James H McKerrow

Author PubWeight™ 140.13‹?›

Top papers

Rank Title Journal Year PubWeight™‹?›
1 Synthesis and evaluation of isatins and thiosemicarbazone derivatives against cruzain, falcipain-2 and rhodesain. Bioorg Med Chem Lett 2003 2.54
2 IL-13 activates a mechanism of tissue fibrosis that is completely TGF-beta independent. J Immunol 2004 2.47
3 Invasion of skin by Schistosoma cercariae. Trends Parasitol 2002 2.44
4 A high-throughput drug screen for Entamoeba histolytica identifies a new lead and target. Nat Med 2012 2.39
5 Drug discovery and development for neglected parasitic diseases. Nat Chem Biol 2006 2.31
6 Schistosomiasis mansoni: novel chemotherapy using a cysteine protease inhibitor. PLoS Med 2007 2.15
7 Tropism of dengue virus in mice and humans defined by viral nonstructural protein 3-specific immunostaining. Am J Trop Med Hyg 2009 1.87
8 A multienzyme network functions in intestinal protein digestion by a platyhelminth parasite. J Biol Chem 2006 1.82
9 Drug discovery for schistosomiasis: hit and lead compounds identified in a library of known drugs by medium-throughput phenotypic screening. PLoS Negl Trop Dis 2009 1.74
10 Synthesis and structure-activity relationship study of potent trypanocidal thio semicarbazone inhibitors of the trypanosomal cysteine protease cruzain. J Med Chem 2002 1.64
11 Discovery of trypanocidal compounds by whole cell HTS of Trypanosoma brucei. Chem Biol Drug Des 2006 1.61
12 A cathepsin B-like protease is required for host protein degradation in Trypanosoma brucei. J Biol Chem 2004 1.57
13 Complementarity between a docking and a high-throughput screen in discovering new cruzain inhibitors. J Med Chem 2010 1.54
14 Proteomic analysis of Schistosoma mansoni cercarial secretions. Mol Cell Proteomics 2005 1.54
15 A cysteine protease inhibitor cures Chagas' disease in an immunodeficient-mouse model of infection. Antimicrob Agents Chemother 2007 1.54
16 Synthesis and structure-activity relationships of parasiticidal thiosemicarbazone cysteine protease inhibitors against Plasmodium falciparum, Trypanosoma brucei, and Trypanosoma cruzi. J Med Chem 2004 1.49
17 IL-22+ CD4+ T cells are associated with therapeutic trichuris trichiura infection in an ulcerative colitis patient. Sci Transl Med 2010 1.42
18 Image-based high-throughput drug screening targeting the intracellular stage of Trypanosoma cruzi, the agent of Chagas' disease. Antimicrob Agents Chemother 2010 1.41
19 A multi-enzyme cascade of hemoglobin proteolysis in the intestine of blood-feeding hookworms. J Biol Chem 2004 1.41
20 A screen against Leishmania intracellular amastigotes: comparison to a promastigote screen and identification of a host cell-specific hit. PLoS Negl Trop Dis 2011 1.39
21 Blood 'n' guts: an update on schistosome digestive peptidases. Trends Parasitol 2004 1.35
22 RNA interference of Trypanosoma brucei cathepsin B and L affects disease progression in a mouse model. PLoS Negl Trop Dis 2008 1.35
23 Functional expression and characterization of Schistosoma mansoni cathepsin B and its trans-activation by an endogenous asparaginyl endopeptidase. Mol Biochem Parasitol 2003 1.34
24 Novel non-peptidic vinylsulfones targeting the S2 and S3 subsites of parasite cysteine proteases. Bioorg Med Chem Lett 2009 1.33
25 RNA interference in Schistosoma mansoni schistosomula: selectivity, sensitivity and operation for larger-scale screening. PLoS Negl Trop Dis 2010 1.32
26 Development of potent purine-derived nitrile inhibitors of the trypanosomal protease TbcatB. J Med Chem 2008 1.32
27 Structural characterization of CYP51 from Trypanosoma cruzi and Trypanosoma brucei bound to the antifungal drugs posaconazole and fluconazole. PLoS Negl Trop Dis 2010 1.30
28 Host pathogen protein interactions predicted by comparative modeling. Protein Sci 2007 1.29
29 Trypanosoma cruzi CYP51 inhibitor derived from a Mycobacterium tuberculosis screen hit. PLoS Negl Trop Dis 2009 1.29
30 Identification of a new class of nonpeptidic inhibitors of cruzain. J Am Chem Soc 2008 1.26
31 Differential use of protease families for invasion by schistosome cercariae. Biochimie 2007 1.24
32 Cercarial elastase is encoded by a functionally conserved gene family across multiple species of schistosomes. J Biol Chem 2002 1.22
