Drug discovery and development for neglected parasitic diseases (Q36654913)

15 August 2017

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title

Drug discovery and development for neglected parasitic diseases (English)

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15 August 2017

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1

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15 August 2017

2

James H McKerrow

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15 August 2017

language of work or name

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1 December 2006

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15 August 2017

published in

Nature Chemical Biology

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15 August 2017

volume

2

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15 August 2017

issue

12

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15 August 2017

page(s)

701-710

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Designing drugs for parasitic diseases of the developing world

15 August 2017

cites work

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Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings

21 January 2018

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

21 January 2018

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Selective targeting of lysosomal cysteine proteases with radiolabeled electrophilic substrate analogs

21 January 2018

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Features of selective kinase inhibitors

21 January 2018

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Ornithine decarboxylase as an enzyme target for therapy

21 January 2018

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Antileishmanial activities of several classes of aromatic dications

21 January 2018

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3D QSAR on a library of heterocyclic diamidine derivatives with antiparasitic activity

21 January 2018

1 reference

Parallel solution-phase synthesis of conformationally restricted congeners of pentamidine and evaluation of their antiplasmodial activities

21 January 2018

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Prodrugs for amidines: synthesis and anti-Pneumocystis carinii activity of carbamates of 2,5-bis(4-amidinophenyl)furan

21 January 2018

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Enhanced permeability of the antimicrobial agent 2,5-bis(4-amidinophenyl)furan across Caco-2 cell monolayers via its methylamidoidme prodrug

21 January 2018

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Liposomal amphotericin B: clinical experience and perspectives

21 January 2018

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Thymidylate synthase-dihydrofolate reductase in protozoa

21 January 2018

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Structure of and kinetic channelling in bifunctional dihydrofolate reductase–thymidylate synthase

21 January 2018

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The structure-based design and synthesis of selective inhibitors of Trypanosoma cruzi dihydrofolate reductase.

21 January 2018

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Novel inhibitors of Trypanosoma cruzi dihydrofolate reductase.

21 January 2018

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Novel inhibitors of Leishmanial dihydrofolate reductase.

21 January 2018

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Inhibitors of dihydrofolate reductase in Leishmania and trypanosomes

21 January 2018

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The roles of pteridine reductase 1 and dihydrofolate reductase-thymidylate synthase in pteridine metabolism in the protozoan parasite Leishmania major

21 January 2018

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Selective inhibition of Leishmania dihydrofolate reductase and Leishmania growth by 5-benzyl-2,4-diaminopyrimidines

21 January 2018

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Design, synthesis, and evaluation of inhibitors of trypanosomal and leishmanial dihydrofolate reductase

21 January 2018

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2,4-Diaminopyrimidines as inhibitors of Leishmanial and Trypanosomal dihydrofolate reductase

21 January 2018

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Trypanosomal dUTPases as potential targets for drug design.

21 January 2018

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dUTPase as a platform for antimalarial drug design: structural basis for the selectivity of a class of nucleoside inhibitors.

21 January 2018

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Trypanosoma brucei CTP synthetase: a target for the treatment of African sleeping sickness

21 January 2018

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Cysteine proteases of parasitic organisms

21 January 2018

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Biological roles of proteases in parasitic protozoa

21 January 2018

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

21 January 2018

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Cysteine protease inhibitors as chemotherapy: lessons from a parasite target

21 January 2018

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

21 January 2018

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Identification and characterization of falcilysin, a metallopeptidase involved in hemoglobin catabolism within the malaria parasite Plasmodium falciparum

21 January 2018

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Incorporation of an intramolecular hydrogen-bonding motif in the side chain of 4-aminoquinolines enhances activity against drug-resistant P. falciparum.

21 January 2018

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Structure-activity relationships for antiplasmodial activity among 7-substituted 4-aminoquinolines.

21 January 2018

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Medicines for Malaria Venture: sustaining antimalarial drug development

21 January 2018

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How might qinghaosu (artemisinin) and related compounds kill the intraerythrocytic malaria parasite? A chemist's view

21 January 2018

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Artemisinins target the SERCA of Plasmodium falciparum

21 January 2018

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Enantiomeric 1,2,4-trioxanes display equivalent in vitro antimalarial activity versus Plasmodium falciparum malaria parasites: implications for the molecular mechanism of action of the artemisinins

21 January 2018

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A medicinal chemistry perspective on artemisinin and related endoperoxides

21 January 2018

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Convenient access both to highly antimalaria-active 10-arylaminoartemisinins, and to 10-alkyl ethers including artemether, arteether, and artelinate

21 January 2018

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Orally Active, Hydrolytically Stable, Semisynthetic, Antimalarial Trioxanes in the Artemisinin Family

21 January 2018

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Novel, potent, semisynthetic antimalarial carba analogues of the first-generation 1,2,4-trioxane artemether

21 January 2018

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Mechanism-based design of parasite-targeted artemisinin derivatives: synthesis and antimalarial activity of new diamine containing analogues

21 January 2018

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Artemisone--a highly active antimalarial drug of the artemisinin class

21 January 2018

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Orally Active Antimalarial 3-Substituted Trioxanes: New Synthetic Methodology and Biological Evaluation

21 January 2018

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Orally active 1,2,4-trioxanes: synthesis and antimalarial assessment of a new series of 9-functionalized 3-(1-arylvinyl)-1,2,5-trioxaspiro[5.5]undecanes against multi-drug-resistant plasmodium yoelii nigeriensis in mice

21 January 2018

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Blood schizontocidal activity of selected 1,2,4-trioxanes (Fenozans) against the multidrug-resistant strain of Plasmodium yoelii nigeriensis (MDR) in vivo

21 January 2018

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Identification of an antimalarial synthetic trioxolane drug development candidate

21 January 2018

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Spiro and dispiro-1,2,4-trioxolanes as antimalarial peroxides: charting a workable structure-activity relationship using simple prototypes

21 January 2018

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Synthesis and antimalarial activity of sixteen dispiro-1,2,4, 5-tetraoxanes: alkyl-substituted 7,8,15,16-tetraoxadispiro[5.2.5. 2]hexadecanes

21 January 2018

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Synthesis and antimalarial activity of novel medium-sized 1,2,4,5-tetraoxacycloalkanes

21 January 2018

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A short synthesis and biological evaluation of potent and nontoxic antimalarial bridged bicyclic beta-sulfonyl-endoperoxides

21 January 2018

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Design and synthesis of endoperoxide antimalarial prodrug models.

