ArticleCell chemical biology2018
Target Identification and Mechanism of Action of Picolinamide and Benzamide Chemotypes with Antifungal Properties.
Article in Cell chemical biology, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
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.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
15 citing papers in PubMed, 31 citations in OpenAlex.
- A brief history of phosphatidylinositol transfer proteins: from the backwaters of cell biology to prime time in lipid signaling.Biochimica et biophysica acta. Molecular and cell biology of lipids · 2025Review
- Beyond Ergosterol: Strategies for Combatting Antifungal Resistance inTetrahedron · 2023Article
- Article
- Small molecules for combating multidrug-resistant superbugActa pharmaceutica Sinica. B · 2022Review
- Cellular Target Deconvolution of Small Molecules Using a Selection-Based Genetic Screening Platform.ACS central science · 2022Article
- New strategies for combating fungal infections: Inhibiting inositol lipid signaling by targeting Sec14 phosphatidylinositol transfer proteins.Advances in biological regulation · 2022Review
- Bis(N-picolinamido)cobalt(II) Complexes Display Antifungal Activity toward Candida albicans and Aspergillus fumigatus.ChemMedChem · 2021Article
- Biological and computational studies provide insights intoBiochemistry and biophysics reports · 2021Article
- Emerging Prospects for Combating Fungal Infections by Targeting Phosphatidylinositol Transfer Proteins.International journal of molecular sciences · 2021Review
- Chemical-Genetic Interactions as a Means to Characterize Drug Synergy.Methods in molecular biology (Clifton, N.J.) · 2021Review
- From Phenotypic Hit to Chemical Probe: Chemical Biology Approaches to Elucidate Small Molecule Action in Complex Biological Systems.Molecules (Basel, Switzerland) · 2020Review
- A marine microbiome antifungal targets urgent-threat drug-resistant fungi.Science (New York, N.Y.) · 2020Article
- An equal opportunity collaboration between lipid metabolism and proteins in the control of membrane trafficking in the trans-Golgi and endosomal systems.Current opinion in cell biology · 2019Review
- A Critical Review on Selected External Physical Cues and Modulation of Cell Behavior: Magnetic Nanoparticles, Non-thermal Plasma and Lasers.Journal of functional biomaterials · 2018Review
- Synthesis, Antifungal Activities and Molecular Docking Studies of Benzoxazole and Benzothiazole Derivatives.Molecules (Basel, Switzerland) · 2018Article
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Authors and funding
19 authors at 7 institutions in 3 countries.
Funding
Abstract
Invasive fungal infections are accompanied by high mortality rates that range up to 90%. At present, only three different compound classes are available for use in the clinic, and these often suffer from low bioavailability, toxicity, and drug resistance. These issues emphasize an urgent need for novel antifungal agents. Herein, we report the identification of chemically versatile benzamide and picolinamide scaffolds with antifungal properties. Chemogenomic profiling and biochemical assays with purified protein identified Sec14p, the major phosphatidylinositol/phosphatidylcholine transfer protein in Saccharomyces cerevisiae, as the sole essential target for these compounds. A functional variomics screen identified resistance-conferring residues that localized to the lipid-binding pocket of Sec14p. Determination of the X-ray co-crystal structure of a Sec14p-compound complex confirmed binding in this cavity and rationalized both the resistance-conferring residues and the observed structure-activity relationships. Taken together, these findings open new avenues for rational compound optimization and development of novel antifungal agents.
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What Socratic 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 Socratic graph.