ArticleJournal of medicinal chemistry2012
Head-to-head prenyl tranferases: anti-infective drug targets.
Article in Journal of medicinal chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 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
11 citing papers in PubMed.
- Adamantane-thiazole hybrids and related derivatives: synthesis, crystal structures, in vitro antibacterial, antifungal, and anti-proliferative activities.BMC chemistry · 2026Article
- Review
- Structure, catalysis, and inhibition mechanism of prenyltransferase.IUBMB life · 2021Review
- Structural and Chemical Biology of Terpenoid Cyclases.Chemical reviews · 2017Review
- Activity of Fluorine-Containing Analogues of WC-9 and Structurally Related Analogues against Two Intracellular Parasites: Trypanosoma cruzi and Toxoplasma gondii.ChemMedChem · 2016Article
- Antiinfectives targeting enzymes and the proton motive force.Proceedings of the National Academy of Sciences of the United States of America · 2015Article
- Aryloxyethyl Thiocyanates Are Potent Growth Inhibitors of Trypanosoma cruzi and Toxoplasma gondii.ChemMedChem · 2015Article
- SQ109, a new drug lead for Chagas disease.Antimicrobial agents and chemotherapy · 2015Article
- Squalene synthase as a target for Chagas disease therapeutics.PLoS pathogens · 2014Article
- Multitarget drug discovery for tuberculosis and other infectious diseases.Journal of medicinal chemistry · 2014Article
- Design, synthesis and biological evaluation of WC-9 analogs as antiparasitic agents.European journal of medicinal chemistry · 2013Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
8 authors.
Funding
Abstract
We report X-ray crystallographic structures of three inhibitors bound to dehydrosqualene synthase from Staphylococcus aureus: 1 (BPH-651), 2 (WC-9), and 3 (SQ-109). Compound 2 binds to the S2 site with its -SCN group surrounded by four hydrogen bond donors. With 1, we report two structures: in both, the quinuclidine headgroup binds in the allylic (S1) site with the side chain in S2, but in the presence of PPi and Mg(2+), the quinuclidine's cationic center interacts with PPi and three Mg(2+), mimicking a transition state involved in diphosphate ionization. With 3, there are again two structures. In one, the geranyl side chain binds to either S1 or S2 and the adamantane headgroup binds to S1. In the second, the side chain binds to S2 while the headgroup binds to S1. These results provide structural clues for the mechanism and inhibition of the head-to-head prenyl transferases and should aid future drug design.
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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.