33 A reprofiled drug, auranofin, is effective against metronidazole-resistant Giardia lamblia. Antimicrob Agents Chemother 2013 1.22
34 A nonazole CYP51 inhibitor cures Chagas' disease in a mouse model of acute infection. Antimicrob Agents Chemother 2010 1.22
35 Gene expression patterns during adaptation of a helminth parasite to different environmental niches. Genome Biol 2007 1.20
36 Structural and functional relationships in the virulence-associated cathepsin L proteases of the parasitic liver fluke, Fasciola hepatica. J Biol Chem 2007 1.19
37 Vinyl sulfones as antiparasitic agents and a structural basis for drug design. J Biol Chem 2009 1.18
38 A comparative chemogenomics strategy to predict potential drug targets in the metazoan pathogen, Schistosoma mansoni. PLoS One 2009 1.17
39 Proteomic analysis of skin invasion by blood fluke larvae. PLoS Negl Trop Dis 2008 1.16
40 Global identification of peptidase specificity by multiplex substrate profiling. Nat Methods 2012 1.14
41 The Plasmodium falciparum cysteine protease falcipain-2 captures its substrate, hemoglobin, via a unique motif. Proc Natl Acad Sci U S A 2005 1.14
42 Delineation of diverse macrophage activation programs in response to intracellular parasites and cytokines. PLoS Negl Trop Dis 2010 1.14
43 Upregulation of retinal dehydrogenase 2 in alternatively activated macrophages during retinoid-dependent type-2 immunity to helminth infection in mice. PLoS Pathog 2012 1.13
44 Diverse inhibitor chemotypes targeting Trypanosoma cruzi CYP51. PLoS Negl Trop Dis 2012 1.12
45 Discovery of potent thiosemicarbazone inhibitors of rhodesain and cruzain. Bioorg Med Chem Lett 2005 1.11
46 Cysteine proteinases from distinct cellular compartments are recruited to phagocytic vesicles by Entamoeba histolytica. Mol Biochem Parasitol 2002 1.09
47 Aziridine-2,3-dicarboxylate inhibitors targeting the major cysteine protease of Trypanosoma brucei as lead trypanocidal agents. Bioorg Med Chem Lett 2006 1.07
48 A gene family of cathepsin L-like proteases of filarial nematodes are associated with larval molting and cuticle and eggshell remodeling. Mol Biochem Parasitol 2004 1.06
49 A parasite cysteine protease is key to host protein degradation and iron acquisition. J Biol Chem 2008 1.06
50 Identification and optimization of inhibitors of Trypanosomal cysteine proteases: cruzain, rhodesain, and TbCatB. J Med Chem 2010 1.04
51 The structure of chagasin in complex with a cysteine protease clarifies the binding mode and evolution of an inhibitor family. Structure 2007 1.03
52 Structural basis for unique mechanisms of folding and hemoglobin binding by a malarial protease. Proc Natl Acad Sci U S A 2006 1.02
53 Discovery of trypanocidal thiosemicarbazone inhibitors of rhodesain and TbcatB. Bioorg Med Chem Lett 2008 1.02
54 High-throughput analysis of an RNAi library identifies novel kinase targets in Trypanosoma brucei. Chem Biol Drug Des 2011 1.01
55 IrAE: an asparaginyl endopeptidase (legumain) in the gut of the hard tick Ixodes ricinus. Int J Parasitol 2007 1.01
56 SmCB2, a novel tegumental cathepsin B from adult Schistosoma mansoni. Mol Biochem Parasitol 2002 1.00
57 Potency and selectivity of P2/P3-modified inhibitors of cysteine proteases from trypanosomes. Bioorg Med Chem Lett 2007 1.00
58 Nonpeptidic tetrafluorophenoxymethyl ketone cruzain inhibitors as promising new leads for Chagas disease chemotherapy. J Med Chem 2010 1.00
59 Aza-peptide Michael acceptors: a new class of inhibitors specific for caspases and other clan CD cysteine proteases. J Med Chem 2004 0.99
60 Metal compounds for the treatment of parasitic diseases. J Inorg Biochem 2008 0.98
61 Hypothemycin, a fungal natural product, identifies therapeutic targets in Trypanosoma brucei [corrected]. Elife 2013 0.98
62 Cruzain : the path from target validation to the clinic. Adv Exp Med Biol 2011 0.98
63 Involvement of TNF in limiting liver pathology and promoting parasite survival during schistosome infection. Int J Parasitol 2004 0.98
64 Biolistic transformation of Schistosoma mansoni with 5' flanking regions of two peptidase genes promotes tissue-specific expression. Int J Parasitol 2005 0.98
65 Natural product libraries to accelerate the high-throughput discovery of therapeutic leads. J Nat Prod 2011 0.97
