Allosteric functional switch of neurokinin A-mediated signaling at the neurokinin NK2 receptor: structural exploration

…, E Maillet, JJ Bourguignon, B Bucher…

Index: Valant, Celine; Maillet, Emeline; Bourguignon, Jean-Jacques; Bucher, Bernard; Utard, Valerie; Galzi, Jean-Luc; Hibert, Marcel Journal of Medicinal Chemistry, 2009 , vol. 52, # 19 p. 5999 - 6011

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Citation Number: 13

Abstract

The neurokinin NK2 receptor is known to pre-exist in equilibrium between at least three states: resting-inactive, calcium-triggering, and cAMP-producing. Its endogeneous ligand, NKA, mainly induces the calcium response. Using a FRET-based assay, we have previously discovered an allosteric modulator of the NK2 receptor that has the unique ability to discriminate among the two signaling pathways: calcium-signaling is not affected while ...