ArticlePloS one2012
Fascaplysin as a specific inhibitor for CDK4: insights from molecular modelling.
Article in PloS one, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 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
18 citing papers in PubMed, 52 citations in OpenAlex.
- Can Fascaplysins Be Considered Analogs of Indolo[2,3-Marine drugs · 2025Review
- Marine-Derived Leads as Anticancer Candidates by Disrupting Hypoxic Signaling through Hypoxia-Inducible Factors Inhibition.Marine drugs · 2024Review
- Marine-Derived Lead Fascaplysin: Pharmacological Activity, Total Synthesis, and Structural Modification.Marine drugs · 2023Review
- Article
- Multiomics Analysis of Spatially Distinct Stromal Cells Reveals Tumor-Induced O-Glycosylation of the CDK4-pRB Axis in Fibroblasts at the Invasive Tumor Edge.Cancer research · 2022Article
- Antitumor effect of proanthocyanidin induced apoptosis in human colorectal cancer (HT-29) cells and its molecular docking studies.BMC chemistry · 2019Article
- Lanatoside C Induces G2/M Cell Cycle Arrest and Suppresses Cancer Cell Growth by Attenuating MAPK, Wnt, JAK-STAT, and PI3K/AKT/mTOR Signaling Pathways.Biomolecules · 2019Article
- Current advances of tubulin inhibitors as dual acting small molecules for cancer therapy.Medicinal research reviews · 2019Review
- Anticancer Activity of Fascaplysin against Lung Cancer Cell and Small Cell Lung Cancer Circulating Tumor Cell Lines.Marine drugs · 2018Article
- Marine-derived protein kinase inhibitors for neuroinflammatory diseases.Biomedical engineering online · 2018Review
- Fascaplysin Sensitizes Anti-Cancer Effects of Drugs Targeting AKT and AMPK.Molecules (Basel, Switzerland) · 2017Article
- Fascaplysin Exerts Anti-Cancer Effects through the Downregulation of Survivin and HIF-1α and Inhibition of VEGFR2 and TRKA.International journal of molecular sciences · 2017Article
- Kinase inhibitor screening identifies CDK4 as a potential therapeutic target for melanoma.International journal of oncology · 2015Article
- Antitumour potential of BPT: a dual inhibitor of cdk4 and tubulin polymerization.Cell death & disease · 2015Article
- Insights on Structural Characteristics and Ligand Binding Mechanisms of CDK2.International journal of molecular sciences · 2015Review
- Cytotoxic effects of fascaplysin against small cell lung cancer cell lines.Marine drugs · 2014Article
- A survey of marine natural compounds and their derivatives with anti-cancer activity reported in 2011.Molecules (Basel, Switzerland) · 2013Review
- Marine-derived angiogenesis inhibitors for cancer therapy.Marine drugs · 2013Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
3 authors at 2 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Cyclin-dependent kinases (CDKs) play a key role in the cell cycle and are important anti-cancer drug targets. The natural product fascaplysin inhibits CDK4 with surprising selectivity (IC(50) = 0.4 µM) compared to the close homolog CDK2 (IC(50) = 500 µM). Free energy calculations of the positively charged fascaplysin and an uncharged iso-electronic derivative in the CDK2 and CDK4 inhibitor complexes indicate that the positive charge of fascaplysin is crucial for selectivity. This finding will guide further improvements in the design of fascaplysin-based selective inhibitors for CDK4.
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What OpenQuestion holds
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.