Literature DB >> 11206479

A disubstituted NAD+ analogue is a nanomolar inhibitor of trypanosomal glyceraldehyde-3-phosphate dehydrogenase.

K J Kennedy1, J C Bressi, M H Gelb.   

Abstract

N6-Naphthalenemethyl-2'-methoxybenzamido-beta-NAD+, a derivative of a low micromolar first-generation inhibitor of trypanosomal glyceraldehyde phosphate dehydrogenase (GAPDH), was synthesized, taking advantage of methodology for the selective phosphitylation of nucleosides. The compound was found to be a poor alternate cosubstrate for GAPDH, but an extremely potent inhibitor. Although intended for use in crystallization trials, the analogue presents possibilities for further drug design.

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Year:  2001        PMID: 11206479     DOI: 10.1016/s0960-894x(00)00608-9

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


  7 in total

Review 1.  Combinatorial chemistry as a new approach in antiparasitic drug discovery.

Authors:  Andreas Link
Journal:  Parasitol Res       Date:  2003-05-07       Impact factor: 2.289

2.  Parallel synthesis of a series of non-functional ATP/NAD analogs with activity against trypanosomatid parasites.

Authors:  Andreas Link; Philipp Heidler; Marcel Kaiser; Reto Brun
Journal:  Mol Divers       Date:  2009-05-30       Impact factor: 2.943

3.  Homology modeling and molecular dynamics study of NAD-dependent glycerol-3-phosphate dehydrogenase from Trypanosoma brucei rhodesiense, a potential target enzyme for anti-sleeping sickness drug development.

Authors:  Igor Z Zubrzycki
Journal:  Biophys J       Date:  2002-06       Impact factor: 4.033

4.  Shikonin, vitamin K3 and vitamin K5 inhibit multiple glycolytic enzymes in MCF-7 cells.

Authors:  Jing Chen; Xun Hu; Jingjie Cui
Journal:  Oncol Lett       Date:  2018-03-13       Impact factor: 2.967

5.  Crystal Structure of Glyceraldehyde-3-Phosphate Dehydrogenase from the Gram-Positive Bacterial Pathogen A. vaginae, an Immunoevasive Factor that Interacts with the Human C5a Anaphylatoxin.

Authors:  Javier Querol-García; Francisco J Fernández; Ana V Marin; Sara Gómez; Daniel Fullà; Cecilia Melchor-Tafur; Virginia Franco-Hidalgo; Sebastián Albertí; Jordi Juanhuix; Santiago Rodríguez de Córdoba; José R Regueiro; M Cristina Vega
Journal:  Front Microbiol       Date:  2017-04-10       Impact factor: 5.640

6.  Combining tubercidin and cordycepin scaffolds results in highly active candidates to treat late-stage sleeping sickness.

Authors:  Fabian Hulpia; Dorien Mabille; Gustavo D Campagnaro; Gabriela Schumann; Louis Maes; Isabel Roditi; Anders Hofer; Harry P de Koning; Guy Caljon; Serge Van Calenbergh
Journal:  Nat Commun       Date:  2019-12-05       Impact factor: 14.919

7.  Antibody-free colorimetric detection of chlorothalonil in cucumber via the inhibition of an enzyme-triggered reaction.

Authors:  Qingju Liu; Ping Han; Hui Wang; Wenwen Gong; Xiaoyuan Feng
Journal:  RSC Adv       Date:  2019-03-29       Impact factor: 3.361

  7 in total

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