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Items: 1 to 50 of 129

1.

European propolis is highly active against trypanosomatids including Crithidia fasciculata.

Alotaibi A, Ebiloma GU, Williams R, Alenezi S, Donachie AM, Guillaume S, Igoli JO, Fearnley J, de Koning HP, Watson DG.

Sci Rep. 2019 Aug 6;9(1):11364. doi: 10.1038/s41598-019-47840-y.

2.

Discovery of novel Schistosoma mansoni PDE4A inhibitors as potential agents against schistosomiasis.

Sebastián-Pérez V, Schroeder S, Munday JC, van der Meer T, Zaldívar-Díez J, Siderius M, de Koning HP, Brown D, Martínez A, Campillo NE, Leurs R, Gil C.

Future Med Chem. 2019 Jul;11(14):1703-1720. doi: 10.4155/fmc-2018-0592. Epub 2019 Aug 2.

PMID:
31370708
3.

Alkynamide phthalazinones as a new class of TbrPDEB1 inhibitors.

de Heuvel E, Singh AK, Edink E, van der Meer T, van der Woude M, Sadek P, Krell-Jørgensen MP, van den Bergh T, Veerman J, Caljon G, Kalejaiye TD, Wijtmans M, Maes L, de Koning HP, Jan Sterk G, Siderius M, de Esch IJP, Brown DG, Leurs R.

Bioorg Med Chem. 2019 Sep 15;27(18):3998-4012. doi: 10.1016/j.bmc.2019.06.027. Epub 2019 Jun 18.

4.

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

Alkhaldi AA, de Koning HP, Bukhari SNA.

Drug Des Devel Ther. 2019 Apr 24;13:1179-1185. doi: 10.2147/DDDT.S204733. eCollection 2019.

5.

Isolation of a Novel Flavanonol and an Alkylresorcinol with Highly Potent Anti-Trypanosomal Activity from Libyan propolis.

Siheri W, Ebiloma GU, Igoli JO, Gray AI, Biddau M, Akrachalanont P, Alenezi S, Alwashih MA, Edrada-Ebel R, Muller S, Lawrence CE, Fearnley J, Watson DG, De Koning HP.

Molecules. 2019 Mar 15;24(6). pii: E1041. doi: 10.3390/molecules24061041.

6.

Novel Minor Groove Binders Cure Animal African Trypanosomiasis in an in Vivo Mouse Model.

Giordani F, Khalaf AI, Gillingwater K, Munday JC, de Koning HP, Suckling CJ, Barrett MP, Scott FJ.

J Med Chem. 2019 Mar 28;62(6):3021-3035. doi: 10.1021/acs.jmedchem.8b01847. Epub 2019 Mar 13.

PMID:
30763102
7.

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

Ebiloma GU, Balogun EO, Cueto-Díaz EJ, de Koning HP, Dardonville C.

Med Res Rev. 2019 Sep;39(5):1553-1602. doi: 10.1002/med.21560. Epub 2019 Jan 29. Review.

PMID:
30693533
8.

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

Eze AA, Igoli J, Gray AI, Skellern GG, De Koning HP.

Int J Parasitol Drugs Drug Resist. 2019 Apr;9:54-58. doi: 10.1016/j.ijpddr.2019.01.003. Epub 2019 Jan 21.

9.

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

Hulpia F, Campagnaro GD, Scortichini M, Van Hecke K, Maes L, de Koning HP, Caljon G, Van Calenbergh S.

Eur J Med Chem. 2019 Feb 15;164:689-705. doi: 10.1016/j.ejmech.2018.12.050. Epub 2018 Dec 21.

PMID:
30677668
10.

Imidazole Derivatives as Promising Agents for the Treatment of Chagas Disease.

de Araújo JS, García-Rubia A, Sebastián-Pérez V, Kalejaiye TD, Bernardino da Silva P, Fonseca-Berzal CR, Maes L, De Koning HP, Soeiro MNC, Gil C.

Antimicrob Agents Chemother. 2019 Mar 27;63(4). pii: e02156-18. doi: 10.1128/AAC.02156-18. Print 2019 Apr.

PMID:
30670432
11.

