Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDR00106

Target Information
NamePlasmepsin 2    
Type of targetResearch target    
SynonymsAspartic hemoglobinase II    
PFAPD    
Plasmepsin II    
DiseaseHuman immunodeficiency virus [HIV] disease
[ICD9: 279.3   ICD10: D84.9]
[1]
Malaria
[ICD9: 084   ICD10: B50-B54]
[2][3][4]
Parasitic diseases[1]
BioChemical ClassHydrolases acting on peptide bonds (Peptidases)    
EC NumberEC 3.4.23.39
UniProt IDP46925
PDB Structure1J8J; 1LEE; 1LF2; 1LF3; 1LF4; 1M43; 1ME6; 1PFZ.    
SequenceMDITVREHDFKHGFIKSNSTFDGLNIDNSKNKKKIQKGFQILYVLLFCSVMCGLFYYVYE NVWLQRDNEMNEILKNSEHLTIGFKVENAHDRILKTIKTHKLKNYIKESVNFLNSGLTKT NYLGSSNDNIELVDFQNIMFYGDAEVGDNQQPFTFILDTGSANLWVPSVKCTTAGCLTKH LYDSSKSRTYEKDGTKVEMNYVSGTVSGFFSKDLVTVGNLSLPYKFIEVIDTNGFEPTYT ASTFDGILGLGWKDLSIGSVDPIVVELKNQNKIENALFTFYLPVHDKHTGFLTIGGIEER FYEGPLTYEKLNHDLYWQITLDAHVGNIMLEKANCIVDSGTSAITVPTDFLNKMLQNLDV IKVPFLPFYVTLCNNSKLPTFEFTSENGKYTLEPEYYLQHIEDVGPGLCMLNIIGLDFPV PTFILGDPFMRKYFTVFDYDNHSVGIALAKKNL
Related US Patent6,326,393
6,432,933
Target ValidationClick to Find Target Validation Information.    
InhibitorE-64[3]
KNI-10006[5]
KNI-10033[6]
KNI-10061[6]
KNI-10062[6]
KNI-10074[7]
KNI-10079[7]
KNI-10080[7]
KNI-10081[7]
KNI-10087[7]
KNI-10088[7]
KNI-10092[7]
KNI-10093[7]
KNI-10094[7]
KNI-10095[7]
KNI-10106[7]
KNI-10113[7]
KNI-10124[7]
KNI-10125[7]
KNI-10152[7]
KNI-10155[7]
KNI-10216[7]
KNI-10217[7]
KNI-10232[6]
KNI-10255[7]
KNI-10256[7]
KNI-10260[7]
KNI-10265[7]
KNI-10266[7]
KNI-10282[7]
KNI-10283[7]
KNI-10313[6]
KNI-10314[6]
KNI-10315[6]
KNI-10316[6]
KNI-10332[6]
KNI-10341[6]
KNI-10342[6]
KNI-10368[6]
KNI-10369[7]
KNI-10372[6]
KNI-10526[7]
KNI-10527[7]
KNI-10529[7]
KNI-10538[5]
KNI-10539[7]
KNI-10541[7]
KNI-10737[5]
KNI-10740[5]
KNI-10741[5]
KNI-10742[5]
KNI-10743[5]
KNI-10758[5]
KNI-10759[5]
KNI-10760[5]
KNI-10761[5]
KNI-10762[5]
KNI-10763[5]
KNI-1293[7]
KNI-227[6]
KNI-272[6]
KNI-727[8]
KNI-764[9]
Leupeptin[10]
Leupeptin[11]
N- (R-Carboxy-Ethyl)-Alpha-[12]
PEPSTATIN A[13]
PS-154636-1,   PS-154636-2[14]
PS-222036[14]
PS-444035[14]
PS-662477[14]
PS-725074[14]
PS-777621[15]
Pepstatin[10]
Pepstatin[11]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Aspartic proteases of Plasmodium falciparum and other parasitic protozoa as drug targets. Trends Parasitol. 2001 Nov;17(11):532-7. To Reference
Ref 2Development of a plasmepsin II fluorescence polarization assay suitable for high throughput antimalarial drug discovery. J Biomol Screen. 2002 Aug;7(4):367-71. To Reference
Ref 3Antimalarial synergy of cysteine and aspartic protease inhibitors. Antimicrob Agents Chemother. 1998 Sep;42(9):2254-8. To Reference
Ref 4Inhibitors of the Plasmodium falciparum parasite aspartic protease plasmepsin II as potential antimalarial agents. Curr Med Chem. 2003 Jun;10(11):883-907. To Reference
Ref 5Bioorg Med Chem Lett. 2010 Aug 15;20(16):4836-9. Epub 2010 Jun 25.Improvement of both plasmepsin inhibitory activity and antimalarial activity by 2-aminoethylamino substitution. To Reference
Ref 6Bioorg Med Chem Lett. 2007 Jun 1;17(11):3048-52. Epub 2007 Mar 21.Additional interaction of allophenylnorstatine-containing tripeptidomimetics with malarial aspartic protease plasmepsin II. To Reference
Ref 7Bioorg Med Chem. 2008 Dec 1;16(23):10049-60. Epub 2008 Oct 10.Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin. To Reference
Ref 8Identification and characterization of allophenylnorstatine-based inhibitors of plasmepsin II, an antimalarial target. Biochemistry. 2002 Feb 19;41(7):2273-80. To Reference
Ref 9Bioorg Med Chem. 2009 Aug 15;17(16):5933-49. Epub 2009 Jul 3.alpha-Substituted norstatines as the transition-state mimic in inhibitors of multiple digestive vacuole malaria aspartic proteases. To Reference
Ref 10Novel molecular targets for antimalarial chemotherapy. Int J Antimicrob Agents. 2007 Jul;30(1):4-10. Epub 2007 Mar 6. To Reference
Ref 11Novel molecular targets for antimalarial drug development. Chem Biol Drug Des. 2008 Apr;71(4):287-97. Epub 2008 Feb 22. To Reference
Ref 12Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. To Reference
Ref 13J Med Chem. 2010 May 27;53(10):4234-47.Mechanism-based inhibitors of the aspartyl protease plasmepsin II as potential antimalarial agents. To Reference
Ref 14Bioorg Med Chem Lett. 1998 Sep 8;8(17):2315-20.Identification of potent inhibitors of Plasmodium falciparum plasmepsin II from an encoded statine combinatorial library. To Reference
Ref 15J Med Chem. 2006 Dec 14;49(25):7440-9.High antiplasmodial activity of novel plasmepsins I and II inhibitors. To Reference



 

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