Daniel R Larson, Christoph Fritzsch ... Robert H Singer
Steroid hormone receptors control the expression of their target genes through a digital on-off switch in individual cells, which leads to an analogue dose-response relationship at the level of the whole organism.
The gustatory receptor PxylGr34 is tuned to the steroid plant hormone brassinolide and mediates the deterrent effects of brassinolide on feeding and ovipositing behaviors in Plutella xylostella.
Dave W Anderson, Alesia N McKeown, Joseph W Thornton
Experimental mapping of the joint sequence space of an ancient transcription factor (TF) and its DNA binding sites reveals that epistasis across the molecular interface permitted the evolution of a new and specific TF-DNA complex.
Steven De Gieter, Casey I Gallagher ... Rouslan G Efremov
Cryo-EM structures of Cys-loop receptor Alpo4 from the thermophilic worm Alvinella pompejana show that a sterol derivative CHAPS binds in and outside of its orthosteric binding site and induces a quaternary twist.
Ecdysone-mediated repression of the TMEM16 channel subdued initiates a sensory switch in peripheral nociceptors during Drosophila larval development, increasing thermal nociceptive behavior and reducing responsiveness to ultraviolet light.
Brian PH Metzger, Yeonwoo Park ... Joseph W Thornton
A complete mutational scan of a protein-DNA interface shows that pairwise epistatic interactions among amino acids determine a transcription factor's specificity for DNA and facilitate the evolution of new functions.
Sabab Hasan Khan, Sean M Braet ... C Denise Okafor
Transcriptional activity is characterized for five steroid receptors complexed with multiple ligands and it is shown that the extent of transcriptional activation in complexes is accurately described by conformational shifts in computationally-generated ensembles.
Yusuke Sugasawa, Wayland WL Cheng ... Alex S Evers
Differential, state-dependent occupancy of three discrete binding sites on α1β3 GABAA receptors determines whether a specific neurosteroid analogue potentiates or inhibits GABA-elicited currents or competitively antagonizes neurosteroid action.