Screening of a PDE-focused library identifies imidazoles with in vitro and in vivo antischistosomal activity.

Botros SS, William S, Sabra AA, El-Lakkany NM, Seif El-Din SH, García-Rubia A, Sebastián-Pérez V, Blaazer AR, de Heuvel E, Sijm M, Zheng Y, Salado IG, Munday JC, Maes L, de Esch IJP, Sterk GJ, Augustyns K, Leurs R, Gil C, De Koning HP.

Int J Parasitol Drugs Drug Resist. 2019 Apr;9:35-43. doi: 10.1016/j.ijpddr.2019.01.001. Epub 2019 Jan 14.

12.

Discovery of Sustainable Drugs for Neglected Tropical Diseases: Cashew Nut Shell Liquid (CNSL)-Based Hybrids Target Mitochondrial Function and ATP Production in Trypanosoma brucei.

Cerone M, Uliassi E, Prati F, Ebiloma GU, Lemgruber L, Bergamini C, Watson DG, de A M Ferreira T, Roth Cardoso GSH, Soares Romeiro LA, de Koning HP, Bolognesi ML.

ChemMedChem. 2019 Mar 22;14(6):621-635. doi: 10.1002/cmdc.201800790. Epub 2019 Feb 5.

13.

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

Nnadi CO, Ebiloma GU, Black JA, Nwodo NJ, Lemgruber L, Schmidt TJ, de Koning HP.

Molecules. 2019 Jan 12;24(2). pii: E268. doi: 10.3390/molecules24020268.

14.

SAR of 4-Alkoxybenzoic Acid Inhibitors of the Trypanosome Alternative Oxidase.

Meco-Navas A, Ebiloma GU, Martín-Domínguez A, Martínez-Benayas I, Cueto-Díaz EJ, Alhejely AS, Balogun EO, Saito M, Matsui M, Arai N, Shiba T, Harada S, de Koning HP, Dardonville C.

ACS Med Chem Lett. 2018 Jul 31;9(9):923-928. doi: 10.1021/acsmedchemlett.8b00282. eCollection 2018 Sep 13.

15.

Cloning and characterisation of the Equilibrative Nucleoside Transporter family of Trypanosoma cruzi: ultra-high affinity and selectivity to survive in the intracellular niche.

Campagnaro GD, de Freitas Nascimento J, Girard RBM, Silber AM, de Koning HP.

Biochim Biophys Acta Gen Subj. 2018 Dec;1862(12):2750-2763. doi: 10.1016/j.bbagen.2018.08.015. Epub 2018 Aug 24.

PMID:
30251664
16.

Targeting a Subpocket in Trypanosoma brucei Phosphodiesterase B1 (TbrPDEB1) Enables the Structure-Based Discovery of Selective Inhibitors with Trypanocidal Activity.

Blaazer AR, Singh AK, de Heuvel E, Edink E, Orrling KM, Veerman JJN, van den Bergh T, Jansen C, Balasubramaniam E, Mooij WJ, Custers H, Sijm M, Tagoe DNA, Kalejaiye TD, Munday JC, Tenor H, Matheeussen A, Wijtmans M, Siderius M, de Graaf C, Maes L, de Koning HP, Bailey DS, Sterk GJ, de Esch IJP, Brown DG, Leurs R.

J Med Chem. 2018 May 10;61(9):3870-3888. doi: 10.1021/acs.jmedchem.7b01670. Epub 2018 May 1.

17.

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

Ebiloma GU, Katsoulis E, Igoli JO, Gray AI, De Koning HP.

Sci Rep. 2018 Mar 15;8(1):4613. doi: 10.1038/s41598-018-22908-3.

18.

Inhibition of trypanosome alternative oxidase without its N-terminal mitochondrial targeting signal (ΔMTS-TAO) by cationic and non-cationic 4-hydroxybenzoate and 4-alkoxybenzaldehyde derivatives active against T. brucei and T. congolense.

Ebiloma GU, Ayuga TD, Balogun EO, Gil LA, Donachie A, Kaiser M, Herraiz T, Inaoka DK, Shiba T, Harada S, Kita K, de Koning HP, Dardonville C.

Eur J Med Chem. 2018 Apr 25;150:385-402. doi: 10.1016/j.ejmech.2018.02.075. Epub 2018 Feb 26.

