ArticleAntimicrobial agents and chemotherapy2013
Antiplasmodial activity and mechanism of action of RSM-932A, a promising synergistic inhibitor of Plasmodium falciparum choline kinase.
Article in Antimicrobial agents and chemotherapy, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed, 29 citations in OpenAlex.
- Identification and Characterization of Entamoeba histolytica Choline Kinase.Acta parasitologica · 2024Article
- Is choline kinase alpha a drug target for obesity?Frontiers in endocrinology · 2024Article
- Quercetin Is a Novel Inhibitor of the Choline Kinase ofAntibiotics (Basel, Switzerland) · 2022Article
- Novel Non-Congeneric Derivatives of the Choline Kinase Alpha Inhibitor ICL-CCIC-0019.Pharmaceutics · 2021Article
- Choline Kinase: An Unexpected Journey for a Precision Medicine Strategy in Human Diseases.Pharmaceutics · 2021Review
- ChoK-ing the Pathogenic Bacteria: Potential of Human Choline Kinase Inhibitors as Antimicrobial Agents.BioMed research international · 2020Review
- Molecular basis for the interaction between human choline kinase alpha and the SH3 domain of the c-Src tyrosine kinase.Scientific reports · 2019Article
- Choline Kinase Emerges as a Promising Drug Target in Gram-Positive Bacteria.Frontiers in microbiology · 2019Article
- Parallel Colorimetric Quantification of Choline and Phosphocholine as a Method for Studying Choline Kinase Activity in Complex Mixtures.Antibiotics (Basel, Switzerland) · 2018Article
- Choline Kinase, A Novel Drug Target for the Inhibition of Streptococcus pneumoniae.Antibiotics (Basel, Switzerland) · 2017Article
- Choline kinase inhibition in rheumatoid arthritis.Annals of the rheumatic diseases · 2015Article
- A new family of choline kinase inhibitors with antiproliferative and antitumor activity derived from natural products.Clinical & translational oncology : official publication of the Federation of Spanish Oncology Societies and of the National Cancer Institute of Mexico · 2015Article
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Authors and funding
7 authors at 4 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
We have investigated the mechanism of action of inhibition of the choline kinase of P. falciparum (p.f.-ChoK) by two inhibitors of the human ChoKα, MN58b and RSM-932A, which have previously been shown to be potent antitumoral agents. The efficacy of these inhibitors against p.f.-ChoK is investigated using enzymatic and in vitro assays. While MN58b may enter the choline/phosphocholine binding site, RSM-932A appears to have an altogether novel mechanism of inhibition and is synergistic with respect to both choline and ATP. A model of inhibition for RSM-932A in which this inhibitor traps p.f.-ChoK in a phosphorylated intermediate state blocking phosphate transfer to choline is presented. Importantly, MN58b and RSM-932A have in vitro inhibitory activity in the low nanomolar range and are equally effective against chloroquine-sensitive and chloroquine-resistant strains. RSM-932A and MN58b significantly reduced parasitemia and induced the accumulation of trophozoites and schizonts, blocking intraerythrocytic development and interfering with parasite egress or invasion, suggesting a delay of the parasite maturation stage. The present data provide two new potent structures for the development of antimalarial compounds and validate p.f.-ChoK as an accessible drug target against the parasite.
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