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List of works by Harry P de Koning

2,N6-disubstituted adenosine analogs with antitrypanosomal and antimalarial activities

scientific article

A Leishmania major nucleobase transporter responsible for allopurinol uptake is a functional homolog of the Trypanosoma brucei H2 transporter

scientific article published in April 2003

A comprehensive model of purine uptake by the malaria parasite Plasmodium falciparum: identification of four purine transport activities in intraerythrocytic parasites

scientific article published in April 2008

A diminazene-resistant strain of Trypanosoma brucei brucei isolated from a dog is cross-resistant to pentamidine in experimentally infected albino rats

scientific article published in January 2006

A drug resistance determinant in Trypanosoma brucei.

scientific article

A fluorescence-based assay for the uptake of CPD0801 (DB829) by African trypanosomes

scientific article published on 15 July 2010

A highly selective, high-affinity transporter for uracil in Trypanosoma brucei brucei: evidence for proton-dependent transport

scientific article

A new nonpolar N-hydroxy imidazoline lead compound with improved activity in a murine model of late-stage Trypanosoma brucei brucei infection is not cross-resistant with diamidines

scientific article

Alternative oxidase inhibitors: Mitochondrion-targeting as a strategy for new drugs against pathogenic parasites and fungi

scientific article published on 29 January 2019

An improved and highly sensitive microfluorimetric method for assessing susceptibility of Plasmodium falciparum to antimalarial drugs in vitro

scientific article

Analysis of autofeedback mechanisms in the secretion of pro-opiomelanocortin-derived peptides by melanotrope cells of Xenopus laevis

scientific article published in September 1992

Analysis of inositol phosphate metabolism in melanotrope cells of Xenopus laevis in relation to background adaptation

scientific article published in May 1993

Antileishmanial and antitrypanosomal activity of symmetrical dibenzyl-substituted α,β-unsaturated carbonyl-based compounds

scientific article published on 24 April 2019

Antitrypanosomal Activity of a Novel Taccalonolide from the Tubers of Tacca leontopetaloides

scientific article published in May 2016

Aquaglyceroporin 2 controls susceptibility to melarsoprol and pentamidine in African trypanosomes

scientific article

Aquaporin 2 mutations in Trypanosoma brucei gambiense field isolates correlate with decreased susceptibility to pentamidine and melarsoprol

scientific article (publication date: 2013)

Biosynthesis and uptake of thiamine (vitamin B1) in bloodstream form Trypanosoma brucei brucei and interference of the vitamin with melarsen oxide activity

scientific article published on 21 November 2005

C6-O-alkylated 7-deazainosine nucleoside analogues: Discovery of potent and selective anti-sleeping sickness agents

scientific article published on 03 January 2020

Characterisation of the plasma membrane subproteome of bloodstream form Trypanosoma brucei.

scientific article

Characterization of a Nucleoside/Proton Symporter in Procyclic Trypanosoma brucei brucei

scientific article published in Journal of Biological Chemistry

Characterization of the choline carrier of Plasmodium falciparum: a route for the selective delivery of novel antimalarial drugs.

scientific article

Chemical and Antimicrobial Profiling of Propolis from Different Regions within Libya

scientific article

Chemical characterisation of Nigerian red propolis and its biological activity against Trypanosoma Brucei

scientific article published on 11 December 2015

Chemotherapeutic strategies against Trypanosoma brucei: drug targets vs. drug targeting.

scientific article published on January 2007

Chimerization at the AQP2-AQP3 locus is the genetic basis of melarsoprol-pentamidine cross-resistance in clinical Trypanosoma brucei gambiense isolates

scientific article published on 7 May 2015

Cloning and functional complementation of ten Schistosoma mansoni phosphodiesterases expressed in the mammalian host stages

scientific article published on 30 July 2020

Cloning, heterologous expression, and in situ characterization of the first high affinity nucleobase transporter from a protozoan

scientific article published on 21 April 2003

Combining tubercidin and cordycepin scaffolds results in highly active candidates to treat late-stage sleeping sickness

