The TLQP-21 neuropeptide has been implicated in functions as diverse as lipolysis, neurodegeneration and metabolism, thus suggesting an important role in several human diseases. Three binding targets have been proposed for TLQP-21: C3aR1, gC1qR and HSPA8. The aim of this review is to critically evaluate the molecular identity of the TLQP-21 receptor and the proposed multi-receptor mechanism of action. Several studies confirm a critical role for C3aR1 in TLQP-21 biological activity and a largely conserved mode of binding, receptor activation and signaling with C3a, its first-identified endogenous ligand. Conversely, data supporting a role of gC1qR and HSPA8 in TLQP-21 activity remain limited, with no signal transduction pathways being described. Overall, C3aR1 is the only receptor for which a necessary and sufficient role in TLQP-21 activity has been confirmed thus far. This conclusion calls into question the validity of a multi-receptor mechanism of action for TLQP-21 and should inform future studies.

The molecular identity of the TLQP-21 peptide receptor / Sahu, B. S.; Nguyen, M. E.; Rodriguez, P.; Pallais, J. P.; Ghosh, V.; Razzoli, M.; Sham, Y. Y.; Salton, S. R.; Bartolomucci, A.. - In: CELLULAR AND MOLECULAR LIFE SCIENCES. - ISSN 1420-682X. - 78:23(2021), pp. 7133-7144. [10.1007/s00018-021-03944-1]

The molecular identity of the TLQP-21 peptide receptor

Bartolomucci A.
2021-01-01

Abstract

The TLQP-21 neuropeptide has been implicated in functions as diverse as lipolysis, neurodegeneration and metabolism, thus suggesting an important role in several human diseases. Three binding targets have been proposed for TLQP-21: C3aR1, gC1qR and HSPA8. The aim of this review is to critically evaluate the molecular identity of the TLQP-21 receptor and the proposed multi-receptor mechanism of action. Several studies confirm a critical role for C3aR1 in TLQP-21 biological activity and a largely conserved mode of binding, receptor activation and signaling with C3a, its first-identified endogenous ligand. Conversely, data supporting a role of gC1qR and HSPA8 in TLQP-21 activity remain limited, with no signal transduction pathways being described. Overall, C3aR1 is the only receptor for which a necessary and sufficient role in TLQP-21 activity has been confirmed thus far. This conclusion calls into question the validity of a multi-receptor mechanism of action for TLQP-21 and should inform future studies.
2021
The molecular identity of the TLQP-21 peptide receptor / Sahu, B. S.; Nguyen, M. E.; Rodriguez, P.; Pallais, J. P.; Ghosh, V.; Razzoli, M.; Sham, Y. Y.; Salton, S. R.; Bartolomucci, A.. - In: CELLULAR AND MOLECULAR LIFE SCIENCES. - ISSN 1420-682X. - 78:23(2021), pp. 7133-7144. [10.1007/s00018-021-03944-1]
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11381/2918004
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