Literature DB >> 9873534

Identification of potent inhibitors of Plasmodium falciparum plasmepsin II from an encoded statine combinatorial library.

C D Carroll1, H Patel, T O Johnson, T Guo, M Orlowski, Z M He, C L Cavallaro, J Guo, A Oksman, I Y Gluzman, J Connelly, D Chelsky, D E Goldberg, R E Dolle.   

Abstract

An encoded 13,020-member combinatorial library was synthesized containing a statine core. Evaluation of this library with plasmepsin II, an aspartyl protease required for hemoglobin metabolism in the malaria parasite, led to the identification of potent and selective inhibitors as well as novel structure-activity relationships.

Entities:  

Mesh:

Substances:

Year:  1998        PMID: 9873534     DOI: 10.1016/s0960-894x(98)00419-3

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


  13 in total

1.  Analysis of libraries encoded with GC tags: compound elution, tag decode analysis, and statistical sampling analysis.

Authors:  R E Dolle; J Guo; W Li; N Zhao; J A Connelly
Journal:  Mol Divers       Date:  2000       Impact factor: 2.943

Review 2.  Combinatorial chemistry as a new approach in antiparasitic drug discovery.

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

3.  Improved prediction of malaria degradomes by supervised learning with SVM and profile kernel.

Authors:  Rui Kuang; Jianying Gu; Hong Cai; Yufeng Wang
Journal:  Genetica       Date:  2008-12-06       Impact factor: 1.082

4.  Structures of plasmepsin II from Plasmodium falciparum in complex with two hydroxyethylamine-based inhibitors.

Authors:  Rosario Recacha; Janis Leitans; Inara Akopjana; Lilija Aprupe; Peteris Trapencieris; Kristaps Jaudzems; Aigars Jirgensons; Kaspars Tars
Journal:  Acta Crystallogr F Struct Biol Commun       Date:  2015-11-27       Impact factor: 1.056

5.  Computational analysis of aspartic protease plasmepsin II complexed with EH58 inhibitor: a QM/MM MD study.

Authors:  Natália de Farias Silva; Jerônimo Lameira; Cláudio Nahum Alves
Journal:  J Mol Model       Date:  2011-01-25       Impact factor: 1.810

6.  Four plasmepsins are active in the Plasmodium falciparum food vacuole, including a protease with an active-site histidine.

Authors:  Ritu Banerjee; Jun Liu; Wandy Beatty; Lorraine Pelosof; Michael Klemba; Daniel E Goldberg
Journal:  Proc Natl Acad Sci U S A       Date:  2002-01-08       Impact factor: 11.205

Review 7.  Structural studies of vacuolar plasmepsins.

Authors:  Prasenjit Bhaumik; Alla Gustchina; Alexander Wlodawer
Journal:  Biochim Biophys Acta       Date:  2011-04-20

8.  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

9.  Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin.

Authors:  Koushi Hidaka; Tooru Kimura; Adam J Ruben; Tsuyoshi Uemura; Mami Kamiya; Aiko Kiso; Tetsuya Okamoto; Yumi Tsuchiya; Yoshio Hayashi; Ernesto Freire; Yoshiaki Kiso
Journal:  Bioorg Med Chem       Date:  2008-10-10       Impact factor: 3.641

10.  Comparative Genomics and Systems Biology of Malaria Parasites Plasmodium.

Authors:  Hong Cai; Zhan Zhou; Jianying Gu; Yufeng Wang
Journal:  Curr Bioinform       Date:  2012-12-01       Impact factor: 3.543

View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.