scientific article published on 05 December 2019

Comparative genomics of drug resistance in Trypanosoma brucei rhodesiense

scientific article published on 14 March 2016

Curcuminoid analogs with potent activity against Trypanosoma and Leishmania species

scientific article

Cyclic AMP effectors in African trypanosomes revealed by genome-scale RNA interference library screening for resistance to the phosphodiesterase inhibitor CpdA

scientific article

Cyclic-nucleotide signalling in protozoa

scientific article published on 26 January 2011

Design and synthesis of a series of truncated neplanocin fleximers

scientific article published on 16 December 2014

Detection of arsenical drug resistance in Trypanosoma brucei with a simple fluorescence test

scientific article

Different substrate recognition motifs of human and trypanosome nucleobase transporters. Selective uptake of purine antimetabolites

scientific article

Differential effects of coexisting dopamine, GABA and NPY on alpha-MSH secretion from melanotrope cells of Xenopus laevis

scientific article published in January 1993

Differential regulation of nucleoside and nucleobase transporters in Crithidia fasciculata and Trypanosoma brucei brucei

scientific article published on 01 February 2000

Divergent metabolism between Trypanosoma congolense and Trypanosoma brucei results in differential sensitivity to metabolic inhibition

scientific article published on 26 July 2021

Drug resistance in African trypanosomiasis: the melarsoprol and pentamidine story ⬇️

scientific article published on January 30, 2013

Drugs and drug resistance in African trypanosomiasis

scientific article published on February 2007

Dual Action of GABA A Receptors on the Secretory Process of Melanotrophs of Xenopus laevis

scientific article published on 01 July 1993

Dynamics of cyclic-AMP efflux in relation to alpha-MSH secretion from melanotrope cells of Xenopus laevis

scientific article published in January 1992

Epidemiology of visceral leishmaniasis in Georgia

scientific article

European propolis is highly active against trypanosomatids including Crithidia fasciculata

scientific article published on 06 August 2019

Evaluation of nucleoside hydrolase inhibitors for treatment of African trypanosomiasis

scientific article

Ever-increasing complexities of diamidine and arsenical crossresistance in African trypanosomes

article

Evolutionary genomics of epidemic visceral leishmaniasis in the Indian subcontinent

scientific article

Exploiting the Achilles' heel of membrane trafficking in trypanosomes

scientific article

Functional analysis of drug resistance-associated mutations in the Trypanosoma brucei adenosine transporter 1 (TbAT1) and the proposal of a structural model for the protein

scientific article published on 21 March 2015

Functional and genetic evidence that nucleoside transport is highly conserved in Leishmania species: Implications for pyrimidine-based chemotherapy

scientific article

Functional expression of TcoAT1 reveals it to be a P1-type nucleoside transporter with no capacity for diminazene uptake

scientific article published on 10 February 2013

Further evidence for a link between melarsoprol resistance and P2 transporter function in African trypanosomes.

scientific article

Genotypic status of the TbAT1/P2 adenosine transporter of Trypanosoma brucei gambiense isolates from Northwestern Uganda following melarsoprol withdrawal

scientific article

Identification and characterisation of high affinity nucleoside and nucleobase transporters in Toxoplasma gondii

scientific article

Identification of the first pyrimidine nucleobase transporter in Leishmania: similarities with the Trypanosoma brucei U1 transporter and antileishmanial activity of uracil analogues.

scientific article published in March 2005

In and out of the minor groove: interaction of an AT-rich DNA with the drug CD27

scientific article

Investigation of 5'-Norcarbocyclic Nucleoside Analogues as Antiprotozoal and Antibacterial Agents

scientific article published on 21 September 2019

Kinetic and mutational analysis of the Trypanosoma brucei NBT1 nucleobase transporter expressed in Saccharomyces cerevisiae reveals structural similarities between ENT and MFS transporters

scientific article published on 22 October 2007

Loss of the high-affinity pentamidine transporter is responsible for high levels of cross-resistance between arsenical and diamidine drugs in African trypanosomes

scientific article published on 18 January 2007

Lowering the pKa of a bisimidazoline lead with halogen atoms results in improved activity and selectivity against Trypanosoma brucei in vitro

