| Structure-activity relationships, kinetics, selectivity, and mechanistic studies of synthetic hydraphile channels in bacterial and mammalian cells. | |
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MedLine Citation:
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PMID: 16172693 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Hydraphile compounds are shown to be cytotoxic to Gram-negative and Gram-positive bacteria, yeast, and mammalian cells. Their cellular toxicity compares favorably with other synthetic ionophores and rivals that potency of natural antibiotics. The effects of structural variations on toxicity are described. The effects of these variations correlate well with previous studies of ion transport in liposomes. Whole cell patch clamping with mammalian cells confirms a channel mechanism in living cells suggesting that this family may comprise novel and flexible pharmacological agents. |
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Authors:
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W Matthew Leevy; Seth T Gammon; Tatiana Levchenko; David D Daranciang; Oscar Murillo; Vladimir Torchilin; David Piwnica-Worms; James E Huettner; George W Gokel |
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Publication Detail:
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Type: Comparative Study; Journal Article; Research Support, N.I.H., Extramural; Research Support, U.S. Gov't, P.H.S. Date: 2005-08-26 |
Journal Detail:
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Title: Organic & biomolecular chemistry Volume: 3 ISSN: 1477-0520 ISO Abbreviation: Org. Biomol. Chem. Publication Date: 2005 Oct |
Date Detail:
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Created Date: 2005-09-20 Completed Date: 2006-01-10 Revised Date: 2013-04-12 |
Medline Journal Info:
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Nlm Unique ID: 101154995 Medline TA: Org Biomol Chem Country: England |
Other Details:
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Languages: eng Pagination: 3544-50 Citation Subset: IM |
Affiliation:
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Department of Molecular Biology & Pharmacology, Washington University School of Medicine, Campus Box 8103, 660 S. Euclid Avenue, St. Louis, MO 63110, USA. ggokel@wustl.edu. |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Animals Anti-Infective Agents / chemical synthesis, pharmacology Bacteria / metabolism* Cells, Cultured Ion Channels / chemical synthesis*, metabolism Kinetics Liposomes / metabolism Patch-Clamp Techniques Structure-Activity Relationship Time Factors Yeasts / metabolism* |
| Grant Support | |
ID/Acronym/Agency:
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GM-36262/GM/NIGMS NIH HHS; NS-30888/NS/NINDS NIH HHS; P50 CA094056-05/CA/NCI NIH HHS; P50 CA94056/CA/NCI NIH HHS; R01 GM036262-22/GM/NIGMS NIH HHS; R01 NS030888-13/NS/NINDS NIH HHS; T32-GM04892/GM/NIGMS NIH HHS |
| Chemical | |
Reg. No./Substance:
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0/Anti-Infective Agents; 0/Ion Channels; 0/Liposomes |
| Comments/Corrections | |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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