You can find more information about cysteine proteinase falcipain 3 using the following links:

Subcellular Localization

• Picture 1
• Picture 2

PDB protein strucure

• 3BWK
• 3BPM

Affecting Drugs
Drug Name	PubMed Articles (year of publication)
(S)-N-((S,E)-6-((S)-2-((1H-indol-3-yl)methyl)-3-methoxy-5-oxo-2,5-dihydro-1H-pyrrol1-yl)-6-oxo-1-phenylhex-4-en-3-yl)-2-((S)-2-((S)-2-(dimethylamino)-3- methylbutanamido)-4-methylpentanamido)-4-methylpentanamideꞏtrifluoroacetate	Falcipain Inhibitors Based on the Natural Product Gallinamide A Are Potent in Vitro and in Vivo Antimalarials(2019)
(s)-n-[1-(cyanomethylamino)-4-methyl-1-oxopentan-2-yl] biphenyl-4-carboxamide	Substrate mapping and inhibitor profiling of falcipain-2, falcipain-3 and berghepain-2: implications for peptidase anti-malarial drug discovery(2006)
[4-[(5-cyclohexa-1,3-dien-1-yl-3-hydroxy-2-oxo-pentyl)carbamoyl]tetrahydrothiopyran-4-yl]carbamic acid	Synthesis, biological evaluation, hydration site thermodynamics, and chemical reactivity analysis of a-keto substituted peptidomimetics for the inhibition of Plasmodium falciparum(2014)
1,2,4-trioxolane	Endoperoxide carbonyl falcipain 2/3 inhibitor hybrids: toward combination chemotherapy of malaria through a single chemical entity(2010)
1-[4-chloro-2-(2-hydroxybutoxy)phenyl]butane-1,2-dione	Synthesis and evaluation of non-peptidic cysteine protease inhibitors of P. falciparum derived from etacrynic acid(2008)
10202732	Substrate mapping and inhibitor profiling of falcipain-2, falcipain-3 and berghepain-2: implications for peptidase anti-malarial drug discovery(2006)
1me3	Identification of novel malarial cysteine protease inhibitors using structure-based virtual screening of a focused cysteine protease inhibitor library(2011)
2 n-[1-(cyanomethylcarbamoyl)cyclohexyl]-4-[1-(2-methoxyethyl)piperidin-4-yl] benzamide , (s)-n-[1-(cyanomethylamino)-4-methyl- 1-oxopentan-2-yl] biphenyl-4-carboxamide, n-(s)- 4-methyl-1-oxo-1-{[r]-3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4- ylaminopentan-2-yl}benzofuran-2-carboxamide, n-(s)- 4-methyl-1-oxo-1-{[s]-3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4- ylaminopentan-2-yl}benzofuran-2-carboxamide, benzyl (2s,2 s)-1,1 -[2,2 -carbonylbis(hydrazine-2,1-diyl)]bis(4-methyl-1-oxopentane-2,1-diyl)dicarbamate, cbz-leu-nhnh-c(o)-o-bz , cbz-leu-nh-nh-c(o)-o-ph] and n-(s)-4-methyl-1-oxo-1-{[s,e]-5-phenyl-1-(phenylsulfonyl)pent-1-en-3-ylaminopentan-2-yl} morpholine-4-carboxamide	Substrate mapping and inhibitor profiling of falcipain-2, falcipain-3 and berghepain-2: implications for peptidase anti-malarial drug discovery(2006)
2-[2,3-dichloro-4-(2-oxobutanoyl)phenoxy]-N-phenacyl-acetamide	Synthesis and evaluation of non-peptidic cysteine protease inhibitors of P. falciparum derived from etacrynic acid(2008)
2oz2	Identification of novel malarial cysteine protease inhibitors using structure-based virtual screening of a focused cysteine protease inhibitor library(2011)
2-pyridone	Design and synthesis of novel 2-pyridone peptidomimetic falcipain 2/3 inhibitors(2008)
3i06	Identification of novel malarial cysteine protease inhibitors using structure-based virtual screening of a focused cysteine protease inhibitor library(2011)
4-[[5-(5-morpholinosulfonyl-2-thienyl)-2-thienyl]sulfonyl]morpholine	Identification of novel parasitic cysteine protease inhibitors by use of virtual screening. 2. The available chemical directory(2006)
5-(1,2,3,4,6,6a-hexahydrothieno[3,4-d]imidazol-3a-yl)-N-[6-[[2-[2,3-dichloro-4-(2-oxobutanoyl)phenoxy]acetyl]amino]hexyl]pentanamide	Synthesis and evaluation of non-peptidic cysteine protease inhibitors of P. falciparum derived from etacrynic acid(2008)
5-phenylthiazole	a-ketoheterocycles as inhibitors of Leishmania mexicana cysteine protease CPB(2010)
6-[1-[[2,3-dichloro-4-(2-oxobutanoyl)phenoxy]methyl]vinylamino]hexanoic acid	Synthesis and evaluation of non-peptidic cysteine protease inhibitors of P. falciparum derived from etacrynic acid(2008)
