Target Information

Target General Infomation
Target ID
T46465
Former ID
TTDR00106
Target Name
Plasmepsin 2
Synonyms
Aspartic hemoglobinase II; PFAPD; Plasmepsin II
Target Type
Discontinued
Disease Malaria [ICD10: B54]
BioChemical Class
Peptidase
Target Validation
T46465
UniProt ID
P46925
EC Number
EC 3.4.23.39
Sequence
MDITVREHDFKHGFIKSNSTFDGLNIDNSKNKKKIQKGFQILYVLLFCSVMCGLFYYVYE
NVWLQRDNEMNEILKNSEHLTIGFKVENAHDRILKTIKTHKLKNYIKESVNFLNSGLTKT
NYLGSSNDNIELVDFQNIMFYGDAEVGDNQQPFTFILDTGSANLWVPSVKCTTAGCLTKH
LYDSSKSRTYEKDGTKVEMNYVSGTVSGFFSKDLVTVGNLSLPYKFIEVIDTNGFEPTYT
ASTFDGILGLGWKDLSIGSVDPIVVELKNQNKIENALFTFYLPVHDKHTGFLTIGGIEER
FYEGPLTYEKLNHDLYWQITLDAHVGNIMLEKANCIVDSGTSAITVPTDFLNKMLQNLDV
IKVPFLPFYVTLCNNSKLPTFEFTSENGKYTLEPEYYLQHIEDVGPGLCMLNIIGLDFPV
PTFILGDPFMRKYFTVFDYDNHSVGIALAKKNL
Drugs and Mode of Action
Drug(s) Pepstatin Drug Info Terminated Malaria [545704]
Inhibitor E-64 Drug Info [538124]
KNI-10006 Drug Info [531036]
KNI-10033 Drug Info [528767]
KNI-10061 Drug Info [528767]
KNI-10062 Drug Info [528767]
KNI-10074 Drug Info [529771]
KNI-10079 Drug Info [529771]
KNI-10080 Drug Info [529771]
KNI-10081 Drug Info [529771]
KNI-10087 Drug Info [529771]
KNI-10088 Drug Info [529771]
KNI-10092 Drug Info [529771]
KNI-10093 Drug Info [529771]
KNI-10094 Drug Info [529771]
KNI-10095 Drug Info [529771]
KNI-10106 Drug Info [529771]
KNI-10113 Drug Info [529771]
KNI-10124 Drug Info [529771]
KNI-10125 Drug Info [529771]
KNI-10152 Drug Info [529771]
KNI-10155 Drug Info [529771]
KNI-10216 Drug Info [529771]
KNI-10217 Drug Info [529771]
KNI-10232 Drug Info [528767]
KNI-10255 Drug Info [529771]
KNI-10256 Drug Info [529771]
KNI-10260 Drug Info [529771]
KNI-10265 Drug Info [529771]
KNI-10266 Drug Info [529771]
KNI-10282 Drug Info [529771]
KNI-10283 Drug Info [529771]
KNI-10313 Drug Info [528767]
KNI-10314 Drug Info [528767]
KNI-10315 Drug Info [528767]
KNI-10316 Drug Info [528767]
KNI-10332 Drug Info [528767]
KNI-10341 Drug Info [528767]
KNI-10342 Drug Info [528767]
KNI-10368 Drug Info [528767]
KNI-10369 Drug Info [529771]
KNI-10372 Drug Info [528767]
KNI-10526 Drug Info [529771]
KNI-10527 Drug Info [529771]
KNI-10529 Drug Info [529771]
KNI-10538 Drug Info [531036]
KNI-10539 Drug Info [529771]
KNI-10541 Drug Info [529771]
KNI-10737 Drug Info [531036]
KNI-10740 Drug Info [531036]
KNI-10741 Drug Info [531036]
KNI-10742 Drug Info [531036]
KNI-10743 Drug Info [531036]
KNI-10758 Drug Info [531036]
KNI-10759 Drug Info [531036]
KNI-10760 Drug Info [531036]
KNI-10761 Drug Info [531036]
KNI-10762 Drug Info [531036]
KNI-10763 Drug Info [531036]
KNI-1293 Drug Info [529771]
KNI-227 Drug Info [528767]
KNI-727 Drug Info [535366]
Leupeptin Drug Info [536365]
N-(R-Carboxy-Ethyl)-Alpha-(S)-(2-Phenylethyl) Drug Info [551393]
Pepstatin Drug Info [536365]
PS-154636-1 Drug Info [534798]
PS-222036 Drug Info [534798]
PS-444035 Drug Info [534798]
PS-662477 Drug Info [534798]
PS-725074 Drug Info [534798]
PS-777621 Drug Info [528560]
References
Ref 545704Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004280)
Ref 528560J Med Chem. 2006 Dec 14;49(25):7440-9.High antiplasmodial activity of novel plasmepsins I and II inhibitors.
Ref 528767Bioorg 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.
Ref 529771Bioorg 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.
Ref 531036Bioorg 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.
Ref 534798Bioorg 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.
Ref 535366Identification and characterization of allophenylnorstatine-based inhibitors of plasmepsin II, an antimalarial target. Biochemistry. 2002 Feb 19;41(7):2273-80.
Ref 536365Novel molecular targets for antimalarial chemotherapy. Int J Antimicrob Agents. 2007 Jul;30(1):4-10. Epub 2007 Mar 6.
Ref 538124Antimalarial synergy of cysteine and aspartic protease inhibitors. Antimicrob Agents Chemother. 1998 Sep;42(9):2254-8.
Ref 551393How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.

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