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Sequence homology and structural analysis of plasmepsin 4 isolated from Indian Plasmodium vivax isolates

June 1, 2011 - 14:20 -- Patrick Sampao
Manmeet Rawat, Sonam Vijay, Yash Gupta, Rajnikant Dixit, P.K. Tiwari, Arun Sharma
Infection, Genetics and Evolution, Volume 11, Issue 5, July 2011, Pages 924-933

This is the first report detailing complete PM4 gene analysis from Indian P. vivax isolates. Blast results of sequences of P. vivax plasmepsin 4 (PvPM4) shows 100% homology among isolates of P. vivax collected from different geographical regions of India.

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Improvement of both plasmepsin inhibitory activity and antimalarial activity by 2-aminoethylamino substitution

July 28, 2010 - 07:56 -- Kabogo Ndegwa
Takuya Miura, Koushi Hidaka, Tsuyoshi Uemura, Keisuke Kashimoto, Yuto Hori, Yuko Kawasaki, Adam J. Ruben, Ernesto Freire, Tooru Kimura, Yoshiaki Kiso
Bioorganic & Medicinal Chemistry Letters, Volume 20, Issue 16, 15 August 2010, Pages 4836-4839

We attached 2-aminoethylamino groups to allophenylnorstatine-containing plasmepsin (Plm) inhibitors and investigated SAR of the methyl or ethyl substitutions on the amino groups. Unexpectedly, compounds 22 (KNI-10743) and 25 (KNI-10742) exhibited extremely potent Plm II inhibitory activities (Ki <0.1 nM).

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Distillery: Therapeutic: Plasmepsin (Plasmodium falciparum)

October 25, 2009 - 17:01 -- Bart G.J. Knols
Science-Business eXchange 2, (15 October 2009) doi:10.1038/scibx.2009.1508

In vitro studies identified a plasmepsin inhibitor that could aid in the development of new treatments for malaria. Further details on the research, next steps and licensing status are discussed in the article.


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