6-benzyloxy-1-(4-benzyloxyphenyl)-7-methoxy-isoquinoline	Analysis of non-peptidic compounds as potential malarial inhibitors against Plasmodial cysteine proteases via integrated virtual screening workflow(2016)
7-aminocoumarin	De novo design of 7-aminocoumarin derivatives as novel falcipain-3 inhibitors(2012)
8-azapurine	Functionalized hydroxyethylamine based peptide nanostructures as potential inhibitors of falcipain-3, an essential proteases of Plasmodium falciparum(2013)
Alln	Biosynthesis, localization, and processing of falcipain cysteine proteases of Plasmodium falciparum(2005)
Artemisinin	Haemoglobin degradation underpins the sensitivity of early ring stage Plasmodium falciparum to artemisinins(2016)
Aziridine-2,3-dicarboxylate	Synthesis and antiplasmodial activity of a cysteine protease-inhibiting biotinylated aziridine-2,3-dicarboxylate(2004)
Aziridine-2,3-dicarboxylic acid	Screening of protease inhibitors as antiplasmodial agents. Part I: Aziridines and epoxides(2007)
Aziridine-2-carboxylic acid	New cis-configured aziridine-2-carboxylates as aspartic acid protease inhibitors(2011)
Aziridine-2-carboxylic acid	Screening of protease inhibitors as antiplasmodial agents. Part I: Aziridines and epoxides(2007)
Benzothiazole	a-ketoheterocycles as inhibitors of Leishmania mexicana cysteine protease CPB(2010)
Benzoxazine	a-ketoheterocycles as inhibitors of Leishmania mexicana cysteine protease CPB(2010)
Benzyl (2s,2's)-1,1 -[2,2 -carbonylbis(hydrazine-2,1-diyl)]bis(4-methyl-1-oxopentane-2,1-diyl)dicarbamate	Substrate mapping and inhibitor profiling of falcipain-2, falcipain-3 and berghepain-2: implications for peptidase anti-malarial drug discovery(2006)
benzyl 2-[(3R)-3-(2-cyclohexa-1,3-dien-1-ylethyl)-4-oxo-5-(p-tolyl)pentanoyl]pyrrolidine-1-carboxylate;methylsulfanylethane	Synthesis, biological evaluation, hydration site thermodynamics, and chemical reactivity analysis of a-keto substituted peptidomimetics for the inhibition of Plasmodium falciparum(2014)
benzyl 2-[(3R)-3-(2-cyclohexa-1,3-dien-1-ylethyl)-5-hydroxy-4-oxo-pentanoyl]pyrrolidine-1-carboxylate	Synthesis, biological evaluation, hydration site thermodynamics, and chemical reactivity analysis of a-keto substituted peptidomimetics for the inhibition of Plasmodium falciparum(2014)
Boc-(s)-phg-(r/s)-vgln(trt)-oet	Michael acceptor based antiplasmodial and antitrypanosomal cysteine protease inhibitors with unusual amino acids(2010)
Cathepsin inhibitor library	Mining a cathepsin inhibitor library for new antiparasitic drug leads(2011)
Cbz-leu-nhnh-c(o)-o-bz	Substrate mapping and inhibitor profiling of falcipain-2, falcipain-3 and berghepain-2: implications for peptidase anti-malarial drug discovery(2006)
Cbz-leu-nh-nh-c(o)-o-ph	Substrate mapping and inhibitor profiling of falcipain-2, falcipain-3 and berghepain-2: implications for peptidase anti-malarial drug discovery(2006)
Chagasin	The structure of chagasin in complex with a cysteine protease clarifies the binding mode and evolution of an inhibitor family(2007) Study of protein complexes via homology modeling, applied to cysteine proteases and their protein inhibitors(2011)
Chembridge hydrazone and imine compounds	Identification of novel parasitic cysteine protease inhibitors using virtual screening. 1. The ChemBridge database(2004)
Crystal structure in complex with leupeptin	Structures of falcipain-2 and falcipain-3 bound to small molecule inhibitors: implications for substrate specificity(2009)
CYS-cIHL	Cyclic peptide engineered from phytocystatin inhibitory hairpin loop as an effective modulator of falcipains and potent antimalarial(2020)
Cystatin	The structure of chagasin in complex with a cysteine protease clarifies the binding mode and evolution of an inhibitor family(2007)
Cystatin a	Study of protein complexes via homology modeling, applied to cysteine proteases and their protein inhibitors(2011)
Cystatin c	Study of protein complexes via homology modeling, applied to cysteine proteases and their protein inhibitors(2011)