PMID:
29544150
19.

Trypanosoma brucei bloodstream forms express highly specific and separate transporters for adenine and hypoxanthine; evidence for a new protozoan purine transporter family?

Campagnaro GD, Alzahrani KJ, Munday JC, De Koning HP.

Mol Biochem Parasitol. 2018 Mar;220:46-56. doi: 10.1016/j.molbiopara.2018.01.005. Epub 2018 Jan 31.

PMID:
29371154
20.

Functional and structural analysis of AT-specific minor groove binders that disrupt DNA-protein interactions and cause disintegration of the Trypanosoma brucei kinetoplast.

Millan CR, Acosta-Reyes FJ, Lagartera L, Ebiloma GU, Lemgruber L, Nué Martínez JJ, Saperas N, Dardonville C, de Koning HP, Campos JL.

Nucleic Acids Res. 2017 Aug 21;45(14):8378-8391. doi: 10.1093/nar/gkx521.

21.

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

Alzahrani KJH, Ali JAM, Eze AA, Looi WL, Tagoe DNA, Creek DJ, Barrett MP, de Koning HP.

Int J Parasitol Drugs Drug Resist. 2017 Aug;7(2):206-226. doi: 10.1016/j.ijpddr.2017.04.003. Epub 2017 Apr 20.

22.

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

Omar R, Igoli JO, Zhang T, Gray AI, Ebiloma GU, Clements CJ, Fearnley J, Edrada Ebel R, Paget T, de Koning HP, Watson DG.

Sci Rep. 2017 Apr 19;7(1):923. doi: 10.1038/s41598-017-01038-2.

23.

9-(2'-Deoxy-2'-Fluoro-β-d-Arabinofuranosyl) Adenine Is a Potent Antitrypanosomal Adenosine Analogue That Circumvents Transport-Related Drug Resistance.

Ranjbarian F, Vodnala M, Alzahrani KJH, Ebiloma GU, de Koning HP, Hofer A.

Antimicrob Agents Chemother. 2017 May 24;61(6). pii: e02719-16. doi: 10.1128/AAC.02719-16. Print 2017 Jun.

24.

Bioassay-guided isolation of active principles from Nigerian medicinal plants identifies new trypanocides with low toxicity and no cross-resistance to diamidines and arsenicals.

Ebiloma GU, Igoli JO, Katsoulis E, Donachie AM, Eze A, Gray AI, de Koning HP.

J Ethnopharmacol. 2017 Apr 18;202:256-264. doi: 10.1016/j.jep.2017.03.028. Epub 2017 Mar 20.

PMID:
28336470
25.

Conjugates of 2,4-Dihydroxybenzoate and Salicylhydroxamate and Lipocations Display Potent Antiparasite Effects by Efficiently Targeting the Trypanosoma brucei and Trypanosoma congolense Mitochondrion.

Fueyo González FJ, Ebiloma GU, Izquierdo García C, Bruggeman V, Sánchez Villamañán JM, Donachie A, Balogun EO, Inaoka DK, Shiba T, Harada S, Kita K, de Koning HP, Dardonville C.

J Med Chem. 2017 Feb 23;60(4):1509-1522. doi: 10.1021/acs.jmedchem.6b01740. Epub 2017 Feb 9.

PMID:
28112515
26.

Exploiting the Achilles' heel of membrane trafficking in trypanosomes.

Zoltner M, Horn D, de Koning HP, Field MC.

Curr Opin Microbiol. 2016 Dec;34:97-103. doi: 10.1016/j.mib.2016.08.005. Epub 2016 Sep 9. Review.

27.

The animal trypanosomiases and their chemotherapy: a review.

Giordani F, Morrison LJ, Rowan TG, DE Koning HP, Barrett MP.

Parasitology. 2016 Dec;143(14):1862-1889. Epub 2016 Oct 10. Review.

28.

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.

Eze AA, Gould MK, Munday JC, Tagoe DN, Stelmanis V, Schnaufer A, De Koning HP.

PLoS Negl Trop Dis. 2016 Aug 12;10(8):e0004791. doi: 10.1371/journal.pntd.0004791. eCollection 2016 Aug.

