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List of works by James H McKerrow

4-Aminopyridyl-Based CYP51 Inhibitors as Anti- Trypanosoma cruzi Drug Leads with Improved Pharmacokinetic Profile and in Vivo Potency

scientific article

A Blood Fluke Serine Protease Inhibitor Regulates an Endogenous Larval Elastase ⬇️

scientific article published on December 15, 2011

A Global Comparison of the Human and T. brucei Degradomes Gives Insights about Possible Parasite Drug Targets ⬇️

scientific article published on December 6, 2012

A High-Throughput Turbidometric Assay for Screening Inhibitors of Leishmania major Protein Disulfide Isomerase ⬇️

scientific article published on March 25, 2011

A cathepsin B-like protease is required for host protein degradation in Trypanosoma brucei

scientific article published on 23 August 2004

A comparative chemogenomics strategy to predict potential drug targets in the metazoan pathogen, Schistosoma mansoni

scientific article

A contiguous compartment functions as endoplasmic reticulum and endosome/lysosome in Giardia lamblia.

scientific article

A cysteine protease inhibitor cures Chagas' disease in an immunodeficient-mouse model of infection

scientific article

A cysteine protease inhibitor rescues mice from a lethal Cryptosporidium parvum infection

scientific article published on 23 September 2013

A gene family of cathepsin L-like proteases of filarial nematodes are associated with larval molting and cuticle and eggshell remodeling

scientific article published in August 2004

A high-throughput drug screen for Entamoeba histolytica identifies a new lead and target

scientific article

A multi-enzyme cascade of hemoglobin proteolysis in the intestine of blood-feeding hookworms

scientific article

A multienzyme network functions in intestinal protein digestion by a platyhelminth parasite

scientific article

A nonazole CYP51 inhibitor cures Chagas' disease in a mouse model of acute infection

scientific article

A novel Entamoeba histolytica cysteine proteinase, EhCP4, is key for invasive amebiasis and a therapeutic target

scientific article

A parasite cysteine protease is key to host protein degradation and iron acquisition

scientific article published on 13 August 2008

A phagocytosis mutant of Entamoeba histolytica is less virulent due to deficient proteinase expression and release

scientific article

A reprofiled drug, auranofin, is effective against metronidazole-resistant Giardia lamblia

scientific article

A screen against Leishmania intracellular amastigotes: comparison to a promastigote screen and identification of a host cell-specific hit

scientific article

A surface amebic cysteine proteinase inactivates interleukin-18.

scientific article

Activation route of the Schistosoma mansoni cathepsin B1 drug target: structural map with a glycosaminoglycan switch

scientific article

Additional insights on the bastadins: isolation of analogues from the sponge Ianthella cf. reticulata and exploration of the oxime configurations ⬇️

scientific article

An image-based assay for high throughput screening of Giardia lamblia

scientific article

Antiparasitic activities of novel, orally available fumagillin analogs

scientific article

Antitrypanosomal activity of 5'-deoxy-5'-(iodomethylene)adenosine and related 6-N-cyclopropyladenosine analogues.

scientific article published on March 2006

Antitrypanosomal and cysteine protease inhibitory activities of alkyldiamine cryptolepine derivatives

scientific article published on 15 August 2012

Ask the Experts ⬇️

scientific article published on 01 July 2012

Assessing the trypanocidal potential of natural and semi-synthetic diketopiperazines from two deep water marine-derived fungi

scientific article

Aza-peptide Michael acceptors: a new class of inhibitors specific for caspases and other clan CD cysteine proteases

scientific article published in April 2004

Aza-peptide epoxides: potent and selective inhibitors of Schistosoma mansoni and pig kidney legumains (asparaginyl endopeptidases).

scientific article

Aza-peptidyl Michael acceptor and epoxide inhibitors--potent and selective inhibitors of Schistosoma mansoni and Ixodes ricinus legumains (asparaginyl endopeptidases).

scientific article published in November 2009

Aza-peptidyl Michael acceptors. A new class of potent and selective inhibitors of asparaginyl endopeptidases (legumains) from evolutionarily diverse pathogens

scientific article published on 17 April 2008

Aziridine-2,3-dicarboxylate inhibitors targeting the major cysteine protease of Trypanosoma brucei as lead trypanocidal agents

scientific article published on 3 March 2006

Binding mode and potency of N-indolyloxopyridinyl-4-aminopropanyl-based inhibitors targeting Trypanosoma cruzi CYP51.