66 A phagocytosis mutant of Entamoeba histolytica is less virulent due to deficient proteinase expression and release. Exp Parasitol 2006 0.97
67 The Trypanosoma cruzi protease cruzain mediates immune evasion. PLoS Pathog 2011 0.96
68 Divergent modes of enzyme inhibition in a homologous structure-activity series. J Med Chem 2009 0.96
69 The marine sponge Diacarnus bismarckensis as a source of peroxiterpene inhibitors of Trypanosoma brucei, the causative agent of sleeping sickness. J Nat Prod 2009 0.95
70 Identification of the major cysteine protease of Giardia and its role in encystation. J Biol Chem 2008 0.95
71 A contiguous compartment functions as endoplasmic reticulum and endosome/lysosome in Giardia lamblia. Eukaryot Cell 2009 0.94
72 In vitro and in vivo studies of the trypanocidal properties of WRR-483 against Trypanosoma cruzi. PLoS Negl Trop Dis 2010 0.93
73 Mining a cathepsin inhibitor library for new antiparasitic drug leads. PLoS Negl Trop Dis 2011 0.93
74 Aza-peptidyl Michael acceptors. A new class of potent and selective inhibitors of asparaginyl endopeptidases (legumains) from evolutionarily diverse pathogens. J Med Chem 2008 0.93
75 Multiple cathepsin B isoforms in schistosomula of Trichobilharzia regenti: identification, characterisation and putative role in migration and nutrition. Int J Parasitol 2005 0.93
76 Substrate specificity of schistosome versus human legumain determined by P1-P3 peptide libraries. Mol Biochem Parasitol 2002 0.92
77 Developmental plasticity in schistosomes and other helminths. Int J Parasitol 2003 0.92
78 Improved trypanocidal activities of cathepsin L inhibitors. Int J Antimicrob Agents 2003 0.92
79 Additional insights on the bastadins: isolation of analogues from the sponge Ianthella cf. reticulata and exploration of the oxime configurations. J Nat Prod 2010 0.90
80 The common gamma chain cytokines interleukin (IL)-2 and IL-7 indirectly modulate blood fluke development via effects on CD4+ T cells. J Infect Dis 2006 0.89
81 SmCL3, a gastrodermal cysteine protease of the human blood fluke Schistosoma mansoni. PLoS Negl Trop Dis 2009 0.89
82 Rational development of 4-aminopyridyl-based inhibitors targeting Trypanosoma cruzi CYP51 as anti-chagas agents. J Med Chem 2013 0.89
83 The oligopeptidase B of Leishmania regulates parasite enolase and immune evasion. J Biol Chem 2010 0.89
84 Proteomic analysis of adult S. mansoni gut contents. Mol Biochem Parasitol 2007 0.89
85 Antitrypanosomal activity of 5'-deoxy-5'-(iodomethylene)adenosine and related 6-N-cyclopropyladenosine analogues. J Med Chem 2006 0.89
86 4-Aminopyridyl-based CYP51 inhibitors as anti-Trypanosoma cruzi drug leads with improved pharmacokinetic profile and in vivo potency. J Med Chem 2014 0.88
87 In vivo imaging of tissue eosinophilia and eosinopoietic responses to schistosome worms and eggs. Int J Parasitol 2005 0.87
88 Proteases from Schistosoma mansoni cercariae cleave IgE at solvent exposed interdomain regions. Mol Immunol 2007 0.87
89 CoMFA and HQSAR of acylhydrazide cruzain inhibitors. Bioorg Med Chem Lett 2002 0.87
90 Characterization of gut-associated cathepsin D hemoglobinase from tick Ixodes ricinus (IrCD1). J Biol Chem 2012 0.86
91 Bis-acridines as lead antiparasitic agents: structure-activity analysis of a discrete compound library in vitro. Antimicrob Agents Chemother 2007 0.86
92 Aza-peptide epoxides: potent and selective inhibitors of Schistosoma mansoni and pig kidney legumains (asparaginyl endopeptidases). Biol Chem 2003 0.86
93 Synthesis of macrocyclic trypanosomal cysteine protease inhibitors. Bioorg Med Chem Lett 2008 0.85
94 Non-peptidic cruzain inhibitors with trypanocidal activity discovered by virtual screening and in vitro assay. PLoS Negl Trop Dis 2013 0.85
95 A surface amebic cysteine proteinase inactivates interleukin-18. Infect Immun 2003 0.84
96 Squamous cell carcinoma antigen 1 is an inhibitor of parasite-derived cysteine proteases. FEBS Lett 2007 0.84
97 An image-based assay for high throughput screening of Giardia lamblia. J Microbiol Methods 2011 0.84
98 Aza-peptidyl Michael acceptor and epoxide inhibitors--potent and selective inhibitors of Schistosoma mansoni and Ixodes ricinus legumains (asparaginyl endopeptidases). J Med Chem 2009 0.84
99 Investigation of the proteolytic functions of an expanded cercarial elastase gene family in Schistosoma mansoni. PLoS Negl Trop Dis 2012 0.84