Cysteine protease inhibitor library	Identification of novel malarial cysteine protease inhibitors using structure-based virtual screening of a focused cysteine protease inhibitor library(2011)
Dibenzyl aziridine	Blocking effect of a biotinylated protease inhibitor on the egress of Plasmodium falciparum merozoites from infected red blood cells(2005)
Dihydroartemisinin	Haemoglobin degradation underpins the sensitivity of early ring stage Plasmodium falciparum to artemisinins(2016)
D-vlk-cmk	Substrate mapping and inhibitor profiling of falcipain-2, falcipain-3 and berghepain-2: implications for peptidase anti-malarial drug discovery(2006)
E-64	Identification of novel malarial cysteine protease inhibitors using structure-based virtual screening of a focused cysteine protease inhibitor library(2011) Substrate specificity studies of the cysteine peptidases falcipain-2 and falcipain-3 from Plasmodium falciparum and demonstration of their kininogenase activity(2013)
E64d	Haemoglobin degradation underpins the sensitivity of early ring stage Plasmodium falciparum to artemisinins(2016)
E-64d	Biosynthesis, localization, and processing of falcipain cysteine proteases of Plasmodium falciparum(2005)
Endoperoxide carbonyl falcipain 2/3 inhibitor hybrids	Endoperoxide carbonyl falcipain 2/3 inhibitor hybrids: toward combination chemotherapy of malaria through a single chemical entity(2010)
Ethacrynic acid	Synthesis and evaluation of non-peptidic cysteine protease inhibitors of P. falciparum derived from etacrynic acid(2008)
ethyl 2-[2-chloro-4-(2-oxobutanoyl)phenoxy]acetate	Synthesis and evaluation of non-peptidic cysteine protease inhibitors of P. falciparum derived from etacrynic acid(2008)
Falstatin	Falstatin, a cysteine protease inhibitor of Plasmodium falciparum, facilitates erythrocyte invasion(2006) Study of protein complexes via homology modeling, applied to cysteine proteases and their protein inhibitors(2011)
Homophenylalanylketones	Synthesis, biological evaluation, hydration site thermodynamics, and chemical reactivity analysis of a-keto substituted peptidomimetics for the inhibition of Plasmodium falciparum(2014)
Hydroxamic acid	Discovery of new potential antimalarial compounds using virtual screening of ZINC database(2015)
Isoxazoles	a-ketoheterocycles as inhibitors of Leishmania mexicana cysteine protease CPB(2010)
K11017	Vinyl sulfones as antiparasitic agents and a structural basis for drug design(2009)
Kininogen	Study of protein complexes via homology modeling, applied to cysteine proteases and their protein inhibitors(2011)
Leupeptin	The structure of chagasin in complex with a cysteine protease clarifies the binding mode and evolution of an inhibitor family(2007) Vinyl sulfones as antiparasitic agents and a structural basis for drug design(2009) Computation-based virtual screening for designing novel antimalarial drugs by targeting falcipain-III: a structure-based drug designing approach(2013)
Lhvs	Substrate mapping and inhibitor profiling of falcipain-2, falcipain-3 and berghepain-2: implications for peptidase anti-malarial drug discovery(2006)
Mg-132	Blocking Plasmodium falciparum development via dual inhibition of hemoglobin degradation and the ubiquitin proteasome system by MG132(2013)
Modeling and docking studies, suggested target	Probing the structure of falcipain-3, a cysteine protease from Plasmodium falciparum: comparative protein modeling and docking studies(2003)
Mu-leu-hph-vsph	Biosynthesis, localization, and processing of falcipain cysteine proteases of Plasmodium falciparum(2005)
N-(2H-1,3-benzodioxol-5-yl)-N'-[2-(1-methyl-1,2,3,4-tetrahydroquinolin-6-yl)ethyl]ethanediamid	Microsecond-long simulation reveals the molecular mechanism for the dual inhibition of falcipain-2 and falcipain-3 by antimalarial lead compounds(2022)
N-(3-([1,1'-biphenyl]-4-carboxamido)propyl)-1H-indole-2-carboxamide	Identification of antimalarial leads with dual falcipain-2 and falcipain-3 inhibitory activity(2020)
