Literature DB >> 22450967

The aminopeptidase inhibitor CHR-2863 is an orally bioavailable inhibitor of murine malaria.

Tina S Skinner-Adams1, Christopher L Peatey, Karen Anderson, Katharine R Trenholme, David Krige, Christopher L Brown, Colin Stack, Desire M M Nsangou, Rency T Mathews, Karine Thivierge, John P Dalton, Donald L Gardiner.   

Abstract

Malaria remains a significant risk in many areas of the world, with resistance to the current antimalarial pharmacopeia an ever-increasing problem. The M1 alanine aminopeptidase (PfM1AAP) and M17 leucine aminopeptidase (PfM17LAP) are believed to play a role in the terminal stages of digestion of host hemoglobin and thereby generate a pool of free amino acids that are essential for parasite growth and development. Here, we show that an orally bioavailable aminopeptidase inhibitor, CHR-2863, is efficacious against murine malaria.

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Year:  2012        PMID： 22450967      PMCID： PMC3370795          DOI： 10.1128/AAC.06245-11

Source DB:  PubMed          Journal:  Antimicrob Agents Chemother        ISSN： 0066-4804            Impact factor:   5.191


  35 in total

1.  Potent inhibitors of the Plasmodium falciparum enzymes plasmepsin I and II devoid of cathepsin D inhibitory activity.

Authors:  Karolina Ersmark; Isabella Feierberg; Sinisa Bjelic; Elizabeth Hamelink; Fiona Hackett; Michael J Blackman; Johan Hultén; Bertil Samuelsson; Johan Aqvist; Anders Hallberg
Journal:  J Med Chem       Date:  2004-01-01       Impact factor: 7.446

2.  Excess haemoglobin digestion by malaria parasites: a strategy to prevent premature host cell lysis.

Authors:  Virgilio L Lew; Lynn Macdonald; Hagai Ginsburg; Miriam Krugliak; Teresa Tiffert
Journal:  Blood Cells Mol Dis       Date:  2004 May-Jun       Impact factor: 3.039

3.  Glide: a new approach for rapid, accurate docking and scoring. 2. Enrichment factors in database screening.

Authors:  Thomas A Halgren; Robert B Murphy; Richard A Friesner; Hege S Beard; Leah L Frye; W Thomas Pollard; Jay L Banks
Journal:  J Med Chem       Date:  2004-03-25       Impact factor: 7.446

4.  Glide: a new approach for rapid, accurate docking and scoring. 1. Method and assessment of docking accuracy.

Authors:  Richard A Friesner; Jay L Banks; Robert B Murphy; Thomas A Halgren; Jasna J Klicic; Daniel T Mainz; Matthew P Repasky; Eric H Knoll; Mee Shelley; Jason K Perry; David E Shaw; Perry Francis; Peter S Shenkin
Journal:  J Med Chem       Date:  2004-03-25       Impact factor: 7.446

5.  Analysis of antimalarial synergy between bestatin and endoprotease inhibitors using statistical response-surface modelling.

Authors:  C S Gavigan; S G Machado; J P Dalton; A Bell
Journal:  Antimicrob Agents Chemother       Date:  2001-11       Impact factor: 5.191

Review 6.  Malaria in pregnancy and the endemicity spectrum: what can we learn?

Authors:  François Nosten; Stephen J Rogerson; James G Beeson; Rose McGready; Theonest K Mutabingwa; Bernard Brabin
Journal:  Trends Parasitol       Date:  2004-09

7.  Human malaria parasites in continuous culture.

Authors:  W Trager; J B Jensen
Journal:  Science       Date:  1976-08-20       Impact factor: 47.728

8.  Randomized double-blind placebo-controlled trial of bestatin in patients with resected stage I squamous-cell lung carcinoma.

Authors:  Yukito Ichinose; Keiichiro Genka; Teruaki Koike; Harubumi Kato; Yoh Watanabe; Takashi Mori; Sogo Iioka; Akira Sakuma; Mitsuo Ohta
Journal:  J Natl Cancer Inst       Date:  2003-04-16       Impact factor: 13.506

9.  Computer-aided design and synthesis of nonpeptidic plasmepsin II and IV inhibitors.

Authors:  Torsten Luksch; Nan-Si Chan; Sascha Brass; Christoph A Sotriffer; Gerhard Klebe; Wibke E Diederich
Journal:  ChemMedChem       Date:  2008-09       Impact factor: 3.466

10.  The most potent organophosphorus inhibitors of leucine aminopeptidase. Structure-based design, chemistry, and activity.

