Literature DB >> 9034754

The antiviral, antitumoural xanthate D609 is a competitive inhibitor of phosphatidylcholine-specific phospholipase C.

E Amtmann1.   

Abstract

The effect of the antiviral, antitumoural xanthate D609 on the activity of phospholipase A2, C (PC- and Pi-specific) and D was investigated. D609 is the first model substance of a new concept of antiviral therapy that interferes with cellular regulation mechanisms, rather than with virus coded enzymes. Exclusively phosphatidylcholine (PC) specific phospholipase C (PC-PLC) was found to be inhibited in a dose-dependent manner. Enzyme activity was determined either as the rate of acid release from PC or as the rate of phosphorylcholine production form 3H labelled PC. Lineweaver-Burk plots revealed D609 as a competitive inhibitor of PC-PLC with a Ki of 6.4 microM. In addition, D609 competitively inhibited PC-PLC mediated cleavage of P-nitrophenylphosphorylcholine (p-NPP), a pseudo-substrate of PC-PLC with a Ki of 8.8 microM. These data suggest that D609 competes with the phosphorylcholine residue of PC for binding to PC-PLC.

Entities:  

Mesh：

Substances：

Year:  1996        PMID： 9034754

Source DB:  PubMed          Journal:  Drugs Exp Clin Res        ISSN： 0378-6501


  37 in total

1.  Phosphatidylcholine-specific phospholipase C and phospholipase D are respectively implicated in mitogen-activated protein kinase and nuclear factor kappaB activation in tumour-necrosis-factor-alpha-treated immature acute-myeloid-leukaemia cells.

Authors:  I Plo; D Lautier; T Levade; H Sekouri; J P Jaffrézou; G Laurent; A Bettaïeb
Journal:  Biochem J       Date:  2000-10-15       Impact factor: 3.857

2.  Sphingomyelin is sorted at the trans Golgi network into a distinct class of secretory vesicle.

Authors:  Yongqiang Deng; Felix E Rivera-Molina; Derek K Toomre; Christopher G Burd
Journal:  Proc Natl Acad Sci U S A       Date:  2016-05-31       Impact factor: 11.205

3.  Synthetic FXR agonist GW4064 is a modulator of multiple G protein-coupled receptors.

Authors:  Nidhi Singh; Manisha Yadav; Abhishek Kumar Singh; Harish Kumar; Shailendra Kumar Dhar Dwivedi; Jay Sharan Mishra; Anagha Gurjar; Amit Manhas; Sharat Chandra; Prem Narayan Yadav; Kumaravelu Jagavelu; Mohammad Imran Siddiqi; Arun Kumar Trivedi; Naibedya Chattopadhyay; Sabyasachi Sanyal
Journal:  Mol Endocrinol       Date:  2014-03-05

Review 4.  Chemical modulation of glycerolipid signaling and metabolic pathways.

Authors:  Sarah A Scott; Thomas P Mathews; Pavlina T Ivanova; Craig W Lindsley; H Alex Brown
Journal:  Biochim Biophys Acta       Date:  2014-01-15

5.  In vivo detection of phospholipase C by enzyme-activated near-infrared probes.

Authors:  Theresa M Mawn; Anatoliy V Popov; Nancy J Beardsley; Klara Stefflova; Matthew Milkevitch; Gang Zheng; E James Delikatny
Journal:  Bioconjug Chem       Date:  2011-11-29       Impact factor: 4.774

6.  Synthesis and phospholipase C inhibitory activity of D609 diastereomers.

Authors:  Albert González-Roura; Josefina Casas; Amadeu Llebaria
Journal:  Lipids       Date:  2002-04       Impact factor: 1.880

7.  In vivo administration of D609 leads to protection of subsequently isolated gerbil brain mitochondria subjected to in vitro oxidative stress induced by amyloid beta-peptide and other oxidative stressors: relevance to Alzheimer's disease and other oxidative stress-related neurodegenerative disorders.

Authors:  Mubeen Ahmad Ansari; Gururaj Joshi; Quanzhen Huang; Wycliffe O Opii; Hafiz Mohmmad Abdul; Rukhsana Sultana; D Allan Butterfield
Journal:  Free Radic Biol Med       Date:  2006-09-08       Impact factor: 7.376

8.  Persistent activation of RelA by respiratory syncytial virus involves protein kinase C, underphosphorylated IkappaBbeta, and sequestration of protein phosphatase 2A by the viral phosphoprotein.

Authors:  V Bitko; S Barik
Journal:  J Virol       Date:  1998-07       Impact factor: 5.103

9.  Phosphatidylcholine-specific phospholipase C activation is required for CCR5-dependent, NF-kB-driven CCL2 secretion elicited in response to HIV-1 gp120 in human primary macrophages.

Authors:  Laura Fantuzzi; Francesca Spadaro; Cristina Purificato; Serena Cecchetti; Franca Podo; Filippo Belardelli; Sandra Gessani; Carlo Ramoni
Journal:  Blood       Date:  2008-01-18       Impact factor: 22.113

10.  Involvement of a phospholipase C in the hemolytic activity of a clinical strain of Pseudomonas fluorescens.

Authors:  Gaelle Rossignol; Annabelle Merieau; Josette Guerillon; Wilfried Veron; Olivier Lesouhaitier; Marc G J Feuilloley; Nicole Orange
Journal:  BMC Microbiol       Date:  2008-10-30       Impact factor: 3.605
View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.