scientific article

Mechanisms of arsenical and diamidine uptake and resistance in Trypanosoma brucei

scientific article

Molecular pharmacology of adenosine transport in Trypanosoma brucei: P1/P2 revisited

scientific article published on 2 June 2005

Multi-target mode of action of a Clerodane-type diterpenoid from Polyalthia longifolia targeting African trypanosomes

scientific article published on 15 March 2018

Multiple genetic mechanisms lead to loss of functional TbAT1 expression in drug-resistant trypanosomes

scientific article

Pentamidine movement across the murine blood-brain and blood-cerebrospinal fluid barriers: effect of trypanosome infection, combination therapy, P-glycoprotein, and multidrug resistance-associated protein

scientific article published on 4 March 2009

Pentamidine uptake and resistance in pathogenic protozoa: past, present and future

scientific article

Pharmacological validation of Trypanosoma brucei phosphodiesterases as novel drug targets

scientific article

Positively selected modifications in the pore of TbAQP2 allow pentamidine to enter Trypanosoma brucei

scientific article published on 07 August 2020

Potent Antitrypanosomal Activities of 3-Aminosteroids against African Trypanosomes: Investigation of Cellular Effects and of Cross-Resistance with Existing Drugs

scientific article published on 12 January 2019

Potent trypanocidal curcumin analogs bearing a monoenone linker motif act on Trypanosoma brucei by forming an adduct with trypanothione

scientific article published on 19 December 2014

Predictive computational models of substrate binding by a nucleoside transporter

scientific article

Progress Towards New Treatments for Human African Trypanosomiasis

Propidium iodide-based methods for monitoring drug action in the kinetoplastidae: comparison with the Alamar Blue assay

scientific article published on 3 August 2008

Protocols for the routine screening of drug sensitivity in the human parasite Trichomonas vaginalis

scientific article published on January 2015

Purine and pyrimidine transport in pathogenic protozoa: from biology to therapy

scientific article

Purine and pyrimidine transporters of pathogenic protozoa - conduits for therapeutic agents

scientific article published on 07 March 2020

Purine nucleobase transport in amastigotes of Leishmania mexicana: involvement in allopurinol uptake

scientific article published on September 2005

Purine nucleobase transport in bloodstream forms of Trypanosoma brucei brucei is mediated by two novel transporters

scientific article published on 01 November 1997

Pyrimidine biosynthesis is not an essential function for Trypanosoma brucei bloodstream forms

scientific article

Pyrimidine salvage in Trypanosoma brucei bloodstream forms and the trypanocidal action of halogenated pyrimidines

scientific article published on 27 November 2012

Pyrimidine transporters of trypanosomes – a class apart?

Rational Selection of Anti-Microbial Drug Targets: Unique or Conserved?

Reduced Mitochondrial Membrane Potential Is a Late Adaptation of Trypanosoma brucei brucei to Isometamidium Preceded by Mutations in the γ Subunit of the F1Fo-ATPase

scientific article

Revisiting tubercidin against kinetoplastid parasites: Aromatic substitutions at position 7 improve activity and reduce toxicity

article published in 2019

SAR Studies of Diphenyl Cationic Trypanocides: Superior Activity of Phosphonium over Ammonium Salts

scientific article published on 10 December 2014

Selective transport of a new class of purine antimetabolites by the protozoan parasite Trypanosoma brucei

scientific article published in October 2004

Seroepidemiology and molecular diversity of Leishmania donovani complex in Georgia

scientific article published on 13 May 2016

Specific Cell Targeting Therapy Bypasses Drug Resistance Mechanisms in African Trypanosomiasis

scientific article (publication date: June 2015)

Structure-activity relationships of synthetic cordycepin analogues as experimental therapeutics for African trypanosomiasis

scientific article published on 10 December 2013

Suramin exposure alters cellular metabolism and mitochondrial energy production in African trypanosomes

scientific article published on 30 April 2020

Symmetrical choline-derived dications display strong anti-kinetoplastid activity

scientific article

Synthesis and structure-activity analysis of new phosphonium salts with potent activity against African trypanosomes.

