Literature DB >> 16686528

The first potent inhibitor of mammalian group X secreted phospholipase A2: elucidation of sites for enhanced binding.

Brian P Smart1, Rob C Oslund, Laura A Walsh, Michael H Gelb.   

Abstract

Using the X-ray structure of human group X secreted phospholipase A(2) (hGX), we carried out structure-based design of indole-based inhibitors and prepared the compounds using a new synthetic route. The most potent compound inhibited hGX and the mouse orthologue with an IC(50) of 75 nM. This compound is the most potent hGX inhibitor reported to date and was also found to inhibit a subset of the other mouse and human sPLA(2)s.

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Year:  2006        PMID： 16686528      PMCID： PMC2963729          DOI： 10.1021/jm060136t

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  22 in total

Review 1.  Increasing molecular diversity of secreted phospholipases A(2) and their receptors and binding proteins.

Authors:  E Valentin; G Lambeau
Journal:  Biochim Biophys Acta       Date:  2000-10-31

Review 2.  Interfacial enzymology: the secreted phospholipase A(2)-paradigm.

Authors:  O G Berg; M H Gelb; M D Tsai; M K Jain
Journal:  Chem Rev       Date:  2001-09       Impact factor: 60.622

3.  Exogenously added human group X secreted phospholipase A(2) but not the group IB, IIA, and V enzymes efficiently release arachidonic acid from adherent mammalian cells.

Authors:  S Bezzine; R S Koduri; E Valentin; M Murakami; I Kudo; F Ghomashchi; M Sadilek; G Lambeau; M H Gelb
Journal:  J Biol Chem       Date:  2000-02-04       Impact factor: 5.157

4.  Purified group X secretory phospholipase A(2) induced prominent release of arachidonic acid from human myeloid leukemia cells.

Authors:  K Hanasaki; T Ono; A Saiga; Y Morioka; M Ikeda; K Kawamoto; K Higashino; K Nakano; K Yamada; J Ishizaki; H Arita
Journal:  J Biol Chem       Date:  1999-11-26       Impact factor: 5.157

Review 5.  The expanding superfamily of phospholipase A(2) enzymes: classification and characterization.

Authors:  D A Six; E A Dennis
Journal:  Biochim Biophys Acta       Date:  2000-10-31

Review 6.  Phospholipase A2.

Authors:  Makoto Murakami; Ichiro Kudo
Journal:  J Biochem       Date:  2002-03       Impact factor: 3.387

7.  Arachidonic acid release from mammalian cells transfected with human groups IIA and X secreted phospholipase A(2) occurs predominantly during the secretory process and with the involvement of cytosolic phospholipase A(2)-alpha.

Authors:  Carine M Mounier; Farideh Ghomashchi; Margaret R Lindsay; Scott James; Alan G Singer; Robert G Parton; Michael H Gelb
Journal:  J Biol Chem       Date:  2004-03-08       Impact factor: 5.157

8.  Role of group V phospholipase A2 in zymosan-induced eicosanoid generation and vascular permeability revealed by targeted gene disruption.

Authors:  Yoshiyuki Satake; Bruno L Diaz; Barbara Balestrieri; Bing K Lam; Yoshihide Kanaoka; Michael J Grusby; Jonathan P Arm
Journal:  J Biol Chem       Date:  2004-02-04       Impact factor: 5.157

9.  Inhibition of the complete set of mammalian secreted phospholipases A(2) by indole analogues: a structure-guided study.

Authors:  Brian P Smart; Ying H Pan; Amanda K Weeks; James G Bollinger; Brian J Bahnson; Michael H Gelb
Journal:  Bioorg Med Chem       Date:  2004-04-01       Impact factor: 3.641

10.  Induction of distinct sets of secretory phospholipase A(2) in rodents during inflammation.

Authors:  Katsuhiko Hamaguchi; Hiroshi Kuwata; Kumiko Yoshihara; Seiko Masuda; Satoko Shimbara; Sachiko Oh-ishi; Makoto Murakami; Ichiro Kudo
Journal:  Biochim Biophys Acta       Date:  2003-11-30
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  16 in total

Review 1.  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

2.  In vitro anti-Plasmodium falciparum properties of the full set of human secreted phospholipases A2.

Authors:  Carole Guillaume; Christine Payré; Ikram Jemel; Louise Jeammet; Sofiane Bezzine; Gajendra S Naika; James Bollinger; Philippe Grellier; Michael H Gelb; Joseph Schrével; Gérard Lambeau; Christiane Deregnaucourt
Journal:  Infect Immun       Date:  2015-03-30       Impact factor: 3.441

3.  Biochemical characterization of selective inhibitors of human group IIA secreted phospholipase A(2) and hyaluronic acid-linked inhibitor conjugates.