scientific article

Biolistic transformation of Schistosoma mansoni with 5' flanking regions of two peptidase genes promotes tissue-specific expression

scientific article

Biolistic transformation of Schistosoma mansoni: Studies with modified reporter-gene constructs containing regulatory regions of protease genes

scientific article published on 13 November 2009

Bis-acridines as lead antiparasitic agents: structure-activity analysis of a discrete compound library in vitro

scientific article

Blood 'n' guts: an update on schistosome digestive peptidases

scientific article published on May 2004

Cercarial elastase is encoded by a functionally conserved gene family across multiple species of schistosomes.

scientific article

Characterization of gut-associated cathepsin D hemoglobinase from tick Ixodes ricinus (IrCD1).

scientific article

CoMFA and HQSAR of acylhydrazide cruzain inhibitors

scientific article published in June 2002

Complementarity Between a Docking and a High-Throughput Screen in Discovering New Cruzain Inhibitors

scientific article

Corifungin, a new drug lead against Naegleria, identified from a high-throughput screen.

scientific article

Cruzain : the path from target validation to the clinic

scientific article published on January 2011

Current and Future Chemotherapy for Chagas Disease

scientific article published on 19 October 2015

Cysteine and Aspartyl Proteases Contribute to Protein Digestion in the Gut of Freshwater Planaria

scientific article (publication date: August 2016)

Cysteine proteinases from distinct cellular compartments are recruited to phagocytic vesicles by Entamoeba histolytica ⬇️

scientific article published on January 1, 2002

Delineation of diverse macrophage activation programs in response to intracellular parasites and cytokines

scientific article

Designing drugs for parasitic diseases of the developing world

scientific article

Detection of HIV-1 in Entamoeba histolytica without evidence of transmission to human cells

scientific article

Determinants of disease phenotype in trypanosomatid parasites

scientific article

Development of potent purine-derived nitrile inhibitors of the trypanosomal protease TbcatB.

scientific article published on 4 January 2008

Development of protease inhibitors for protozoan infections

scientific article published on December 2008

Developmental plasticity in schistosomes and other helminths

scientific article

Differential use of protease families for invasion by schistosome cercariae

scientific article

Dipeptidyl-alpha,beta-epoxyesters as potent irreversible inhibitors of the cysteine proteases cruzain and rhodesain

scientific article published on 22 October 2007

Discovery of novel benzoxaborole-based potent antitrypanosomal agents

scientific article

Discovery of potent thiosemicarbazone inhibitors of rhodesain and cruzain

scientific article published in January 2005

Discovery of trypanocidal compounds by whole cell HTS of Trypanosoma brucei

scientific article published in May 2006

Discovery of trypanocidal thiosemicarbazone inhibitors of rhodesain and TbcatB

scientific article published on 8 April 2008

Divergent modes of enzyme inhibition in a homologous structure-activity series

scientific article published on August 2009

Diverse Inhibitor Chemotypes Targeting Trypanosoma cruzi CYP51 ⬇️

scientific article published on July 31, 2012

Diversity-oriented synthesis yields a new drug lead for treatment of chagas disease

scientific article

Drug Susceptibility of Genetically Engineered Trypanosoma cruzi Strains and Sterile Cure in Animal Models as a Criterion for Potential Clinical Efficacy of Anti-T. cruzi Drugs

scientific article published on December 2015

Drug discovery and development for neglected parasitic diseases

scientific article published on December 2006

Drug discovery for schistosomiasis: hit and lead compounds identified in a library of known drugs by medium-throughput phenotypic screening

scientific article

Early invasion of brain parenchyma by African trypanosomes ⬇️

scientific article published in 2012

Editorial: Drug Development for Parasite-Induced Diarrheal Diseases

scientific article published on 4 April 2017

Evaluation of Antigens for Development of a Serological Test for Human African Trypanosomiasis

scientific article

Examination of the mode of action of the almiramide family of natural products against the kinetoplastid parasite Trypanosoma brucei

scientific article

Functional expression and characterization of Schistosoma mansoni cathepsin B and its trans-activation by an endogenous asparaginyl endopeptidase

scientific article

Gene expression patterns during adaptation of a helminth parasite to different environmental niches.

