Literature DB >> 30996801

Covalent Inhibitors of Plasmodium falciparum Glyceraldehyde 3-Phosphate Dehydrogenase with Antimalarial Activity in Vitro.

Gregorio Cullia1, Stefano Bruno2, Silvia Parapini3, Marilena Margiotta2, Lucia Tamborini1, Andrea Pinto4, Andrea Galbiati1, Andrea Mozzarelli2, Marco Persico5, Antonella Paladino6, Caterina Fattorusso5, Donatella Taramelli7, Paola Conti1.   

Abstract

Covalent inhibitors of PfGAPDH characterized by a 3-bromoisoxazoline warhead were developed, and their mode of interaction with the target enzyme was interpreted by means of molecular modeling studies: some of them displayed a submicromolar antiplasmodial activity against both chloroquine sensitive and resistant strains of Plasmodium falciparum, with good selectivity indices.

Entities:  

Year:  2019        PMID： 30996801      PMCID： PMC6466836          DOI： 10.1021/acsmedchemlett.8b00592

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  26 in total

Review 1.  Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings.

Authors:  C A Lipinski; F Lombardo; B W Dominy; P J Feeney
Journal:  Adv Drug Deliv Rev       Date:  2001-03-01       Impact factor: 15.470

Review 2.  Membrane transport in the malaria-infected erythrocyte.

Authors:  K Kirk
Journal:  Physiol Rev       Date:  2001-04       Impact factor: 37.312

3.  Esters of methanesulfonic acid as irreversible inhibitors of acetylcholinesterase.

Authors:  R KITZ; I B WILSON
Journal:  J Biol Chem       Date:  1962-10       Impact factor: 5.157

4.  The role of sulfhydryl groups in the activity of D-glyceraldehyde 3-phosphate dehydrogenase.

Authors:  H L SEGAL; P D BOYER
Journal:  J Biol Chem       Date:  1953-09       Impact factor: 5.157

5.  Crystal structure of glyceraldehyde-3-phosphate dehydrogenase from Plasmodium falciparum at 2.25 A resolution reveals intriguing extra electron density in the active site.

Authors:  Mark A Robien; Jürgen Bosch; Frederick S Buckner; Wesley C E Van Voorhis; Elizabeth A Worthey; Peter Myler; Christopher Mehlin; Erica E Boni; Oleksandr Kalyuzhniy; Lori Anderson; Angela Lauricella; Stacy Gulde; Joseph R Luft; George DeTitta; Jonathan M Caruthers; Keith O Hodgson; Michael Soltis; Frank Zucker; Christophe L M J Verlinde; Ethan A Merritt; Lori W Schoenfeld; Wim G J Hol
Journal:  Proteins       Date:  2006-03-15

6.  Trapping of the thioacylglyceraldehyde-3-phosphate dehydrogenase intermediate from Bacillus stearothermophilus. Direct evidence for a flip-flop mechanism.

Authors:  Sébastien Moniot; Stefano Bruno; Clemens Vonrhein; Claude Didierjean; Sandrine Boschi-Muller; Mária Vas; Gérard Bricogne; Guy Branlant; Andrea Mozzarelli; Catherine Corbier
Journal:  J Biol Chem       Date:  2008-05-14       Impact factor: 5.157

7.  Structure of glyceraldehyde-3-phosphate dehydrogenase from Plasmodium falciparum.

Authors:  Jacqueline F Satchell; Robyn L Malby; Cindy S Luo; Akinola Adisa; Aysun E Alpyurek; Nectarios Klonis; Brian J Smith; Leann Tilley; Peter M Colman
Journal:  Acta Crystallogr D Biol Crystallogr       Date:  2005-08-16

8.  Synthesis and biological evaluation of new amino acids structurally related to the antitumor agent acivicin.

Authors:  Paola Conti; Gabriella Roda; Helena Stabile; Maria Antonietta Vanoni; Bruno Curti; Marco De Amici
Journal:  Farmaco       Date:  2003-09

9.  Synthesis and pharmacological characterization at glutamate receptors of the four enantiopure isomers of tricholomic acid.

Authors:  Andrea Pinto; Paola Conti; Marco De Amici; Lucia Tamborini; Ulf Madsen; Birgitte Nielsen; Thomas Christesen; Hans Bräuner-Osborne; Carlo De Micheli
Journal:  J Med Chem       Date:  2008-03-14       Impact factor: 7.446

10.  Evidence for the two phosphate binding sites of an analogue of the thioacyl intermediate for the Trypanosoma cruzi glyceraldehyde-3-phosphate dehydrogenase-catalyzed reaction, from its crystal structure.

Authors:  Marcelo S Castilho; Fernando Pavão; Glaucius Oliva; Sylvain Ladame; Michèle Willson; Jacques Périé
Journal:  Biochemistry       Date:  2003-06-17       Impact factor: 3.162
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  1 in total

1.  3-Bromo-Isoxazoline Derivatives Inhibit GAPDH Enzyme in PDAC Cells Triggering Autophagy and Apoptotic Cell Death.

Authors:  Raffaella Pacchiana; Nidula Mullappilly; Andrea Pinto; Stefania Bova; Stefania Forciniti; Gregorio Cullia; Elisa Dalla Pozza; Emanuela Bottani; Ilaria Decimo; Ilaria Dando; Stefano Bruno; Paola Conti; Massimo Donadelli
Journal:  Cancers (Basel)       Date:  2022-06-27       Impact factor: 6.575
  1 in total

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