ArticleProceedings of the National Academy of Sciences of the United States of America2026
Conformational equilibria in the activation of cystine-knot hormone receptors.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Abstract
Human glycoprotein hormones such as thyroid-stimulating hormone (TSH) and follicle-stimulating hormone (FSH) belong to a broader family of cystine-knot hormones (CKHs), all of which act through leucine-rich-repeat (LRR)-containing G protein-coupled receptors (LGRs) with which they have coevolved from evolutionary predecessors in metazoan animals. There is substantial evidence for LGR dimers being required in the transmission of G-protein signals elicited by mammalian CKHs acting on their cognate LGRs. Yet, human LGRs are monomeric as extracted from cell membranes and also in cryo-EM structures, both when in apo, inactive state and when hormone bound in an LRR-elevated active state. Fortunately, the LGR from the nematode
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