scientific article published in January 2007

Genome-Directed Lead Discovery: Biosynthesis, Structure Elucidation, and Biological Evaluation of Two Families of Polyene Macrolactams against Trypanosoma brucei

scientific article published on 13 August 2015

Giardia lamblia cysteine proteases

scientific article

Global identification of peptidase specificity by multiplex substrate profiling

scientific article

Heat shock protein 90 inhibitors repurposed against Entamoeba histolytica

scientific article published on 28 April 2015

Helminth Cysteine Proteases

High-throughput analysis of an RNAi library identifies novel kinase targets in Trypanosoma brucei

scientific article

Hit-to-lead development of the chamigrane endoperoxide merulin A for the treatment of African sleeping sickness

scientific article

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.

scientific article published in April 2005

Host pathogen protein interactions predicted by comparative modeling

scientific article

Hsp90 inhibitors as new leads to target parasitic diarrheal diseases

scientific article

Hypothemycin, a fungal natural product, identifies therapeutic targets in Trypanosoma brucei [corrected].

scientific article published on 09 July 2013

IL-13 activates a mechanism of tissue fibrosis that is completely TGF-beta independent

scientific article published in September 2004

IL-22+ CD4+ T cells are associated with therapeutic trichuris trichiura infection in an ulcerative colitis patient.

scientific article

Identification and Optimization of Inhibitors of Trypanosomal Cysteine Proteases: Cruzain, Rhodesain, and TbCatB

scientific article

Identification and characterization of a cathepsin L-like cysteine protease from Gnathostoma spinigerum

scientific article

Identification of a new class of nonpeptidic inhibitors of cruzain

scientific article

Identification of cysteine protease inhibitors as new drug leads against Naegleria fowleri

scientific article published on 15 March 2018

Identification of genomic responses to collagen binding by trophozoites of Entamoeba histolytica

scientific article published on 2 July 2004

Identification of the major cysteine protease of Giardia and its role in encystation

scientific article published on 29 April 2008

Image-based high-throughput drug screening targeting the intracellular stage of Trypanosoma cruzi, the agent of Chagas' disease

scientific article

Improved trypanocidal activities of cathepsin L inhibitors

scientific article published in August 2003

In Vitro Efficacy of Ebselen and BAY 11-7082 Against Naegleria fowleri

scientific article published on 6 March 2018

In Vitro and In Vivo Studies of the Trypanocidal Properties of WRR-483 against Trypanosoma cruzi ⬇️

scientific article published on September 14, 2010

In vitro efficacy of corifungin against Acanthamoeba castellanii trophozoites and cysts

scientific article

In vivo imaging of tissue eosinophilia and eosinopoietic responses to schistosome worms and eggs

scientific article

Inhibición de la Cruzaína: estrategia molecular en la búsqueda de nuevos fármacos para el Mal de Chagas

Inhibitors of SARS-CoV entry--identification using an internally-controlled dual envelope pseudovirion assay

scientific article

Introduction: drug discovery and development for neglected diseases

scientific article published on November 2014

Invasion of skin by Schistosoma cercariae

scientific article published in May 2002

Investigation of the proteolytic functions of an expanded cercarial elastase gene family in Schistosoma mansoni

scientific article

Involvement of TNF in limiting liver pathology and promoting parasite survival during schistosome infection

scientific article

IrAE – An asparaginyl endopeptidase (legumain) in the gut of the hard tick Ixodes ricinus

scientific article (publication date: June 2007)

IrCL1 - the haemoglobinolytic cathepsin L of the hard tick, Ixodes ricinus.

scientific article

Lead identification to clinical candidate selection: drugs for Chagas disease

scientific article

Leishmania Subtilisin Is a Maturase for the Trypanothione Reductase System and Contributes to Disease Pathology ⬇️

scientific article published on July 30, 2010

Leishmania major protein disulfide isomerase as a drug target: enzymatic and functional characterization

scientific article

Location, Location, Location: Five Facts about Tissue Tropism and Pathogenesis

scientific article

Machine Learning Models and Pathway Genome Data Base for Trypanosoma cruzi Drug Discovery

scientific article

Mapping Inhibitor Binding Modes on an Active Cysteine Protease via Nuclear Magnetic Resonance Spectroscopy ⬇️

scientific article published on December 10, 2012

Metal compounds for the treatment of parasitic diseases

scientific article published on 4 June 2008

Mining a cathepsin inhibitor library for new antiparasitic drug leads

scientific article

Multiple cathepsin B isoforms in schistosomula of Trichobilharzia regenti: identification, characterisation and putative role in migration and nutrition.

