Ono.   

Abstract

We synthesized a potent and crystallized human cytosolic phospholipase A2alpha inhibitor, pyrrophenone (6) which inhibits the isolated enzyme with an IC50 value of 4.2 nM. Pyrrophenone shows potent inhibition of arachidonic acid release, prostaglandin E2, thromboxane B2, and leukotriene B4 formation in human whole blood. The magnitudes of prostaglandin E2 and thromboxane B2 inhibition are the same as those of indomethacin.

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Year:  2001        PMID： 11229777     DOI： 10.1016/s0960-894x(01)00003-8

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  26 in total

1.  Effects of the inhibition of cytosolic phospholipase A(2)α in non-small cell lung cancer cells.

Authors:  Shenbagamoorthy Sundarraj; Soundarapandian Kannan; Ramar Thangam; Palani Gunasekaran
Journal:  J Cancer Res Clin Oncol       Date:  2012-01-25       Impact factor: 4.553

2.  Eosinophil cysteinyl leukotriene synthesis mediated by exogenous secreted phospholipase A2 group X.

Authors:  Ying Lai; Rob C Oslund; James G Bollinger; William R Henderson; Luis F Santana; William A Altemeier; Michael H Gelb; Teal S Hallstrand
Journal:  J Biol Chem       Date:  2010-10-25       Impact factor: 5.157

3.  Golgi-associated cPLA2alpha regulates endothelial cell-cell junction integrity by controlling the trafficking of transmembrane junction proteins.

Authors:  Elsa Regan-Klapisz; Vincent Krouwer; Miriam Langelaar-Makkinje; Laxman Nallan; Michael Gelb; Hans Gerritsen; Arie J Verkleij; Jan Andries Post
Journal:  Mol Biol Cell       Date:  2009-08-12       Impact factor: 4.138

Review 4.  Phospholipase A2 enzymes: physical structure, biological function, disease implication, chemical inhibition, and therapeutic intervention.

Authors:  Edward A Dennis; Jian Cao; Yuan-Hao Hsu; Victoria Magrioti; George Kokotos
Journal:  Chem Rev       Date:  2011-09-12       Impact factor: 60.622

5.  Sustained activation of proton channels and NADPH oxidase in human eosinophils and murine granulocytes requires PKC but not cPLA2 alpha activity.

Authors:  Deri Morgan; Vladimir V Cherny; Alison Finnegan; James Bollinger; Michael H Gelb; Thomas E DeCoursey
Journal:  J Physiol       Date:  2006-12-21       Impact factor: 5.182

6.  2-Oxoamide inhibitors of cytosolic group IVA phospholipase A2 with reduced lipophilicity.

Authors:  Georgia Antonopoulou; Victoria Magrioti; Maroula G Kokotou; Aikaterini Nikolaou; Efrosini Barbayianni; Varnavas D Mouchlis; Edward A Dennis; George Kokotos
Journal:  Bioorg Med Chem       Date:  2016-07-27       Impact factor: 3.641

7.  Synthesis of polyfluoro ketones for selective inhibition of human phospholipase A2 enzymes.

Authors:  Constantinos Baskakis; Victoria Magrioti; Naomi Cotton; Daren Stephens; Violetta Constantinou-Kokotou; Edward A Dennis; George Kokotos
Journal:  J Med Chem       Date:  2008-12-25       Impact factor: 7.446

8.  Location of inhibitors bound to group IVA phospholipase A2 determined by molecular dynamics and deuterium exchange mass spectrometry.

Authors:  John E Burke; Arneh Babakhani; Alemayehu A Gorfe; George Kokotos; Sheng Li; Virgil L Woods; J Andrew McCammon; Edward A Dennis
Journal:  J Am Chem Soc       Date:  2009-06-17       Impact factor: 15.419

Review 9.  Membrane and inhibitor interactions of intracellular phospholipases A2.

Authors:  Varnavas D Mouchlis; Edward A Dennis
Journal:  Adv Biol Regul       Date:  2015-12-19

10.  Cytosolic phospholipase A2 enzymes are not required by mouse bone marrow-derived macrophages for the control of Mycobacterium tuberculosis in vitro.

Authors:  Omar H Vandal; Michael H Gelb; Sabine Ehrt; Carl F Nathan
Journal:  Infect Immun       Date:  2006-03       Impact factor: 3.441
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