You can find more information about plasmepsin IV using the following links:

Subcellular Localization

• Picture 1
• Picture 2

PDB protein strucure

• 1LS5
• 5I70
• 5JOD
• 2ANL
• 1ME6

Affecting Drugs
Drug Name	PubMed Articles (year of publication)
(2R,3R,4R)-2-Benzyloxy-3,4-dihydroxy-N-[(1S,2R)- 2-hydroxyindan-1-yl]-4-[(2R)-3-oxo-1-oxa-4-aza-cyclotridec-2-yl]-butyramide	Macrocyclic inhibitors of the malarial aspartic proteases plasmepsin I, II, and IV(2006)
(3R,4R)-3-benzyl-4-hydroxy-7-(3-methoxyphenyl)-7-methyl-1-(3-(2-propylpentanoyl)phenyl)octan-1-one	Computational insights for predicting the binding and selectivity of peptidomimetic plasmepsin IV inhibitors against cathepsin D(2022)
(4R)-3-[(2S,3S)-3-[[(2R)-2-[[2-(4-aminophenyl)acetyl]amino]-3-methylsulfanylpropanoyl]amino]-2-hydroxy-4-phenylbutanoyl]-N-[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]-5,5-dimethyl-1,3-thiazolidine-4-carboxamide	Deciphering the mechanism of potent peptidomimetic inhibitors targeting plasmepsins - biochemical and structural insights(2018)
(4R)-N-tert-Butyl-3-[(2S,3S)-2-hydroxy-3-({N-[(isoquinolin-5-yloxy)acetyl]-S-methyl-L-cysteinyl}amino)-4-phenylbutanoyl]-1,3-thiazolidine-4-carboxamide	High-affinity inhibition of a family of Plasmodium falciparum proteases by a designed adaptive inhibitor(2003)
(S)-N-((2R,3S)-4-(4-(4-Bromobenzyl)piperazin-1-yl)-3-hydroxy-1-phenylbutan-2-yl)-2-(1,3-dioxoisoindolin-2-yl)-3-methylbutanamide.	Hydroxyethylamine Based Phthalimides as New Class of Plasmepsin Hits: Design, Synthesis and Antimalarial Evaluation(2015)
(S)-N-((2R,3S)-4-(4-(4-Fluorobenzyl)piperazin-1-yl)-3-hydroxy-1-phenylbutan-2-yl)-2-(1,3-dioxoisoindolin-2-yl)-3-phenylpropanamide.	Hydroxyethylamine Based Phthalimides as New Class of Plasmepsin Hits: Design, Synthesis and Antimalarial Evaluation(2015)
[amino({5-phenyl-3-[(E)-2-phenylethenyl]- 4,5-dihydro-1H-pyrazol-1-yl})methylidene]azanium	Successful application of virtual screening and molecular dynamics simulations against antimalarial molecular targets(2016)
1-[2-methoxy-5-[(1E)-3-phenylbuta-1,3-dienyl]phenyl]sulfonylpyridine	Antimalarial activity of 4-metoxychalcones: docking studies as falcipain/plasmepsin inhibitors, ADMET and lipophilic efficiency analysis to identify a putative oral lead candidate(2013)
1-[2-methoxy-5-[(1E)-3-phenylbuta-1,3-dienyl]phenyl]sulfonylpyrrolidine	Antimalarial activity of 4-metoxychalcones: docking studies as falcipain/plasmepsin inhibitors, ADMET and lipophilic efficiency analysis to identify a putative oral lead candidate(2013)
11-azatricyclo[6.2.1.02,7]undeca-2(7),3,5-triene tricycle	De Novo design, synthesis, and in vitro evaluation of a new class of nonpeptidic inhibitors of the malarial enzyme plasmepsin II(2002)
13- and 16-membred macrocycles	Macrocyclic inhibitors of the malarial aspartic proteases plasmepsin I, II, and IV(2006)
2,3,4,7-tetrahydro-1h-azepine	Computer-aided design and synthesis of nonpeptidic plasmepsin II and IV inhibitors(2008)
2-Amino-3-(((2S*,5R*)-5-isopropyltetrahydrofuran-2-yl)methyl)-7- phenylquinazolin-4(3H)-one	Fragment-Based Discovery of 2-Aminoquinazolin-4(3H)-ones As Novel Class Nonpeptidomimetic Inhibitors of the Plasmepsins I, II, and IV(2016)
2-Amino-7-phenyl-3-(((2R,5S)-5-phenyltetrahydrofuran-2-yl)methyl)quinazolin- 4(3H)-one	Fragment-Based Discovery of 2-Aminoquinazolin-4(3H)-ones As Novel Class Nonpeptidomimetic Inhibitors of the Plasmepsins I, II, and IV(2016)
2-Amino-7-phenyl-3-(((2S*,5R*)-5-phenyltetrahydrofuran-2- yl)methyl)quinazolin-4(3H)-one	Fragment-Based Discovery of 2-Aminoquinazolin-4(3H)-ones As Novel Class Nonpeptidomimetic Inhibitors of the Plasmepsins I, II, and IV(2016)
3-(7-(4-(4l3-butyl)phenyl)-2-amino-4-oxo-3-((tetrahydrofuran-2-yl)methyl)-3,4-dihydroquinazolin-5-yl)propanoic acid	2-Aminoquinazolin-4(3H)-one based plasmepsin inhibitors with improved hydrophilicity and selectivity(2018)
4-[2-methoxy-5-[(1E)-3-phenylbuta-1,3-dienyl]phenyl]sulfonylmorpholine	Antimalarial activity of 4-metoxychalcones: docking studies as falcipain/plasmepsin inhibitors, ADMET and lipophilic efficiency analysis to identify a putative oral lead candidate(2013)