scientific article

Synthesis of marine-derived 3-alkylpyridinium alkaloids with potent antiprotozoal activity

scientific article published on 5 October 2011

Targeting the parasite's DNA with methyltriazenyl purine analogs is a safe, selective, and efficacious antitrypanosomal strategy

scientific article

The CRF-related peptide sauvagine stimulates and the GABAB receptor agonist baclofen inhibits cyclic-AMP production in melanotrope cells of Xenopus laevis

article

The Chemical Characterization of Nigerian Propolis samples and Their Activity Against Trypanosoma brucei.

scientific article published on 19 April 2017

The Drugs of Sleeping Sickness: Their Mechanisms of Action and Resistance, and a Brief History

scientific article published on 19 January 2020

The Secretion of ?40-MSH from Xenopus Melanotropes Involves Calcium Influx through ?-Conotoxin-Sensitive Voltage-Operated Calcium Channels

scientific article published on 01 August 1994

The Strong Anti-Kinetoplastid Properties of Bee Propolis: Composition and Identification of the Active Agents and Their Biochemical Targets

scientific article published on 05 November 2020

The animal trypanosomiases and their chemotherapy: a review

scientific article

The diamidine diminazene aceturate is a substrate for the high-affinity pentamidine transporter: implications for the development of high resistance levels in trypanosomes

scientific article

The ever unfolding story of cAMP signaling in trypanosomatids: vive la difference!

scientific article

The individual components of commercial isometamidium do not possess stronger trypanocidal activity than the mixture, nor bypass isometamidium resistance

scientific article published on 21 January 2019

The significance of multiple inhibitory mechanisms converging on the melanotrope cell of Xenopus laevis

scientific article published in May 1998

The trypanocide diminazene aceturate is accumulated predominantly through the TbAT1 purine transporter: additional insights on diamidine resistance in african trypanosomes.

scientific article published on May 2004

Therapeutic potential of phosphodiesterase inhibitors in parasitic diseases

scientific article published on January 2011

Transport proteins determine drug sensitivity and resistance in a protozoan parasite, Trypanosoma brucei

scientific article

Transporters in Anti-Parasitic Drug Development and Resistance

article

TrypanoCyc: a community-led biochemical pathways database for Trypanosoma brucei

scientific article

Trypanocidal action of bisphosphonium salts through a mitochondrial target in bloodstream form Trypanosoma brucei

scientific article published on 11 December 2015

Trypanocidal furamidine analogues: influence of pyridine nitrogens on trypanocidal activity, transport kinetics, and resistance patterns

scientific article

Trypanosoma brucei Methylthioadenosine Phosphorylase Protects the Parasite from the Antitrypanosomal Effect of Deoxyadenosine: IMPLICATIONS FOR THE PHARMACOLOGY OF ADENOSINE ANTIMETABOLITES.

scientific article

Trypanosoma brucei adenine-phosphoribosyltransferases mediate adenine salvage and aminopurinol susceptibility but not adenine toxicity

scientific article published on 19 December 2013

Trypanosoma brucei aquaglyceroporin 2 is a high-affinity transporter for pentamidine and melaminophenyl arsenic drugs and the main genetic determinant of resistance to these drugs

scientific article

Trypanosoma brucei: A survey of pyrimidine transport activities

article published in 2006

Trypanosoma brucei: expression of multiple purine transporters prevents the development of allopurinol resistance

scientific article

Uptake of pentamidine in Trypanosoma brucei brucei is mediated by the P2 adenosine transporter and at least one novel, unrelated transporter

scientific article published in December 2001

Uptake of purines in Plasmodium falciparum-infected human erythrocytes is mostly mediated by the human Equilibrative Nucleoside Transporter and the human Facilitative Nucleobase Transporter

Uptake of purines in Plasmodium falciparum-infected human erythrocytes is mostly mediated by the human equilibrative nucleoside transporter and the human facilitative nucleobase transporter

scientific article published on 29 January 2010

Validation of novel fluorescence assays for the routine screening of drug susceptibilities of Trichomonas vaginalis

scientific article

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