29.

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

Dike VT, Vihiior B, Bosha JA, Yin TM, Ebiloma GU, de Koning HP, Igoli JO, Gray AI.

Phytochem Anal. 2016 May;27(3-4):217-21. doi: 10.1002/pca.2619.

PMID:
27313159
30.

Chemical and Antimicrobial Profiling of Propolis from Different Regions within Libya.

Siheri W, Zhang T, Ebiloma GU, Biddau M, Woods N, Hussain MY, Clements CJ, Fearnley J, Ebel RE, Paget T, Muller S, Carter KC, Ferro VA, De Koning HP, Watson DG.

PLoS One. 2016 May 19;11(5):e0155355. doi: 10.1371/journal.pone.0155355. eCollection 2016.

31.

Seroepidemiology and molecular diversity of Leishmania donovani complex in Georgia.

Babuadze G, Farlow J, de Koning HP, Carrillo E, Chakhunashvili G, Murskvaladze M, Kekelidze M, Karseladze I, Kokaia N, Kalandadze I, Tsereteli D, Markhvashvili I, Sidamonidze K, Chanturia G, Adeishvili E, Imnadze P.

Parasit Vectors. 2016 May 13;9(1):279. doi: 10.1186/s13071-016-1558-6.

32.

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

Alkhaldi AAM, Martinek J, Panicucci B, Dardonville C, Zíková A, de Koning HP.

Int J Parasitol Drugs Drug Resist. 2015 Dec 11;6(1):23-34. doi: 10.1016/j.ijpddr.2015.12.002. eCollection 2016 Apr.

33.

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

Vodnala M, Ranjbarian F, Pavlova A, de Koning HP, Hofer A.

J Biol Chem. 2016 May 27;291(22):11717-26. doi: 10.1074/jbc.M116.715615. Epub 2016 Apr 1.

34.

Evolutionary genomics of epidemic visceral leishmaniasis in the Indian subcontinent.

Imamura H, Downing T, Van den Broeck F, Sanders MJ, Rijal S, Sundar S, Mannaert A, Vanaerschot M, Berg M, De Muylder G, Dumetz F, Cuypers B, Maes I, Domagalska M, Decuypere S, Rai K, Uranw S, Bhattarai NR, Khanal B, Prajapati VK, Sharma S, Stark O, Schönian G, De Koning HP, Settimo L, Vanhollebeke B, Roy S, Ostyn B, Boelaert M, Maes L, Berriman M, Dujardin JC, Cotton JA.

Elife. 2016 Mar 22;5. pii: e12613. doi: 10.7554/eLife.12613.

35.

Comparative genomics of drug resistance in Trypanosoma brucei rhodesiense.

Graf FE, Ludin P, Arquint C, Schmidt RS, Schaub N, Kunz Renggli C, Munday JC, Krezdorn J, Baker N, Horn D, Balmer O, Caccone A, de Koning HP, Mäser P.

Cell Mol Life Sci. 2016 Sep;73(17):3387-400. doi: 10.1007/s00018-016-2173-6. Epub 2016 Mar 14.

36.

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

Omar RM, Igoli J, Gray AI, Ebiloma GU, Clements C, Fearnley J, Ebel RA, Zhang T, De Koning HP, Watson DG.

Phytochem Anal. 2016 Mar-Apr;27(2):107-15. doi: 10.1002/pca.2605. Epub 2015 Dec 11.

37.

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

Tagoe DN, Kalejaiye TD, de Koning HP.

Front Pharmacol. 2015 Sep 7;6:185. doi: 10.3389/fphar.2015.00185. eCollection 2015. Review.

38.

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

Rodenko B, Wanner MJ, Alkhaldi AA, Ebiloma GU, Barnes RL, Kaiser M, Brun R, McCulloch R, Koomen GJ, de Koning HP.

Antimicrob Agents Chemother. 2015 Nov;59(11):6708-16. doi: 10.1128/AAC.00596-15. Epub 2015 Aug 17.

39.

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

Ríos Martínez CH, Nué Martínez JJ, Ebiloma GU, de Koning HP, Alkorta I, Dardonville C.

