論文 - 詳細
| RRC ID | 46980 |
|---|---|
| 著者 | Ueno K, Tamura Y, Chibana H. |
| タイトル | Target validation and ligand development for a pathogenic fungal profilin, using a knock-down strain of pathogenic yeast Candida glabrata and structure-based ligand design. |
| ジャーナル | Yeast |
| Abstract |
The emergence of antifungal drug resistance is triggering vigorous searches for novel antifungal targets and lead compounds. In this study, we focused on fungal profilin, which is a small actin control protein sharing limited homology to human profilin. To validate its potentiality as a target, a profilin-conditional mutant of the pathogenic yeast Candida glabrata was constructed, using a regulatable Tet promoter, and its growth was monitored in vitro. Repression of profilin expression led to severe growth defect, demonstrating the potential of this protein as a novel antifungal target. Next, novel peptides binding to the active interface of profilin were designed by computer simulation. ELISA analysis showed that these peptides did bind to the wild-type profilin but bound less strongly to a profilin with amino acid substitutions at the active interface. Hence, we show here that profilin is a potential antifungal target and offer novel peptide ligands. |
| 巻・号 | 27(7) |
| ページ | 369-78 |
| 公開日 | 2010-7-1 |
| DOI | 10.1002/yea.1759 |
| PMID | 20148388 |
| MeSH | Antifungal Agents / metabolism Antifungal Agents / pharmacology* Candida glabrata / drug effects* Candida glabrata / genetics Candida glabrata / growth & development Computer Simulation Designer Drugs / metabolism Designer Drugs / pharmacology* Drug Design* Enzyme-Linked Immunosorbent Assay Gene Knockdown Techniques Humans Peptides / metabolism Peptides / pharmacology* Profilins / antagonists & inhibitors* Profilins / metabolism Protein Binding |
| IF | 3.143 |
| 引用数 | 1 |
| WOS 分野 | BIOTECHNOLOGY & APPLIED MICROBIOLOGY MYCOLOGY MICROBIOLOGY BIOCHEMISTRY & MOLECULAR BIOLOGY |
| オルトメトリクス指標 |
オルトメトリクス指標項目
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| 最多言及媒体 | Patent(IFI CLAIMS) |
| 各媒体での言及数の合計 | 3 |
| 過去6か月間でのオルトメトリクス指標の変動値 | 0.0 |
| リソース情報 | |
| 病原微生物 | |