4-aminopiperidine	Achiral, cheap, and potent inhibitors of Plasmepsins I, II, and IV(2006)
4-aminoquinoline	Antiplasmodial activities of 4-aminoquinoline-statine compounds(2012)
7-azabicyclo[2.2.1]heptane	Potent inhibitors of malarial aspartic proteases, the plasmepsins, by hydroformylation of substituted 7-azanorbornenes(2013)
Alln	Role of Plasmodium falciparum digestive vacuole plasmepsins in the specificity and antimalarial mode of action of cysteine and aspartic protease inhibitors(2009)
Allophenylnorstatine	Computational analysis of plasmepsin IV bound to an allophenylnorstatine inhibitor(2006)
Aminohydantoin	Evaluation of aminohydantoins as a novel class of antimalarial agents(2013)
Atazanavir	Critical roles for the digestive vacuole plasmepsins of Plasmodium falciparum in vacuolar function(2007)
Atovaquone	Telithromycin and quinupristin-dalfopristin induce delayed death in Plasmodium falciparum(2008)
Benzophenone	Prodomain processing of recombinant plasmepsin II and IV, the aspartic proteases of Plasmodium falciparum, is auto- and trans-catalytic(2006)
Catestatin	Catestatin, an endogenous chromogranin A-derived peptide, inhibits in vitro growth of Plasmodium falciparum(2010)
Diphenylurea	Design of new plasmepsin inhibitors: a virtual high throughput screening approach on the EGEE grid(2007) Role of Plasmodium falciparum digestive vacuole plasmepsins in the specificity and antimalarial mode of action of cysteine and aspartic protease inhibitors(2009)
E-64	Critical roles for the digestive vacuole plasmepsins of Plasmodium falciparum in vacuolar function(2007) Role of Plasmodium falciparum digestive vacuole plasmepsins in the specificity and antimalarial mode of action of cysteine and aspartic protease inhibitors(2009)
G16	Functional profiling, identification, and inhibition of plasmepsins in intraerythrocytic malaria parasites(2009)
Guanidino	Design of new plasmepsin inhibitors: a virtual high throughput screening approach on the EGEE grid(2007)
Indinavir	Critical roles for the digestive vacuole plasmepsins of Plasmodium falciparum in vacuolar function(2007)
Kni-10740	Optimization of plasmepsin inhibitor by focusing on similar structural feature with chloroquine to avoid drug-resistant mechanism of Plasmodium falciparum(2014)
Kni-10823	Optimization of plasmepsin inhibitor by focusing on similar structural feature with chloroquine to avoid drug-resistant mechanism of Plasmodium falciparum(2014)
Kni-764	Structure of the aspartic protease plasmepsin 4 from the malarial parasite Plasmodium malariae bound to an allophenylnorstatine-based inhibitor(2006)
Leupeptin	Critical roles for the digestive vacuole plasmepsins of Plasmodium falciparum in vacuolar function(2007) Role of Plasmodium falciparum digestive vacuole plasmepsins in the specificity and antimalarial mode of action of cysteine and aspartic protease inhibitors(2009)
Ligand based virtual screening, mdg419, mdg421, mdg422, mdg425, mdg426, mdg427, mdg430, mdg432	Identification of plasmepsin inhibitors as selective anti-malarial agents using ligand based drug design(2011)
Lopinavir	Potencies of human immunodeficiency virus protease inhibitors in vitro against Plasmodium falciparum and in vivo against murine malaria(2006) Critical roles for the digestive vacuole plasmepsins of Plasmodium falciparum in vacuolar function(2007)
N,N'-((2R,2'R,3S,3'S)-piperazine-1,4-diylbis(3-hydroxy-1-phenylbutane-4,2-diyl))bis(2-(1,3-dioxoisoindolin-2-yl)-3 phenylpropanamide)	Hydroxyethylamine Based Phthalimides as New Class of Plasmepsin Hits: Design, Synthesis and Antimalarial Evaluation(2015)
N1-((2S,3R)-1-cyclohexyl-3-hydroxy-4-((2-(3-methoxyphenyl)propan-2-yl)amino)butan-2-yl)-5-(piperidin-1-yl)-N3-(3,3,3-trifluoropropyl)isophthalamide	Peptidomimetic plasmepsin inhibitors with potent anti-malarial activity and selectivity against cathepsin D(2019)
