Target Information
Target General Infomation | |||||
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Target ID |
T50547
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Former ID |
TTDR00107
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Target Name |
Plasmepsin 1
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Synonyms |
Aspartic hemoglobinase I; PFAPG; Plasmepsin I
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Target Type |
Discontinued
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Disease | Malaria [ICD10: B54] | ||||
Function |
Participates in the digestion of the host hemoglobin. Initial cleavage at the hinge region of hemoglobin, than cleaves at other sites, leading to denaturation of the molecule and to further degradation.
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BioChemical Class |
Peptidase
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Target Validation |
T50547
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UniProt ID | |||||
EC Number |
EC 3.4.23.38
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Sequence |
MALSIKEDFSSAFAKNESAVNSSTFNNNMKTWKIQKRFQILYVFFFLLITGALFYYLIDN
VLFPKNKKINEIMNTSKHVIIGFSIENSHDRIMKTVKQHRLKNYIKESLKFFKTGLTQKP HLGNAGDSVTLNDVANVMYYGEAQIGDNKQKFAFIFDTGSANLWVPSAQCNTIGCKTKNL YDSNKSKTYEKDGTKVEMNYVSGTVSGFFSKDIVTIANLSFPYKFIEVTDTNGFEPAYTL GQFDGIVGLGWKDLSIGSVDPVVVELKNQNKIEQAVFTFYLPFDDKHKGYLTIGGIEDRF YEGQLTYEKLNHDLYWQVDLDLHFGNLTVEKATAIVDSGTSSITAPTEFLNKFFEGLDVV KIPFLPLYITTCNNPKLPTLEFRSATNVYTLEPEYYLQQIFDFGISLCMVSIIPVDLNKN TFILGDPFMRKYFTVFDYDNHTVGFALAKKKL |
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Drugs and Mode of Action | |||||
References | |||||
Ref 525693 | J Med Chem. 2000 Feb 10;43(3):305-41.Protease inhibitors: current status and future prospects. | ||||
Ref 527739 | J Med Chem. 2005 Sep 22;48(19):6090-106.Synthesis of malarial plasmepsin inhibitors and prediction of binding modes by molecular dynamics simulations. | ||||
Ref 528560 | J Med Chem. 2006 Dec 14;49(25):7440-9.High antiplasmodial activity of novel plasmepsins I and II inhibitors. | ||||
Ref 530280 | Bioorg 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. |
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