Experimental Strategies to Explore Drug Action and Resistance in Kinetoplastid Parasites
Kinetoplastids are the causative agents of leishmaniasis, human African trypanosomiasis, and American trypanosomiasis. They are responsible for high mortality and morbidity in (sub)tropical regions. Adequate treatment options are limited and have several drawbacks, such as toxicity, need for parente...
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| Format: | Article |
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MDPI AG
2020-06-01
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| Series: | Microorganisms |
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| Online Access: | https://www.mdpi.com/2076-2607/8/6/950 |
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| author | Magali Van den Kerkhof Yann G.-J. Sterckx Philippe Leprohon Louis Maes Guy Caljon |
| author_facet | Magali Van den Kerkhof Yann G.-J. Sterckx Philippe Leprohon Louis Maes Guy Caljon |
| author_sort | Magali Van den Kerkhof |
| collection | DOAJ |
| description | Kinetoplastids are the causative agents of leishmaniasis, human African trypanosomiasis, and American trypanosomiasis. They are responsible for high mortality and morbidity in (sub)tropical regions. Adequate treatment options are limited and have several drawbacks, such as toxicity, need for parenteral administration, and occurrence of treatment failure and drug resistance. Therefore, there is an urgency for the development of new drugs. Phenotypic screening already allowed the identification of promising new chemical entities with anti-kinetoplastid activity potential, but knowledge on their mode-of-action (MoA) is lacking due to the generally applied whole-cell based approach. However, identification of the drug target is essential to steer further drug discovery and development. Multiple complementary techniques have indeed been used for MoA elucidation. In this review, the different ‘omics’ approaches employed to define the MoA or mode-of-resistance of current reference drugs and some new anti-kinetoplastid compounds are discussed. |
| first_indexed | 2024-03-10T18:55:53Z |
| format | Article |
| id | doaj.art-f3e470960ffb4fe090dbda7325524fe8 |
| institution | Directory Open Access Journal |
| issn | 2076-2607 |
| language | English |
| last_indexed | 2024-03-10T18:55:53Z |
| publishDate | 2020-06-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Microorganisms |
| spelling | doaj.art-f3e470960ffb4fe090dbda7325524fe82023-11-20T04:48:54ZengMDPI AGMicroorganisms2076-26072020-06-018695010.3390/microorganisms8060950Experimental Strategies to Explore Drug Action and Resistance in Kinetoplastid ParasitesMagali Van den Kerkhof0Yann G.-J. Sterckx1Philippe Leprohon2Louis Maes3Guy Caljon4Laboratory of Microbiology, Parasitology and Hygiene (LMPH), University of Antwerp, 2610 Wilrijk, BelgiumLaboratory of Medical Biochemistry (LMB), University of Antwerp, 2610 Wilrijk, BelgiumCentre de Recherche en Infectiologie du Centre de Recherche du Centre Hospitalier Universitaire de Québec, Université Laval, Québec, QC G1V 0A6, CanadaLaboratory of Microbiology, Parasitology and Hygiene (LMPH), University of Antwerp, 2610 Wilrijk, BelgiumLaboratory of Microbiology, Parasitology and Hygiene (LMPH), University of Antwerp, 2610 Wilrijk, BelgiumKinetoplastids are the causative agents of leishmaniasis, human African trypanosomiasis, and American trypanosomiasis. They are responsible for high mortality and morbidity in (sub)tropical regions. Adequate treatment options are limited and have several drawbacks, such as toxicity, need for parenteral administration, and occurrence of treatment failure and drug resistance. Therefore, there is an urgency for the development of new drugs. Phenotypic screening already allowed the identification of promising new chemical entities with anti-kinetoplastid activity potential, but knowledge on their mode-of-action (MoA) is lacking due to the generally applied whole-cell based approach. However, identification of the drug target is essential to steer further drug discovery and development. Multiple complementary techniques have indeed been used for MoA elucidation. In this review, the different ‘omics’ approaches employed to define the MoA or mode-of-resistance of current reference drugs and some new anti-kinetoplastid compounds are discussed.https://www.mdpi.com/2076-2607/8/6/950kinetoplastidresistancetargetdrugomicsmechanism |
| spellingShingle | Magali Van den Kerkhof Yann G.-J. Sterckx Philippe Leprohon Louis Maes Guy Caljon Experimental Strategies to Explore Drug Action and Resistance in Kinetoplastid Parasites Microorganisms kinetoplastid resistance target drug omics mechanism |
| title | Experimental Strategies to Explore Drug Action and Resistance in Kinetoplastid Parasites |
| title_full | Experimental Strategies to Explore Drug Action and Resistance in Kinetoplastid Parasites |
| title_fullStr | Experimental Strategies to Explore Drug Action and Resistance in Kinetoplastid Parasites |
| title_full_unstemmed | Experimental Strategies to Explore Drug Action and Resistance in Kinetoplastid Parasites |
| title_short | Experimental Strategies to Explore Drug Action and Resistance in Kinetoplastid Parasites |
| title_sort | experimental strategies to explore drug action and resistance in kinetoplastid parasites |
| topic | kinetoplastid resistance target drug omics mechanism |
| url | https://www.mdpi.com/2076-2607/8/6/950 |
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