N-acetyl-l-leucyl-l-leucyl-norleucinal	Prodomain processing of recombinant plasmepsin II and IV, the aspartic proteases of Plasmodium falciparum, is auto- and trans-catalytic(2006)
N-alkyl chains	Exploring the flap pocket of the antimalarial target plasmepsin II: the "55 % rule" applied to enzymes(2008)
N-benzyl-2-methoxy-5-[(1E)-3-phenylbuta-1,3-dienyl]benzenesulfonamide	Antimalarial activity of 4-metoxychalcones: docking studies as falcipain/plasmepsin inhibitors, ADMET and lipophilic efficiency analysis to identify a putative oral lead candidate(2013)
Nelfinavir	Critical roles for the digestive vacuole plasmepsins of Plasmodium falciparum in vacuolar function(2007)
Norstatines	alpha-Substituted norstatines as the transition-state mimic in inhibitors of multiple digestive vacuole malaria aspartic proteases(2009)
Pepstatin a	Prodomain processing of recombinant plasmepsin II and IV, the aspartic proteases of Plasmodium falciparum, is auto- and trans-catalytic(2006) Antimalarial activity of thiosemicarbazones and purine derived nitriles(2009) Role of Plasmodium falciparum digestive vacuole plasmepsins in the specificity and antimalarial mode of action of cysteine and aspartic protease inhibitors(2009)
Plm iv selective symmetrical nonpeptidic inhibitor 18	Synthesis of malarial plasmepsin inhibitors and prediction of binding modes by molecular dynamics simulations(2005)
Purine	Antimalarial activity of thiosemicarbazones and purine derived nitriles(2009)
Ritonavir	Potencies of human immunodeficiency virus protease inhibitors in vitro against Plasmodium falciparum and in vivo against murine malaria(2006) Critical roles for the digestive vacuole plasmepsins of Plasmodium falciparum in vacuolar function(2007)
Ro 40-4388	Role of Plasmodium falciparum digestive vacuole plasmepsins in the specificity and antimalarial mode of action of cysteine and aspartic protease inhibitors(2009)
Saquinavir	Potencies of human immunodeficiency virus protease inhibitors in vitro against Plasmodium falciparum and in vivo against murine malaria(2006) Critical roles for the digestive vacuole plasmepsins of Plasmodium falciparum in vacuolar function(2007)
Statine	Targeting the plasmepsin 4 orthologs of Plasmodium sp. with "double drug" inhibitors(2008)
Suggested target	Plasmepsin 4, the food vacuole aspartic proteinase found in all Plasmodium spp. infecting man(2003) Genetic disruption of the Plasmodium falciparum digestive vacuole plasmepsins demonstrates their functional redundancy(2004) Structural and active site analysis of plasmepsins of Plasmodium falciparum: potential anti-malarial targets(2005)
Sulfonamide 4-metychalcone	Antimalarial activity of 4-metoxychalcones: docking studies as falcipain/plasmepsin inhibitors, ADMET and lipophilic efficiency analysis to identify a putative oral lead candidate(2013)
Tcmdc-134527	Thousands of chemical starting points for antimalarial lead identification(2010)
Tcmdc-134674	Plasmepsin inhibitory activity and structure-guided optimization of a potent hydroxyethylamine-based antimalarial hit(2014)
tert-butyl ((S)-1-(((2S,3S)-4-(4-((2S,3R)-3-((S)-2-((tert-butoxycarbonyl)amino)-4-methylpentanamido)-2-hydroxy-4-phenylbutyl)piperazin-1-yl)-3-hydroxy-1-phenylbutan-2-yl)amino)-4-methyl-1-oxopentan-2-yl)carbamate	Fast-Acting Small Molecules Targeting Malarial Aspartyl Proteases, Plasmepsins, Inhibit Malaria Infection at Multiple Life Stages(2019)
tert-Butyl((2R,3S)-4-([1,4'-bipiperidin]-1'-yl)-3-hydroxy-1-phenylbutan-2-yl)carbamate	Hydroxyethylamine Based Phthalimides as New Class of Plasmepsin Hits: Design, Synthesis and Antimalarial Evaluation(2015)
Thiourea	Design of new plasmepsin inhibitors: a virtual high throughput screening approach on the EGEE grid(2007)
X-ray structures and 3d models , suggested target	Predicting functional residues in Plasmodium falciparum plasmepsins by combining sequence and structural analysis with molecular dynamics simulations(2008)
ZINC03351002	Unveiling a New Era in Malaria Therapeutics: A Tailored Molecular Approach Towards the Design of Plasmepsin IX Inhibitors(2019)