scientific article

Naloxonazine, an Amastigote-Specific Compound, Affects Leishmania Parasites through Modulation of Host-Encoded Functions

scientific article

Natural Product Libraries to Accelerate the High-Throughput Discovery of Therapeutic Leads ⬇️

scientific article published on November 30, 2011

Nonpeptidic Tetrafluorophenoxymethyl Ketone Cruzain Inhibitors as Promising New Leads for Chagas Disease Chemotherapy

scientific article

Novel non-peptidic vinylsulfones targeting the S2 and S3 subsites of parasite cysteine proteases

scientific article

Optimization of anti-Trypanosoma cruzi oxadiazoles leads to identification of compounds with efficacy in infected mice

scientific article published on 31 August 2012

Peptidyl allyl sulfones: a new class of inhibitors for clan CA cysteine proteases

scientific article published in October 2004

Phase I Clinical Trial Results of Auranofin, a Novel Antiparasitic Agent

scientific article

Phenotypic, chemical and functional characterization of cyclic nucleotide phosphodiesterase 4 (PDE4) as a potential anthelmintic drug target

scientific article published on 13 July 2017

Potency and selectivity of P2/P3-modified inhibitors of cysteine proteases from trypanosomes

scientific article published on 22 November 2007

Predictions of novel Schistosoma mansoni - human protein interactions consistent with experimental data

scientific article published in Scientific Reports

Production and processing of a recombinant Fasciola hepatica cathepsin B-like enzyme (FhcatB1) reveals potential processing mechanisms in the parasite.

scientific article

Protease inhibitors targeting coronavirus and filovirus entry

scientific article

Proteases from Schistosoma mansoni cercariae cleave IgE at solvent exposed interdomain regions

scientific article

Proteases in parasitic diseases

scientific article published on January 2006

Proteomic Analysis of Human Skin Treated with Larval Schistosome Peptidases Reveals Distinct Invasion Strategies among Species of Blood Flukes ⬇️

scientific article published on September 27, 2011

Proteomic Identification of IPSE/alpha-1 as a Major Hepatotoxin Secreted by Schistosoma mansoni Eggs ⬇️

scientific article published on October 25, 2011

Proteomic analysis of Schistosoma mansoni cercarial secretions

scientific article published on 18 August 2005

Proteomic analysis of adult S. mansoni gut contents

scientific article published on 20 March 2007

Proteomic analysis of skin invasion by blood fluke larvae ⬇️

scientific article

R -Configuration of 4-Aminopyridyl-Based Inhibitors of CYP51 Confers Superior Efficacy Against Trypanosoma cruzi

scientific article

RNA interference in Schistosoma mansoni schistosomula: selectivity, sensitivity and operation for larger-scale screening

scientific article

RNA interference of Trypanosoma brucei cathepsin B and L affects disease progression in a mouse model

scientific article

Rapid Chagas Disease Drug Target Discovery Using Directed Evolution in Drug-Sensitive Yeast

scientific article published on 15 December 2016

Rational Development of 4-Aminopyridyl-Based Inhibitors Targeting Trypanosoma cruzi CYP51 as Anti-Chagas Agents

scientific article

Recognition of the role of Natural Products as drugs to treat neglected tropical diseases by the 2015 Nobel prize in physiology or medicine

scientific article

Repurposing auranofin as a lead candidate for treatment of lymphatic filariasis and onchocerciasis

scientific article

Schistosoma mansoni: sex-specific modulation of parasite growth by host immune signals

scientific article

Schistosome serine protease inhibitors: parasite defense or homeostasis? ⬇️

scientific article published on June 1, 2011

Schistosomiasis mansoni: novel chemotherapy using a cysteine protease inhibitor

scientific article

Screening of acyl hydrazide proteinase inhibitors for antiparasitic activity against Trypanosoma brucei

scientific article

SmCB2, a novel tegumental cathepsin B from adult Schistosoma mansoni

scientific article published on April 2002

SmCL3, a gastrodermal cysteine protease of the human blood fluke Schistosoma mansoni

scientific article

Squamous cell carcinoma antigen 1 is an inhibitor of parasite-derived cysteine proteases

scientific article published on 9 August 2007

Structural Basis for Inhibition of Cathepsin B Drug Target from the Human Blood Fluke, Schistosoma mansoni

scientific article

Structural Characterization of CYP51 from Trypanosoma cruzi and Trypanosoma brucei Bound to the Antifungal Drugs Posaconazole and Fluconazole

scientific article

Structural and Functional Relationships in the Virulence-associated Cathepsin L Proteases of the Parasitic Liver Fluke, Fasciola hepatica

scientific article

Structural basis for unique mechanisms of folding and hemoglobin binding by a malarial protease

scientific article (publication date: August 2006)

