Seifert, Roland and Dove, Stefan (2012) Towards selective inhibitors of adenylyl cyclase toxin from Bordetella pertussis. TRENDS IN MICROBIOLOGY, 20 (7). pp. 343-351. ISSN 0966-842X, 1878-4380
Full text not available from this repository. (Request a copy)Abstract
Whooping cough is a very important medical problem that requires novel approaches for treatment. The disease is caused by Bordetella pertussis, with the calmodulin (CaM)-activated adenylyl cyclase (AC) toxin (also known as CyaA) being a major virulence factor. Hence, CyaA inhibitors could constitute novel therapeutics, but it has been difficult to develop potent drugs with high selectivity over mammalian membranous ACs (mACs). Recent studies have shown that bis-anthraniloyl-substituted nucleoside 5'-triphosphates are potent and selective CyaA inhibitors. In addition, the interaction of CyaA with CaM is very different from the interaction of membranous mAC1 with CaM. Accordingly, compounds that interfere with the CyaA-CaM interaction may constitute a novel class of drugs against whooping cough.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | SOLUBLE GUANYLYL CYCLASE; ANTHRACIS EDEMA FACTOR; CALMODULIN ANTAGONISTS; STRUCTURAL BASIS; NUCLEOSIDE 5'-TRIPHOSPHATES; DIFFERENTIAL INHIBITION; PYRIMIDINE NUCLEOTIDES; WHOOPING-COUGH; ISOFORMS; ANALOGS; adenylyl cyclase; Bordetella pertussis; CyaA; calmodulin; cyclic AMP; inhibitor |
| Subjects: | 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy > Alumni or Retired Professors > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer) |
| Depositing User: | Petra Gürster |
| Date Deposited: | 18 May 2020 06:09 |
| Last Modified: | 18 May 2020 06:09 |
| URI: | https://pred.uni-regensburg.de/id/eprint/18492 |
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