21 January 2018

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Total syntheses of Yingzhaosu A and of its C(14)-epimer including the first evaluation of their antimalarial and cytotoxic activities

21 January 2018

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Therapeutic intervention based on protein prenylation and associated modifications

21 January 2018

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Protein prenyltransferases.

21 January 2018

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Ras Farnesyltransferase: A New Therapeutic Target

21 January 2018

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Protein farnesyl and N-myristoyl transferases: piggy-back medicinal chemistry targets for the development of antitrypanosomatid and antimalarial therapeutics.

21 January 2018

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Protein farnesyltransferase inhibitors exhibit potent antimalarial activity

21 January 2018

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Structurally simple, potent, Plasmodium selective farnesyltransferase inhibitors that arrest the growth of malaria parasites

21 January 2018

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Localization of nine glycolytic enzymes in a microbody-like organelle in Trypanosoma brucei : The glycosome

21 January 2018

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Metabolic compartmentation in African trypanosomes

21 January 2018

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History of the development of azole derivatives

21 January 2018

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Second-generation azole antifungal agents

21 January 2018

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Activity of the new triazole derivative albaconazole against Trypanosoma (Schizotrypanum) cruzi in dog hosts

21 January 2018

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Upregulation of sterol C14-demethylase expression in Trypanosoma cruzi treated with sterol biosynthesis inhibitors.

21 January 2018

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Protein kinases as drug targets in trypanosomes and Leishmania

21 January 2018

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New ways with old bones. Osteoporosis researchers look for drugs to replace hormone replacement therapy

21 January 2018

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Schistosome calcium channel beta subunits. Unusual modulatory effects and potential role in the action of the antischistosomal drug praziquantel

21 January 2018

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Cysteine protease inhibitors block schistosome hemoglobin degradation in vitro and decrease worm burden and egg production in vivo

21 January 2018

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Discovery of trypanocidal compounds by whole cell HTS of Trypanosoma brucei

21 January 2018

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Novel compounds active against Leishmania major

21 January 2018

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Searching for new antimalarial therapeutics amongst known drugs

21 January 2018

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A clinical drug library screen identifies astemizole as an antimalarial agent

21 January 2018

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DNA Binding Affinity of Bisguanidine and Bis(2-aminoimidazoline) Derivatives with in Vivo Antitrypanosomal Activity

21 January 2018

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Distribution and quantitation of the anti-trypanosomal diamidine 2,5-bis(4-amidinophenyl)furan (DB75) and its N-methoxy prodrug DB289 in murine brain tissue

21 January 2018

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7 January 2021

Dihydrofolate reductase as a therapeutic target

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7 January 2021

Induced fit, drug design, and dUTPase

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7 January 2021

Antimalarial synergy of cysteine and aspartic protease inhibitors

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7 January 2021

Schistosomiasis mansoni: novel chemotherapy using a cysteine protease inhibitor

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7 January 2021

The mechanisms of Trypanosoma cruzi invasion of mammalian cells

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7 January 2021

Pharmacokinetics of the antimalarial drug, AQ-13, in rats and cynomolgus macaques

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7 January 2021

Highly Antimalaria-Active Artemisinin Derivatives: Biological Activity Does Not Correlate with Chemical Reactivity

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7 January 2021

Antimalarial activity of artemisinin (qinghaosu) and related trioxanes: mechanism(s) of action

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7 January 2021

Artemisinins: mechanisms of action and potential for resistance

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7 January 2021

Antimalarial cyclic peroxy ketals

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7 January 2021

Thematic review series: lipid posttranslational modifications. Fighting parasitic disease by blocking protein farnesylation

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7 January 2021

Enzymes of carbohydrate metabolism as potential drug targets.

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7 January 2021

Glycolysis as a target for the design of new anti-trypanosome drugs.

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7 January 2021

Treatment of chronic Chagas' disease with itraconazole and allopurinol.

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7 January 2021

Failure of ketoconazole to cure chronic murine Chagas' disease

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7 January 2021

An experimental and clinical assay with ketoconazole in the treatment of Chagas disease

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7 January 2021

Induction of resistance to azole drugs in Trypanosoma cruzi

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7 January 2021

Antiproliferative effects and mechanism of action of SCH 56592 against Trypanosoma (Schizotrypanum) cruzi: in vitro and in vivo studies.

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7 January 2021

Activities of the triazole derivative SCH 56592 (posaconazole) against drug-resistant strains of the protozoan parasite Trypanosoma (Schizotrypanum) cruzi in immunocompetent and immunosuppressed murine hosts

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7 January 2021

Kwanzoquinones A–G and other constituents of Hemerocallis fulva ‘Kwanzo’ roots and their activity against the human pathogenic trematode Schistosoma mansoni

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7 January 2021

Identifiers

DOI

10.1038/NCHEMBIO837

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15 August 2017

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