100 Schistosome serine protease inhibitors: parasite defense or homeostasis? An Acad Bras Cienc 2011 0.84
101 Structure-guided development of selective TbcatB inhibitors. J Med Chem 2009 0.84
102 A cysteine protease inhibitor rescues mice from a lethal Cryptosporidium parvum infection. Antimicrob Agents Chemother 2013 0.84
103 IrCL1 - the haemoglobinolytic cathepsin L of the hard tick, Ixodes ricinus. Int J Parasitol 2011 0.84
104 Dissecting the active site of the collagenolytic cathepsin L3 protease of the invasive stage of Fasciola hepatica. PLoS Negl Trop Dis 2013 0.83
105 Biolistic transformation of Schistosoma mansoni: Studies with modified reporter-gene constructs containing regulatory regions of protease genes. Mol Biochem Parasitol 2009 0.83
106 Production and processing of a recombinant Fasciola hepatica cathepsin B-like enzyme (FhcatB1) reveals potential processing mechanisms in the parasite. Biol Chem 2006 0.83
107 Identification of genomic responses to collagen binding by trophozoites of Entamoeba histolytica. J Infect Dis 2004 0.83
108 Homology modeling and SAR analysis of Schistosoma japonicum cathepsin D (SjCD) with statin inhibitors identify a unique active site steric barrier with potential for the design of specific inhibitors. Biol Chem 2005 0.83
109 Giardia lamblia cysteine proteases. Parasitol Res 2006 0.83
110 The aignopsanes, a new class of sesquiterpenes from selected chemotypes of the sponge Cacospongia mycofijiensis. Org Lett 2009 0.82
111 Corifungin, a new drug lead against Naegleria, identified from a high-throughput screen. Antimicrob Agents Chemother 2012 0.82
112 Structural basis for inhibition of cathepsin B drug target from the human blood fluke, Schistosoma mansoni. J Biol Chem 2011 0.82
113 Current and Future Chemotherapy for Chagas Disease. Curr Med Chem 2015 0.82
114 Proteomic identification of IPSE/alpha-1 as a major hepatotoxin secreted by Schistosoma mansoni eggs. PLoS Negl Trop Dis 2011 0.81
115 Schistosoma mansoni: sex-specific modulation of parasite growth by host immune signals. Exp Parasitol 2004 0.81
116 Transcriptional and secretory responses of Entamoeba histolytica to mucins, epithelial cells and bacteria. Int J Parasitol 2007 0.81
117 Identification and characterization of a cathepsin L-like cysteine protease from Gnathostoma spinigerum. Mol Biochem Parasitol 2008 0.80
118 A blood fluke serine protease inhibitor regulates an endogenous larval elastase. J Biol Chem 2011 0.80
119 Leishmania subtilisin is a maturase for the trypanothione reductase system and contributes to disease pathology. J Biol Chem 2010 0.80
120 Dipeptidyl-alpha,beta-epoxyesters as potent irreversible inhibitors of the cysteine proteases cruzain and rhodesain. Bioorg Med Chem Lett 2007 0.78
121 Peptidyl allyl sulfones: a new class of inhibitors for clan CA cysteine proteases. Bioorg Med Chem 2004 0.78
122 Antiparasitic activities of novel, orally available fumagillin analogs. Bioorg Med Chem Lett 2009 0.78
123 Mapping inhibitor binding modes on an active cysteine protease via nuclear magnetic resonance spectroscopy. Biochemistry 2012 0.77
124 In vitro efficacy of corifungin against Acanthamoeba castellanii trophozoites and cysts. Antimicrob Agents Chemother 2013 0.77
125 Hit-to-lead development of the chamigrane endoperoxide merulin A for the treatment of African sleeping sickness. PLoS One 2012 0.77
126 Examination of the mode of action of the almiramide family of natural products against the kinetoplastid parasite Trypanosoma brucei. J Nat Prod 2013 0.76
127 Optimization of anti-Trypanosoma cruzi oxadiazoles leads to identification of compounds with efficacy in infected mice. Bioorg Med Chem 2012 0.76
128 A global comparison of the human and T. brucei degradomes gives insights about possible parasite drug targets. PLoS Negl Trop Dis 2012 0.75
129 Binding mode and potency of N-indolyloxopyridinyl-4-aminopropanyl-based inhibitors targeting Trypanosoma cruzi CYP51. J Med Chem 2014 0.75
130 Screening of acyl hydrazide proteinase inhibitors for antiparasitic activity against Trypanosoma brucei. Int J Antimicrob Agents 2002 0.75
131 Antitrypanosomal and cysteine protease inhibitory activities of alkyldiamine cryptolepine derivatives. Bioorg Med Chem Lett 2012 0.75