Eur J Med Chem. 2015 Aug 28;101:806-17. doi: 10.1016/j.ejmech.2015.07.013. Epub 2015 Jul 10.

PMID:
26231081
40.

Specific Cell Targeting Therapy Bypasses Drug Resistance Mechanisms in African Trypanosomiasis.

Unciti-Broceta JD, Arias JL, Maceira J, Soriano M, Ortiz-González M, Hernández-Quero J, Muñóz-Torres M, de Koning HP, Magez S, Garcia-Salcedo JA.

PLoS Pathog. 2015 Jun 25;11(6):e1004942. doi: 10.1371/journal.ppat.1004942. eCollection 2015 Jun.

41.

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

Graf FE, Baker N, Munday JC, de Koning HP, Horn D, Mäser P.

Int J Parasitol Drugs Drug Resist. 2015 May 7;5(2):65-8. doi: 10.1016/j.ijpddr.2015.04.002. eCollection 2015 Aug.

42.

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

Munday JC, Settimo L, de Koning HP.

Front Pharmacol. 2015 Mar 9;6:32. doi: 10.3389/fphar.2015.00032. eCollection 2015. Review.

43.

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.

Munday JC, Tagoe DN, Eze AA, Krezdorn JA, Rojas López KE, Alkhaldi AA, McDonald F, Still J, Alzahrani KJ, Settimo L, De Koning HP.

Mol Microbiol. 2015 May;96(4):887-900. doi: 10.1111/mmi.12979. Epub 2015 Mar 21.

44.

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

Dardonville C, Alkhaldi AA, De Koning HP.

ACS Med Chem Lett. 2014 Dec 10;6(2):151-5. doi: 10.1021/ml500408d. eCollection 2015 Feb 12.

45.

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

Natto MJ, Eze AA, de Koning HP.

Methods Mol Biol. 2015;1263:103-10. doi: 10.1007/978-1-4939-2269-7_8.

PMID:
25618339
46.

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

Alkhaldi AA, Creek DJ, Ibrahim H, Kim DH, Quashie NB, Burgess KE, Changtam C, Barrett MP, Suksamrarn A, de Koning HP.

Mol Pharmacol. 2015;87(3):451-64. doi: 10.1124/mol.114.096016. Epub 2014 Dec 19.

PMID:
25527638
47.

Design and synthesis of a series of truncated neplanocin fleximers.

Zimmermann SC, O'Neill E, Ebiloma GU, Wallace LJ, De Koning HP, Seley-Radtke KL.

Molecules. 2014 Dec 16;19(12):21200-14. doi: 10.3390/molecules191221200.

48.

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.

Ríos Martínez CH, Miller F, Ganeshamoorthy K, Glacial F, Kaiser M, de Koning HP, Eze AA, Lagartera L, Herraiz T, Dardonville C.

Antimicrob Agents Chemother. 2015 Feb;59(2):890-904. doi: 10.1128/AAC.03958-14. Epub 2014 Nov 24.

49.

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

Shameer S, Logan-Klumpler FJ, Vinson F, Cottret L, Merlet B, Achcar F, Boshart M, Berriman M, Breitling R, Bringaud F, Bütikofer P, Cattanach AM, Bannerman-Chukualim B, Creek DJ, Crouch K, de Koning HP, Denise H, Ebikeme C, Fairlamb AH, Ferguson MA, Ginger ML, Hertz-Fowler C, Kerkhoven EJ, Mäser P, Michels PA, Nayak A, Nes DW, Nolan DP, Olsen C, Silva-Franco F, Smith TK, Taylor MC, Tielens AG, Urbaniak MD, van Hellemond JJ, Vincent IM, Wilkinson SR, Wyllie S, Opperdoes FR, Barrett MP, Jourdan F.

Nucleic Acids Res. 2015 Jan;43(Database issue):D637-44. doi: 10.1093/nar/gku944. Epub 2014 Oct 9.

50.

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

Acosta-Reyes FJ, Dardonville C, de Koning HP, Natto M, Subirana JA, Campos JL.

Acta Crystallogr D Biol Crystallogr. 2014 Jun;70(Pt 6):1614-21. doi: 10.1107/S139900471400697X. Epub 2014 May 24.

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