N'-(3-cyanophenyl)-N'-cyclohexyl-4-(4-methyl-1-piperidyl)benzohydrazide	Analysis of non-peptidic compounds as potential malarial inhibitors against Plasmodial cysteine proteases via integrated virtual screening workflow(2016)
N'-(3-cyanophenyl)-N'-cyclopentyl-3-[4-(1-piperidylmethyl)phenyl]benzohydrazide	Analysis of non-peptidic compounds as potential malarial inhibitors against Plasmodial cysteine proteases via integrated virtual screening workflow(2016)
N'-(5-bromo-2-cyano-pyrimidin-4-yl)-N'-[(2R)-2-methylcyclopentyl]-4-[(4-methylpiperazin-1-yl)methyl]benzohydrazide	Binding affinity models for Falcipain inhibition based on the Linear Interaction Energy method(2016)
N-(s)- 4-methyl-1-oxo-1-{[r]-3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4- ylaminopentan-2-yl}benzofuran-2-carboxamide	Substrate mapping and inhibitor profiling of falcipain-2, falcipain-3 and berghepain-2: implications for peptidase anti-malarial drug discovery(2006)
N-(s)-4-methyl-1-oxo-1-{[s,e]-5-phenyl-1-(phenylsulfonyl)pent-1-en-3-ylaminopentan-2-yl} morpholine-4-carboxamide	Substrate mapping and inhibitor profiling of falcipain-2, falcipain-3 and berghepain-2: implications for peptidase anti-malarial drug discovery(2006)
N-[1-(cyanomethylcarbamoyl)cyclohexyl]-4-[1-(2-methoxyethyl)piperidin-4-yl] benzamide	Substrate mapping and inhibitor profiling of falcipain-2, falcipain-3 and berghepain-2: implications for peptidase anti-malarial drug discovery(2006)
N-[2-[[3-hydroxy-1-[[7-hydroxy-2-[(Z)-prop-1-enyl]-1H-indol-4-yl]methyl]propyl]amino]-2-oxo-ethyl]naphthalene-1-carboxamide	Computation-based virtual screening for designing novel antimalarial drugs by targeting falcipain-III: a structure-based drug designing approach(2013)
N-[3-(dimethylsulfamoyl)phenyl]-5-isoxazol-3-yl-tetrahydrothiophene-2-sulfonamide	Identification of novel parasitic cysteine protease inhibitors by use of virtual screening. 2. The available chemical directory(2006)
N2,N7-bis(2-furylmethyl)-9H-fluorene-2,7-disulfonamide	Identification of novel parasitic cysteine protease inhibitors by use of virtual screening. 2. The available chemical directory(2006)
N-acetyl-Leu-Leu-norLeu	Haemoglobin degradation underpins the sensitivity of early ring stage Plasmodium falciparum to artemisinins(2016) Haemoglobin degradation underpins the sensitivity of early ring stage Plasmodium falciparum to artemisinins(2016) Haemoglobin degradation underpins the sensitivity of early ring stage Plasmodium falciparum to artemisinins(2016)
N-benzyl-N'-[(Z)-[1-[2-(3-methylanilino)-2-oxo-ethyl]-2-oxo-indolin-3-ylidene]amino]oxamide	Identification of novel parasitic cysteine protease inhibitors by use of virtual screening. 2. The available chemical directory(2006)
N-tert-butyl-2-(2-fluoro-4-(2-methylenebutanoyl)phenoxy)acetamide	Synthesis and evaluation of non-peptidic cysteine protease inhibitors of P. falciparum derived from etacrynic acid(2008)
Oxadiazole	a-ketoheterocycles as inhibitors of Leishmania mexicana cysteine protease CPB(2010)
Pepstatin	Expression and characterization of the Plasmodium falciparum haemoglobinase falcipain-3(2001)
Pmsf	Expression and characterization of the Plasmodium falciparum haemoglobinase falcipain-3(2001)
Pyrazoleamide	Synthesis of gallinamide A analogues as potent falcipain inhibitors and antimalarials(2014)
SAHA	a-ketoheterocycles as inhibitors of Leishmania mexicana cysteine protease CPB(2010) a-ketoheterocycles as inhibitors of Leishmania mexicana cysteine protease CPB(2010)
Statine	Design and synthesis of potent inhibitors of the malaria aspartyl proteases plasmepsin I and II. Use of solid-phase synthesis to explore novel statine motifs(2004)
stefin-A	Structure-Based Optimization of Protease-Inhibitor Interactions to Enhance Specificity of Human Stefin-A against Falcipain-2 from the Plasmodium falciparum 3D7 Strain(2023)
structural analysis, suggested target	Independent amino acid residues in the S2 pocket of falcipain-3 determine its specificity for P2 residues in substrates(2015)
