Journal of medicinal and pharmaceutical chemistry 2013-06-27

Synthesis and structure-activity relationships of phosphonic arginine mimetics as inhibitors of the M1 and M17 aminopeptidases from Plasmodium falciparum.

Komagal Kannan Sivaraman, Alessandro Paiardini, Marcin Sieńczyk, Chiara Ruggeri, Christine A Oellig, John P Dalton, Peter J Scammells, Marcin Drag, Sheena McGowan

文献索引：J. Med. Chem. 56(12) , 5213-7, (2013)

全文：HTML全文

摘要

The malaria parasite Plasmodium falciparum employs two metallo-aminopeptidases, PfA-M1 and PfA-M17, which are essential for parasite survival. Compounds that inhibit the activity of either enzyme represent leads for the development of new antimalarial drugs. Here we report the synthesis and structure-activity relationships of a small library of phosphonic acid arginine mimetics that probe the S1 pocket of both enzymes and map the necessary interactions that would be important for a dual inhibitor.

相关化合物

  • L-精氨酸
  • 亮氨酸氨基肽酶,微...

相关文献：

Hepatitis E virus (HEV) protease: a chymotrypsin-like enzyme that processes both non-structural (pORF1) and capsid (pORF2) protein.

2014-08-01

[J. Gen. Virol. 95(Pt 8) , 1689-700, (2014)]

Mechanistic studies on the flavin-dependent N⁶-lysine monooxygenase MbsG reveal an unusual control for catalysis.

2014-05-15

[Arch. Biochem. Biophys. 550-551 , 58-66, (2014)]

Sustained Arginase 1 Expression Modulates Pathological Tau Deposits in a Mouse Model of Tauopathy.

2015-11-04

[J. Neurosci. 35 , 14842-60, (2015)]

Down regulation of NO signaling in Trypanosoma cruzi upon parasite-extracellular matrix interaction: changes in protein modification by nitrosylation and nitration.

2015-04-01

[PLoS Negl. Trop. Dis. 9 , e0003683, (2015)]

Cmr1/WDR76 defines a nuclear genotoxic stress body linking genome integrity and protein quality control.

2015-01-01

[Nat. Commun. 6 , 6533, (2015)]

更多文献...