Authors:  Rob C Oslund; Michael H Gelb
Journal:  Biochemistry       Date:  2012-10-18       Impact factor: 3.162

4.  Group X phospholipase A2 is released during sperm acrosome reaction and controls fertility outcome in mice.

Authors:  Jessica Escoffier; Ikram Jemel; Akemi Tanemoto; Yoshitaka Taketomi; Christine Payre; Christelle Coatrieux; Hiroyasu Sato; Kei Yamamoto; Seiko Masuda; Karin Pernet-Gallay; Virginie Pierre; Shuntaro Hara; Makoto Murakami; Michel De Waard; Gérard Lambeau; Christophe Arnoult
Journal:  J Clin Invest       Date:  2010-04-26       Impact factor: 14.808

5.  Blockade of human group X secreted phospholipase A2 (GX-sPLA2)-induced airway inflammation and hyperresponsiveness in a mouse asthma model by a selective GX-sPLA2 inhibitor.

Authors:  William R Henderson; Rob C Oslund; James G Bollinger; Xin Ye; Ying-Tzang Tien; Jun Xue; Michael H Gelb
Journal:  J Biol Chem       Date:  2011-06-07       Impact factor: 5.157

6.  Total synthesis of thiaplakortone a: derivatives as metabolically stable leads for the treatment of malaria.

Authors:  Rebecca H Pouwer; Sophie M Deydier; Phuc Van Le; Brett D Schwartz; Nicole C Franken; Rohan A Davis; Mark J Coster; Susan A Charman; Michael D Edstein; Tina S Skinner-Adams; Katherine T Andrews; Ian D Jenkins; Ronald J Quinn
Journal:  ACS Med Chem Lett       Date:  2013-12-27       Impact factor: 4.345

7.  Discovery of a Series of Indole-2 Carboxamides as Selective Secreted Phospholipase A2 Type X (sPLA2-X) Inhibitors.

Authors:  Laurent Knerr; Fabrizio Giordanetto; Peter Nordberg; Daniel Pettersen; Nidhal Selmi; Hans-Georg Beisel; Hannah de la Motte; Thomas Olsson; Tim D J Perkins; Margareta Herslöf; Åsa Månsson; Mikael Dahlström; Ingemar Starke; Johan Broddefalk; Gabrielle Saarinen; Fredrik Klingegård; Eva Hurt-Camejo; Birgitta Rosengren; Johan Brengdahl; Frank Jansen; Mattias Rohman; Jenny Sandmark; Kenth Hallberg; Tomas Åkerud; Robert G Roth; Marie Ahlqvist
Journal:  ACS Med Chem Lett       Date:  2018-06-23       Impact factor: 4.345

8.  Group X phospholipase A2 stimulates the proliferation of colon cancer cells by producing various lipid mediators.

Authors:  Fanny Surrel; Ikram Jemel; Eric Boilard; James G Bollinger; Christine Payré; Carine M Mounier; Kati A Talvinen; Veli J O Laine; Timo J Nevalainen; Michael H Gelb; Gérard Lambeau
Journal:  Mol Pharmacol       Date:  2009-07-14       Impact factor: 4.436

9.  Development of a potent 2-oxoamide inhibitor of secreted phospholipase A2 guided by molecular docking calculations and molecular dynamics simulations.

Authors:  Sofia Vasilakaki; Efrosini Barbayianni; Georgios Leonis; Manthos G Papadopoulos; Thomas Mavromoustakos; Michael H Gelb; George Kokotos
Journal:  Bioorg Med Chem       Date:  2016-03-02       Impact factor: 3.641

10.  Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2.

Authors:  Rob C Oslund; Nathan Cermak; Michael H Gelb
Journal:  J Med Chem       Date:  2008-07-08       Impact factor: 7.446
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