Two calmodulin binding elements contribute distinctly to TRPA1 calcium desensitization
Gregory Quevedo1, Kehinde M Taiwo1, Justin H Sanders1
1Department of Molecular Biophysics and Biochemistry, Yale University, New Haven, Connecticut, USA.
Abstract:
The "wasabi receptor," transient receptor potential ankyrin 1 (TRPA1), is a critical pain receptor that is activated by reactive environmental and endogenous irritants to initiate pain perception, local inflammation, and protective behaviors. TRPA1 is a calcium-permeable ion channel; calcium influx tightly controls channel function by first potentiating currents and then triggering rapid desensitization. Here, we provide evidence that the universal calcium sensor calmodulin (CaM) controls TRPA1 desensitization by engaging two distinct CaM-binding sites in the cytoplasmic C terminus: the distal C-terminal CaM binding element (DCTCaMBE) and the TRP CaMBD. Specifically, we found that CaM binds TRPA1 at the DCTCaMBE beginning at low calcium and the TRP CaMBD at high calcium concentrations. Pull-down experiments revealed that the DCTCaMBE and TRP CaMBD exhibit distinct CaM lobe binding specificities. Competition experiments showed that CaM can bind both sites simultaneously as isolated peptides. Molecular modeling identified residues predicted to contribute to the CaM-TRP CaMBD interaction. Mutation of these residues revealed that CaM binding to the TRP CaMBD controls a second kinetic step in TRPA1 desensitization. Finally, complete ablation of CaM binding at both the TRPA1 DCTCaMBE and TRP CaMBD showed that they contribute to a concerted desensitization mechanism. Together, these results support a model where CaM associates with TRPA1 at rest through the DCTCaMBE, which primes the channel for rapid desensitization. As intracellular calcium levels rise, CaM then binds the TRP CaMBD-through bridged or separate interactions-to promote a terminal desensitization step. Our work provides further mechanistic insight into how calcium and CaM tightly control TRPA1 channel function to promote nociceptive signaling.
Insights
Calmodulin (CaM) controls the desensitization of the TRPA1 pain receptor by binding to two distinct sites. This interaction, influenced by calcium levels, regulates pain perception and inflammation.
Area of Science:
- Molecular biology
- Neuroscience
- Ion channel physiology
Background:
- Transient receptor potential ankyrin 1 (TRPA1) is a key pain receptor activated by irritants.
- TRPA1 function is modulated by intracellular calcium, which causes potentiation and desensitization.
- Calmodulin (CaM) is a universal calcium sensor involved in cellular signaling.
Purpose of the Study:
- To elucidate the mechanism by which CaM controls TRPA1 desensitization.
- To identify the specific CaM-binding sites on TRPA1 and their roles in calcium-dependent regulation.
- To understand how CaM binding influences TRPA1 channel gating and nociceptive signaling.
Main Methods:
- Biochemical pull-down assays to assess CaM binding to TRPA1 domains.
- Competition experiments using isolated peptides to study CaM binding specificities.
- Molecular modeling to predict CaM-TRP CaMBD interaction sites.
- Site-directed mutagenesis to investigate the functional role of CaM binding sites.
Main Results:
- CaM binds TRPA1 at two distinct sites: DCTCaMBE (low calcium) and TRP CaMBD (high calcium).
- CaM binding to the TRP CaMBD is crucial for a late step in TRPA1 desensitization.
- Simultaneous CaM binding to both sites contributes to a coordinated desensitization mechanism.
- CaM binding at rest primes TRPA1 for rapid desensitization, with high calcium promoting terminal desensitization.
Conclusions:
- CaM acts as a critical regulator of TRPA1 desensitization through dual binding sites.
- The calcium-dependent interaction of CaM with TRPA1 fine-tunes nociceptive signaling.
- This study provides mechanistic insights into calcium and CaM control of TRPA1 channel activity.
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