at Google ScholarTitle data
Ramos-Espiritu, Lavoisier ; Kleinbölting, Silke ; Navarrete, Felipe A. ; Alvau, Antonio ; Visconti, Pablo E. ; Valsecchi, Federica ; Starkov, Anatoly ; Manfredi, Giovanni ; Buck, Hannes ; Adura, Carolina ; Zippin, Jonathan H. ; van den Heuvel, Joop ; Glickman, J. Fraser ; Steegborn, Clemens ; Levin, Lonny R. ; Buck, Jochen:
Discovery of LRE1 as a specific and allosteric inhibitor of soluble adenylyl cyclase.
In: Nature Chemical Biology.
Vol. 12
(2016)
.
- pp. 838-844.
ISSN 1552-4469
DOI: https://doi.org/10.1038/nchembio.2151
Abstract in another language
The prototypical second messenger cAMP regulates a wide variety of physiological processes. It can simultaneously mediate diverse functions by acting locally in independently regulated microdomains. In mammalian cells, two types of adenylyl cyclase generate cAMP: G-protein-regulated transmembrane adenylyl cyclases and bicarbonate-, calcium- and ATP-regulated soluble adenylyl cyclase (sAC). Because each type of cyclase regulates distinct microdomains, methods to distinguish between them are needed to understand cAMP signaling. We developed a mass-spectrometry-based adenylyl cyclase assay, which we used to identify a new sAC-specific inhibitor, LRE1. LRE1 bound to the bicarbonate activator binding site and inhibited sAC via a unique allosteric mechanism. LRE1 prevented sAC-dependent processes in cellular and physiological systems, and it will facilitate exploration of the therapeutic potential of sAC inhibition.
Further data
| Item Type: | Article in a journal |
|---|---|
| Refereed: | No |
| Institutions of the University: | Faculties > Faculty of Biology, Chemistry and Earth Sciences > Department of Chemistry > Chair Biochemistry I - Proteinbiochemie der Signaltransduktion > Chair Biochemistry - Univ.-Prof. Dr. Clemens Steegborn Faculties Faculties > Faculty of Biology, Chemistry and Earth Sciences Faculties > Faculty of Biology, Chemistry and Earth Sciences > Department of Chemistry Faculties > Faculty of Biology, Chemistry and Earth Sciences > Department of Chemistry > Chair Biochemistry I - Proteinbiochemie der Signaltransduktion |
| Result of work at the UBT: | No |
| DDC Subjects: | 500 Science 500 Science > 540 Chemistry 500 Science > 570 Life sciences, biology |
| Date Deposited: | 06 Apr 2017 08:57 |
| Last Modified: | 09 Jan 2025 08:49 |
| URI: | https://eref.uni-bayreuth.de/id/eprint/36767 |