Target Information

Target General Infomation
Target ID
T50547
Former ID
TTDR00107
Target Name
Plasmepsin 1
Synonyms
Aspartic hemoglobinase I; PFAPG; Plasmepsin I
Target Type
Discontinued
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.
BioChemical Class
Peptidase
Target Validation
T50547
UniProt ID
P39898
EC Number
EC 3.4.23.38
Sequence
MALSIKEDFSSAFAKNESAVNSSTFNNNMKTWKIQKRFQILYVFFFLLITGALFYYLIDN
VLFPKNKKINEIMNTSKHVIIGFSIENSHDRIMKTVKQHRLKNYIKESLKFFKTGLTQKP
HLGNAGDSVTLNDVANVMYYGEAQIGDNKQKFAFIFDTGSANLWVPSAQCNTIGCKTKNL
YDSNKSKTYEKDGTKVEMNYVSGTVSGFFSKDIVTIANLSFPYKFIEVTDTNGFEPAYTL
GQFDGIVGLGWKDLSIGSVDPVVVELKNQNKIEQAVFTFYLPFDDKHKGYLTIGGIEDRF
YEGQLTYEKLNHDLYWQVDLDLHFGNLTVEKATAIVDSGTSSITAPTEFLNKFFEGLDVV
KIPFLPLYITTCNNPKLPTLEFRSATNVYTLEPEYYLQQIFDFGISLCMVSIIPVDLNKN
TFILGDPFMRKYFTVFDYDNHTVGFALAKKKL
Drugs and Mode of Action
Drug(s) Pepstatin Drug Info Terminated Malaria [545704]
Inhibitor E-64 Drug Info [538124]
KNI-10006 Drug Info [530280]
L-mannitol derivative Drug Info [527739]
Leupeptin Drug Info [536365]
Pepstatin Drug Info [536365]
PS-777621 Drug Info [528560]
SC-5003 Drug Info [525693]
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 525693J Med Chem. 2000 Feb 10;43(3):305-41.Protease inhibitors: current status and future prospects.
Ref 527739J Med Chem. 2005 Sep 22;48(19):6090-106.Synthesis of malarial plasmepsin inhibitors and prediction of binding modes by molecular dynamics simulations.
Ref 528560J Med Chem. 2006 Dec 14;49(25):7440-9.High antiplasmodial activity of novel plasmepsins I and II inhibitors.
Ref 530280Bioorg 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.
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.

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