Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTXMNHO)

DTT Name Plasmodium Plasmepsin 2 (Malaria PLA2)
Synonyms Plasmepsin-2; PFAPD; Aspartic hemoglobinase II
Gene Name Malaria PLA2
DTT Type
Patented-recorded target
 [1]
BioChemical Class
Peptidase
UniProt ID
PLM2_PLAFA
TTD ID
T46465
EC Number
EC 3.4.23.39
Sequence
MDITVREHDFKHGFIKSNSTFDGLNIDNSKNKKKIQKGFQILYVLLFCSVMCGLFYYVYE
NVWLQRDNEMNEILKNSEHLTIGFKVENAHDRILKTIKTHKLKNYIKESVNFLNSGLTKT
NYLGSSNDNIELVDFQNIMFYGDAEVGDNQQPFTFILDTGSANLWVPSVKCTTAGCLTKH
LYDSSKSRTYEKDGTKVEMNYVSGTVSGFFSKDLVTVGNLSLPYKFIEVIDTNGFEPTYT
ASTFDGILGLGWKDLSIGSVDPIVVELKNQNKIENALFTFYLPVHDKHTGFLTIGGIEER
FYEGPLTYEKLNHDLYWQITLDAHVGNIMLEKANCIVDSGTSAITVPTDFLNKMLQNLDV
IKVPFLPFYVTLCNNSKLPTFEFTSENGKYTLEPEYYLQHIEDVGPGLCMLNIIGLDFPV
PTFILGDPFMRKYFTVFDYDNHSVGIALAKKNL
Function Hydrolysis of the bonds linking certain hydrophobic residues in hemoglobin or globin. Also cleaves small molecules substrates such as Ala-Leu-Glu-Arg-Thr-Phe-|-Phe(NO(2))-Ser-Phe-Pro-Thr.
BioCyc Pathway
MetaCyc:MON-15374

