ArticlePloS one2014
Selectivity and potency of microcystin congeners against OATP1B1 and OATP1B3 expressing cancer cells.
Article in PloS one, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
27 citing papers in PubMed, 75 citations in OpenAlex.
- Cyanopeptide Mixtures Induce Variable Synergistic and Antagonistic Effects Across Diverse Human Cell Lines.Environmental toxicology · 2026Article
- Mechanistic investigation of the hepatotoxicity and potential carcinogenicity of microcystin-LR, -LA, and -RR in the HepaRG cell line model.Archives of toxicology · 2026Article
- Transporter-Mediated Uptake of Microcystin-LR in Human Trophoblasts: Regulation By Oxygen Concentration and Cell Fusion.bioRxiv : the preprint server for biology · 2026Article
- Biotransformation Dynamics and Products of Cyanobacterial Secondary Metabolites in Surface Waters.Environmental science & technology · 2025Article
- Cyanobacterial Peptides in Anticancer Therapy: A Comprehensive Review of Mechanisms, Clinical Advances, and Biotechnological Innovation.Marine drugs · 2025Review
- Derivatization of Microcystins Can Increase Target Inhibition while Reducing Cellular Uptake.Journal of natural products · 2025Article
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- Article
- Aerosolized Cyanobacterial Harmful Algal Bloom Toxins: Microcystin Congeners Quantified in the Atmosphere.Environmental science & technology · 2023Article
- A Summer of Cyanobacterial Blooms in Belgian Waterbodies: Microcystin Quantification and Molecular Characterizations.Toxins · 2022Article
- Congeners-Specific Intestinal Absorption Of Microcystins In AnFrontiers in toxicology · 2022Article
- Natural Cyclopeptides as Anticancer Agents in the Last 20 Years.International journal of molecular sciences · 2021Review
- The tide turns: Episodic and localized cross-contamination of a California coastline with cyanotoxins.Harmful algae · 2021Article
- Article
- Rapid uptake and slow depuration: Health risks following cyanotoxin accumulation in mussels?Environmental pollution (Barking, Essex : 1987) · 2021Article
- Microcystins and Microcystis aeruginosa PCC7806 extracts modulate steroidogenesis differentially in the human H295R adrenal model.PloS one · 2020Article
- Review
- Article
- Sub-Chronic Microcystin-LR Liver Toxicity in Preexisting Diet-Induced Nonalcoholic Steatohepatitis in Rats.Toxins · 2019Article
- Antiproliferative, neurotoxic, genotoxic and mutagenic effects of toxic cyanobacterial extracts.Interdisciplinary toxicology · 2018Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
4 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Microcystins are potent phosphatase inhibitors and cellular toxins. They require active transport by OATP1B1 and OATP1B3 transporters for uptake into human cells, and the high expression of these transporters in the liver accounts for their selective hepatic toxicity. Several human tumors have been shown to have high levels of expression of OATP1B3 but not OATP1B1, the main transporter in liver cells. We hypothesized that microcystin variants could be isolated that are transported preferentially by OATP1B3 relative to OATP1B1 to advance as anticancer agents with clinically tolerable hepatic toxicity. Microcystin variants have been isolated and tested for cytotoxicity in cancer cells stably transfected with OATP1B1 and OATP1B3 transporters. Microcystin variants with cytotoxic OATP1B1/OATP1B3 IC50 ratios that ranged between 0.2 and 32 were found, representing a 150-fold range in transporter selectivity. As microcystin structure has a significant impact on transporter selectivity, it is potentially possible to develop analogs with even more pronounced OATP1B3 selectivity and thus enable their development as anticancer drugs.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.