Authors:  Jolanta Grembecka; Artur Mucha; Tomasz Cierpicki; Paweł Kafarski
Journal:  J Med Chem       Date:  2003-06-19       Impact factor: 7.446
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  9 in total

1.  Structural characterization of plasmodial aminopeptidase: a combined molecular docking and QSAR-based in silico approaches.

Authors:  Fangfang Wang; Xiaojun Hu; Bo Zhou
Journal:  Mol Divers       Date:  2019-02-07       Impact factor: 2.943

2.  Genetic and chemical validation of Plasmodium falciparum aminopeptidase PfA-M17 as a drug target in the hemoglobin digestion pathway.

Authors:  Rebecca C S Edgar; Ghizal Siddiqui; Katheryn Hjerrild; Tess R Malcolm; Natalie B Vinh; Chaille T Webb; Clare Holmes; Christopher A MacRaild; Hope C Chernih; Willy W Suen; Natalie A Counihan; Darren J Creek; Peter J Scammells; Sheena McGowan; Tania F de Koning-Ward
Journal:  Elife       Date:  2022-09-13       Impact factor: 8.713

3.  Screening the Medicines for Malaria Venture "Malaria Box" against the Plasmodium falciparum aminopeptidases, M1, M17 and M18.

Authors:  Alessandro Paiardini; Rebecca S Bamert; Komagal Kannan-Sivaraman; Nyssa Drinkwater; Shailesh N Mistry; Peter J Scammells; Sheena McGowan
Journal:  PLoS One       Date:  2015-02-20       Impact factor: 3.240

4.  Selective inhibition of PfA-M1, over PfA-M17, by an amino-benzosuberone derivative blocks malaria parasites development in vitro and in vivo.

Authors:  Lotfi Bounaadja; Marjorie Schmitt; Sébastien Albrecht; Elisabeth Mouray; Céline Tarnus; Isabelle Florent
Journal:  Malar J       Date:  2017-09-21       Impact factor: 2.979

Review 5.  M1 aminopeptidases as drug targets: broad applications or therapeutic niche?

Authors:  Nyssa Drinkwater; Jisook Lee; Wei Yang; Tess R Malcolm; Sheena McGowan
Journal:  FEBS J       Date:  2017-02-03       Impact factor: 5.542

6.  Biochemical and cellular characterisation of the Plasmodium falciparum M1 alanyl aminopeptidase (PfM1AAP) and M17 leucyl aminopeptidase (PfM17LAP).

Authors:  Rency Mathew; Juliane Wunderlich; Karine Thivierge; Krystyna Cwiklinski; Claire Dumont; Leann Tilley; Petra Rohrbach; John P Dalton
Journal:  Sci Rep       Date:  2021-02-03       Impact factor: 4.379

7.  Sitagliptin does not inhibit the M1 alanyl aminopeptidase from Plasmodium falciparum.

Authors:  Sheena McGowan
Journal:  Bioinformation       Date:  2013-07-17

8.  Multifactorial resistance to aminopeptidase inhibitor prodrug CHR2863 in myeloid leukemia cells: down-regulation of carboxylesterase 1, drug sequestration in lipid droplets and pro-survival activation ERK/Akt/mTOR.

Authors:  Sue Ellen Verbrugge; Marjon Al; Yehuda G Assaraf; Sarah Kammerer; Durga M S H Chandrupatla; Richard Honeywell; Rene P J Musters; Elisa Giovannetti; Tom O'Toole; George L Scheffer; David Krige; Tanja D de Gruijl; Hans W M Niessen; Willem F Lems; Pieternella A Kramer; Rik J Scheper; Jacqueline Cloos; Gert J Ossenkoppele; Godefridus J Peters; Gerrit Jansen
Journal:  Oncotarget       Date:  2016-02-02

Review 9.  Driving antimalarial design through understanding of target mechanism.

Authors:  Petar P S Calic; Mahta Mansouri; Peter J Scammells; Sheena McGowan
Journal:  Biochem Soc Trans       Date:  2020-10-30       Impact factor: 5.407
  9 in total

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