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
3 Patented Agent(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
US9353089, 135 DMWG98Z N. A. N. A. Patented [2]
US9353089, 327 DMB4MJ0 N. A. N. A. Patented [2]
US9353089, 330 DMK02LS N. A. N. A. Patented [2]
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1 Discontinued Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Pepstatin DM9S1EA Malaria 1F40-1F45 Terminated [1]
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69 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
E-64 DMMOPAK Discovery agent N.A. Investigative [3]
KNI-10006 DMMISH6 Discovery agent N.A. Investigative [4]
KNI-10033 DMLOXMQ Discovery agent N.A. Investigative [5]
KNI-10061 DMMZ6AO Discovery agent N.A. Investigative [5]
KNI-10062 DMYSDN4 Discovery agent N.A. Investigative [5]
KNI-10074 DMM5SDT Discovery agent N.A. Investigative [6]
KNI-10079 DMCZOX9 Discovery agent N.A. Investigative [6]
KNI-10080 DMEN4DZ Discovery agent N.A. Investigative [6]
KNI-10081 DM1Z7QK Discovery agent N.A. Investigative [6]
KNI-10087 DMYN2U4 Discovery agent N.A. Investigative [6]
KNI-10088 DM4GASE Discovery agent N.A. Investigative [6]
KNI-10092 DMV1KI2 Discovery agent N.A. Investigative [6]
KNI-10093 DMGY5Z0 Discovery agent N.A. Investigative [6]
KNI-10094 DMJIQG2 Discovery agent N.A. Investigative [6]
KNI-10095 DMEHPVF Discovery agent N.A. Investigative [6]
KNI-10106 DMBTRHG Discovery agent N.A. Investigative [6]
KNI-10113 DM78A6F Discovery agent N.A. Investigative [6]
KNI-10124 DMA9104 Discovery agent N.A. Investigative [6]
KNI-10125 DMDBERC Discovery agent N.A. Investigative [6]
KNI-10152 DMNBUS4 Discovery agent N.A. Investigative [6]
KNI-10155 DM1PKWA Discovery agent N.A. Investigative [6]
KNI-10216 DM64NBG Discovery agent N.A. Investigative [6]
KNI-10217 DMHLFAE Discovery agent N.A. Investigative [6]
KNI-10232 DMQY1ST Discovery agent N.A. Investigative [5]
KNI-10255 DMV3U9Z Discovery agent N.A. Investigative [6]
KNI-10256 DMZFVHT Discovery agent N.A. Investigative [6]
KNI-10260 DMZXI6U Discovery agent N.A. Investigative [6]
KNI-10265 DMQLB3T Discovery agent N.A. Investigative [6]
KNI-10266 DMP2E3I Discovery agent N.A. Investigative [6]
KNI-10282 DMAR35H Discovery agent N.A. Investigative [6]
KNI-10283 DMGVBIT Discovery agent N.A. Investigative [6]
KNI-10313 DMP7M8O Discovery agent N.A. Investigative [5]
KNI-10314 DMYGNZA Discovery agent N.A. Investigative [5]
KNI-10315 DM1OPYT Discovery agent N.A. Investigative [5]
KNI-10316 DMMIDCG Discovery agent N.A. Investigative [5]
KNI-10332 DMKVPMS Discovery agent N.A. Investigative [5]
KNI-10341 DMF9P25 Discovery agent N.A. Investigative [5]
KNI-10342 DMDM5BL Discovery agent N.A. Investigative [5]
KNI-10368 DM8SIRL Discovery agent N.A. Investigative [5]
KNI-10369 DM97STY Discovery agent N.A. Investigative [6]
KNI-10372 DM4AUCE Discovery agent N.A. Investigative [5]
KNI-10526 DMEN2L3 Discovery agent N.A. Investigative [6]
KNI-10527 DMU4K7O Discovery agent N.A. Investigative [6]
KNI-10529 DMDRWYG Discovery agent N.A. Investigative [6]
KNI-10538 DM7XEIY Discovery agent N.A. Investigative [4]
KNI-10539 DMLWOFY Discovery agent N.A. Investigative [6]
KNI-10541 DMP87U4 Discovery agent N.A. Investigative [6]
KNI-10737 DMGUABP Discovery agent N.A. Investigative [4]
KNI-10740 DMPWY6H Discovery agent N.A. Investigative [4]
KNI-10741 DM7TW4C Discovery agent N.A. Investigative [4]
KNI-10742 DM4D9T3 Discovery agent N.A. Investigative [4]
KNI-10743 DM0VSPE Discovery agent N.A. Investigative [4]
KNI-10758 DMM2A5Q Discovery agent N.A. Investigative [4]
KNI-10759 DMAF1W3 Discovery agent N.A. Investigative [4]
KNI-10760 DMT5FIP Discovery agent N.A. Investigative [4]
KNI-10761 DMXUTWZ Discovery agent N.A. Investigative [4]
KNI-10762 DM73WB2 Discovery agent N.A. Investigative [4]
KNI-10763 DMKAY5G Discovery agent N.A. Investigative [4]
KNI-1293 DMZX430 Discovery agent N.A. Investigative [6]
KNI-227 DMS61DB Discovery agent N.A. Investigative [5]
KNI-727 DM105NU Discovery agent N.A. Investigative [7]
Leupeptin DMU075F Malaria 1F40-1F45 Investigative [1]
N-(R-Carboxy-Ethyl)-Alpha-(S)-(2-Phenylethyl) DM2SNXB Discovery agent N.A. Investigative [8]
PS-154636-1 DMQUG0K Discovery agent N.A. Investigative [9]
PS-222036 DMQVI5U Discovery agent N.A. Investigative [9]
PS-444035 DMH8YMP Discovery agent N.A. Investigative [9]
PS-662477 DMT4YFR Discovery agent N.A. Investigative [9]
PS-725074 DM05DOF Discovery agent N.A. Investigative [9]
PS-777621 DM3F7SD Discovery agent N.A. Investigative [10]
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⏷ Show the Full List of 69 Investigative Drug(s)

References

1 Novel molecular targets for antimalarial chemotherapy. Int J Antimicrob Agents. 2007 Jul;30(1):4-10.
2 Compositions and methods for the treatment of malaria. US9353089.
3 Antimalarial synergy of cysteine and aspartic protease inhibitors. Antimicrob Agents Chemother. 1998 Sep;42(9):2254-8.
4 Improvement of both plasmepsin inhibitory activity and antimalarial activity by 2-aminoethylamino substitution. Bioorg Med Chem Lett. 2010 Aug 15;20(16):4836-9.
5 Additional interaction of allophenylnorstatine-containing tripeptidomimetics with malarial aspartic protease plasmepsin II. Bioorg Med Chem Lett. 2007 Jun 1;17(11):3048-52.
6 Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin. Bioorg Med Chem. 2008 Dec 1;16(23):10049-60.
7 Identification and characterization of allophenylnorstatine-based inhibitors of plasmepsin II, an antimalarial target. Biochemistry. 2002 Feb 19;41(7):2273-80.
8 How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
9 Identification of potent inhibitors of Plasmodium falciparum plasmepsin II from an encoded statine combinatorial library. Bioorg Med Chem Lett. 1998 Sep 8;8(17):2315-20.
10 High antiplasmodial activity of novel plasmepsins I and II inhibitors. J Med Chem. 2006 Dec 14;49(25):7440-9.