Literature DB >> 7088033

Mechanism of action of MK-401 against Fasciola hepatica: inhibition of phosphoglycerate kinase.

M D Schulman, D A Ostlind, D Valentino.   

Abstract

The effect of MK-401 (4-amino-6-trichloroethenyl 1,3-benzenedisulfonamide) on Fasciola hepatica phosphoglycerate kinase (EC 2.7.2.3) was investigated. MK-401 was a competitive inhibitor of both 3-phosphoglycerate and ATP and had a Ki of 0.29 mM. ATP, 1,3-diphosphoglycerate and MK-401 protected the Fasciola enzyme from inhibition by N-ethylmaleimide. Analogues of MK-401 with different substituents at the 6 position (R = Cl, CF3, C2 F3, C3 F7) were competitive inhibitors of both 3-phosphoglycerate and ATP and a good correlation between the Ki and in vivo activity of these analogues was observed.

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Year:  1982        PMID： 7088033     DOI： 10.1016/0166-6851(82)90016-0

Source DB:  PubMed          Journal:  Mol Biochem Parasitol        ISSN： 0166-6851            Impact factor:   1.759


  8 in total

1.  Fasciola hepatica: effects of the fasciolicide clorsulon in vitro and in vivo on the tegumental surface, and a comparison of the effects on young- and old-mature flukes.

Authors:  M Meaney; I Fairweather; G P Brennan; L S L McDowell; A B Forbes
Journal:  Parasitol Res       Date:  2003-08-22       Impact factor: 2.289

2.  TOMOCOMD-CARDD, a novel approach for computer-aided 'rational' drug design: I. Theoretical and experimental assessment of a promising method for computational screening and in silico design of new anthelmintic compounds.

Authors:  Yovani Marrero-Ponce; Juan A Castillo-Garit; Ervelio Olazabal; Hector S Serrano; Alcidez Morales; Nilo Castañedo; Froylán Ibarra-Velarde; Alma Huesca-Guillen; Elisa Jorge; Arletys del Valle; Francisco Torrens; Eduardo A Castro
Journal:  J Comput Aided Mol Des       Date:  2004-10       Impact factor: 3.686

3.  A cell-based phenotypic assay to identify cardioprotective agents.

Authors:  Stephanie Guo; Adam Olm-Shipman; Andrew Walters; William R Urciuoli; Stefanie Devito; Sergiy M Nadtochiy; Andrew P Wojtovich; Paul S Brookes
Journal:  Circ Res       Date:  2012-03-06       Impact factor: 17.367

4.  Ultrastructural observations on oral ingestion and trans-tegumental uptake of clorsulon by the liver fluke, Fasciola hepatica.

Authors:  M Meaney; S Haughey; G P Brennan; I Fairweather
Journal:  Parasitol Res       Date:  2005-01-06       Impact factor: 2.289

5.  In vitro efficacy of triclabendazole and clorsulon against the larval stage of Echinococcus multilocularis.

Authors:  David Richter; Joachim Richter; Beate Grüner; Kathrin Kranz; Juliane Franz; Peter Kern
Journal:  Parasitol Res       Date:  2013-02-28       Impact factor: 2.289

6.  Transmission electron microscope study of the ultrastructural changes induced in the tegument and gut of Fasciola hepatica following in vivo drug treatment with clorsulon.

Authors:  M Meaney; I Fairweather; G P Brennan; A B Forbes
Journal:  Parasitol Res       Date:  2004-01-09       Impact factor: 2.289

7.  In vitro and in vivo effects of 3-bromopyruvate against Echinococcus metacestodes.

Authors:  Qi Xin; Miaomiao Yuan; Huanping Li; Xiaoxia Song; Jun Lu; Tao Jing
Journal:  Vet Res       Date:  2019-11-19       Impact factor: 3.683

8.  Inhibition of Schistosoma mansoni carbonic anhydrase by the antiparasitic drug clorsulon: X-ray crystallographic and in vitro studies.

Authors:  Marta Ferraroni; Andrea Angeli; Simone Carradori; Claudiu T Supuran
Journal:  Acta Crystallogr D Struct Biol       Date:  2022-02-18       Impact factor: 7.652
  8 in total

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