Structure-Bioactivity Relationship for Benzimidazole Thiophene Inhibitors of Polo-Like Kinase 1 (PLK1), a Potential Drug Target in Schistosoma mansoni

scientific article

Structure-guided development of selective TbcatB inhibitors

scientific article published on October 2009

Substrate specificity of schistosome versus human legumain determined by P1-P3 peptide libraries

scientific article

Synthesis and Evaluation of Oxyguanidine Analogues of the Cysteine Protease Inhibitor WRR-483 against Cruzain

scientific article

Synthesis and evaluation of isatins and thiosemicarbazone derivatives against cruzain, falcipain-2 and rhodesain

scientific article published in October 2003

Synthesis and structure-activity relationship study of potent trypanocidal thio semicarbazone inhibitors of the trypanosomal cysteine protease cruzain

scientific article

Synthesis and structure-activity relationships of parasiticidal thiosemicarbazone cysteine protease inhibitors against Plasmodium falciparum, Trypanosoma brucei, and Trypanosoma cruzi

scientific article published in June 2004

Synthesis of a sugar-based thiosemicarbazone series and structure-activity relationship versus the parasite cysteine proteases rhodesain, cruzain, and Schistosoma mansoni cathepsin B1.

scientific article

Synthesis of macrocyclic trypanosomal cysteine protease inhibitors

scientific article published on 10 June 2008

TLTF in cerebrospinal fluid for detection and staging of T. b. gambiense infection

scientific article

Targeting Ergosterol biosynthesis in Leishmania donovani: essentiality of sterol 14 alpha-demethylase

scientific article

The Plasmodium falciparum cysteine protease falcipain-2 captures its substrate, hemoglobin, via a unique motif

scientific article

The Trypanosoma cruzi protease cruzain mediates immune evasion

scientific article

The aignopsanes, a new class of sesquiterpenes from selected chemotypes of the sponge Cacospongia mycofijiensis ⬇️

scientific article published on May 2009

The common gamma chain cytokines interleukin (IL)-2 and IL-7 indirectly modulate blood fluke development via effects on CD4+ T cells

scientific article

The diverse roles of cysteine proteases in parasites and their suitability as drug targets

scholarly article by James H McKerrow published August 2018 in PLoS Neglected Tropical Diseases

The marine sponge Diacarnus bismarckensis as a source of peroxiterpene inhibitors of Trypanosoma brucei, the causative agent of sleeping sickness ⬇️

scientific article

The oligopeptidase B of Leishmania regulates parasite enolase and immune evasion

scientific article

The rule of five should not impede anti-parasitic drug development

scientific article

The structure of chagasin in complex with a cysteine protease clarifies the binding mode and evolution of an inhibitor family

scientific article

Transcriptional and secretory responses of Entamoeba histolytica to mucins, epithelial cells and bacteria

scientific article published on 12 February 2007

Tropism of dengue virus in mice and humans defined by viral nonstructural protein 3-specific immunostaining.

scientific article published on March 2009

Trypanosoma cruzi CYP51 Inhibitor Derived from a Mycobacterium tuberculosis Screen Hit

scientific article

Trypsin- and Chymotrypsin-like serine proteases in schistosoma mansoni-- 'the undiscovered country'.

scientific article

Two key cathepsins, TgCPB and TgCPL, are targeted by the vinyl sulfone inhibitor K11777 in in vitro and in vivo models of toxoplasmosis

scientific article published on 22 March 2018

Update on drug development targeting parasite cysteine proteases

article

Upregulation of retinal dehydrogenase 2 in alternatively activated macrophages during retinoid-dependent type-2 immunity to helminth infection in mice

scientific article

Use of recombinant Entamoeba histolytica cysteine proteinase 1 to identify a potent inhibitor of amebic invasion in a human colonic model ⬇️

scientific article

Utilizing Chemical Genomics to Identify Cytochrome b as a Novel Drug Target for Chagas Disease

scientific article (publication date: July 2015)

Vinyl Sulfones as Antiparasitic Agents and a Structural Basis for Drug Design

scientific article

WormAssay: A Novel Computer Application for Whole-Plate Motion-based Screening of Macroscopic Parasites ⬇️

scientific article published on January 31, 2012

X-ray structures of thioredoxin and thioredoxin reductase from Entamoeba histolytica and prevailing hypothesis of the mechanism of Auranofin action

scientific article published on 11 February 2016

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