Structure-based virtual screening suggested target	Computer-aided drug design of falcipain inhibitors: virtual screening, structure-activity relationships, hydration site thermodynamics, and reactivity analysis(2012)
Substrate specificity, suggested target	Hemoglobin cleavage site-specificity of the Plasmodium falciparum cysteine proteases falcipain-2 and falcipain-3(2009)
sugarcane cystatin	Inhibition of Plasmodium falciparum cysteine proteases by the sugarcane cystatin CaneCPI-4(2018)
Suggested target	Falcipain cysteine proteases require bipartite motifs for trafficking to the Plasmodium falciparum food vacuole(2007) Novel anti-plasmodial hits identified by virtual screening of the ZINC database(2013)
Symplostatin	The antimalarial natural product symplostatin 4 is a nanomolar inhibitor of the food vacuole falcipains(2012)
Synthetic peptidyl aldehyde and alpha-ketoamide cysteine protease inhibitors	Antimalarial activities of novel synthetic cysteine protease inhibitors(2003)
Tarocystatin	Study of protein complexes via homology modeling, applied to cysteine proteases and their protein inhibitors(2011)
Tcmdc-135965	Thousands of chemical starting points for antimalarial lead identification(2010)
tert-butyl N-[(2-cyano-5-nitro-pyrimidin-4-yl)-isobutyl-amino]carbamate	Falcipain inhibitors: optimization studies of the 2-pyrimidinecarbonitrile lead series(2010)
tert-butyl N-[(5-bromo-2-cyano-pyrimidin-4-yl)-cyclohexyl-amino]carbamate	Binding affinity models for Falcipain inhibition based on the Linear Interaction Energy method(2016)
tert-butyl N-[(5-chloro-2-cyano-pyrimidin-4-yl)-isobutyl-amino]carbamate	Falcipain inhibitors: optimization studies of the 2-pyrimidinecarbonitrile lead series(2010)
tert-butyl N-[(6-chloro-5-cyano-pyrazin-2-yl)-isobutyl-amino]carbamate	Falcipain inhibitors: optimization studies of the 2-pyrimidinecarbonitrile lead series(2010)
tert-butyl N-[(6-cyano-4-methoxy-pyrazin-2-yl)-isobutyl-amino]carbamate	Falcipain inhibitors: optimization studies of the 2-pyrimidinecarbonitrile lead series(2010)
tert-butyl N-[(6-cyanopyrazin-2-yl)-isobutyl-amino]carbamate	Falcipain inhibitors: optimization studies of the 2-pyrimidinecarbonitrile lead series(2010)
Thiophene	Mining a cathepsin inhibitor library for new antiparasitic drug leads(2011)
Triazole	a-ketoheterocycles as inhibitors of Leishmania mexicana cysteine protease CPB(2010)
Vinyl sulfone	Structure-activity relationships for inhibition of cysteine protease activity and development of Plasmodium falciparum by peptidyl vinyl sulfones(2003) Selection of cysteine protease inhibitor-resistant malaria parasites is accompanied by amplification of falcipain genes and alteration in inhibitor transport(2004) Identification of novel parasitic cysteine protease inhibitors by use of virtual screening. 2. The available chemical directory(2006) Vinyl sulfones as antiparasitic agents and a structural basis for drug design(2009) Mining a cathepsin inhibitor library for new antiparasitic drug leads(2011)
yoelipain 2	Comparing sequence and structure of falcipains and human homologs at prodomain and catalytic active site for malarial peptide based inhibitor design(2019)
ZINC69668302	Discovery of new potential antimalarial compounds using virtual screening of ZINC database(2015)
ZINC76061857	Discovery of new potential antimalarial compounds using virtual screening of ZINC database(2015)
ZINC78241300	Discovery of new potential antimalarial compounds using virtual screening of ZINC database(2015)
ZINC90631044	Discovery of new potential antimalarial compounds using virtual screening of ZINC database(2015)
ZINC97034145	Discovery of new potential antimalarial compounds using virtual screening of ZINC database(2015)
Z-lly-fmk	Substrate mapping and inhibitor profiling of falcipain-2, falcipain-3 and berghepain-2: implications for peptidase anti-malarial drug discovery(2006)
Zphe-arg-fmk	Expression and characterization of the Plasmodium falciparum haemoglobinase falcipain-3(2001)