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Romanin, C.

Publications and source records attributed to Romanin, C..

2 recordsLinked to original sources

STIM1 transmembrane helix dimerization captured by AI-guided transition path sampling

STIM1 is a Ca2+-sensing protein in the endoplasmic reticulum (ER) membrane. The depletion of ER Ca2+ stores induces a large conformational transition of the cytosolic STIM1 C-terminus, initiated by the dimerization of the transmembrane (TM) domain. We use the AI-guided transition path sampling algorithm aimmd to extensively sample the dimerization of STIM1-TM helices in an ER-mimicking lipid bilayer. In nearly 0.5 milliseconds of all-atom molecular dynamics simulations without bias potentials, we harvest over 170 transition paths, each about 1.2 {micro}s long on average. We find that STIM1 dimerizes into three distinct and coexisting configurations, which reconciles conflicting results from earlier crosslinking studies. The dominant X-shaped bound state centers around contacts supported by the SxxxG TM interfacial motif. Mutating residues in this contact interface allows us to tune the STIM1-dimerization propensity in fluorescence experiments. From the trained model of the committor probability of dimerization, we identify the transition state ensemble for TM-helix dimerization. At the transition state, interhelical contacts in the luminal halves of the two monomers dominate, which likely enables the luminal Ca2+-sensing domain in STIM1 to condition the dimerization of the TM helices. Our work demonstrates the unique power of AI-guided simulations to sample rare and slow molecular transitions, and to produce detailed atomistic insight into the mechanism of STIM1 TM-helix dimerization as a key step in ER Ca2+-sensing. SignificanceSTIM1 is a protein sensor that signals drops in the Ca2+ concentration inside the endoplasmic reticulum (ER) to the cytosol. As Ca2+ levels decrease, the STIM1 transmembrane (TM) helices dimerize. We sample this TM helix dimerization in AI-guided atomistic molecular simulations, revealing two distinct pathways of dimerization. We reconcile conflicting results of earlier crosslinking studies by showing that both reported dimer configurations coexist as the end points of distinct association pathways. The dominance of interhelical contacts on the luminal side at the transition state enables the luminal Ca2+-sensing domain to condition helix dimerization. AI-guided path sampling made it possible to sample rare helix dimerization events far outside the current reach of regular molecular simulations.

biophysics↗

A series of Orai1 gating checkpoints in transmembrane and cytosolic regions requires clearance for CRAC channel opening/ Clearance and synergy of Orai1 gating checkpoints controls pore opening

The initial activation step in gating of ubiquitously expressed Orai1 Calcium (Ca2+) ion channels represents the store-dependent coupling to the Ca2+ sensor protein STIM1. An array of constitutively active Orai1 mutants gave rise to the hypothesis that STIM1 mediated Orai1 pore opening is accompanied by a global conformational change of all Orai TM helices within the channel complex. Here, we prove that a local conformational change spreads omnidirectionally within the Orai1 complex. Our results demonstrate that a global, opening-permissive allosteric communication of TM helices is indispensable for pore opening and requires clearance of a series of Orai1 gating checkpoints. We discovered these gating checkpoints in middle and cytosolic extended TM domain regions. Our findings are based on a library of double point mutants that contain each one loss-of-function (LoF) with one gain-of-function (GoF) point mutation in a series of possible combinations. We demonstrated that an array of LoF mutations act dominant over most GoF mutations within the same as well as of an adjacent Orai subunit. We further established inter- and intramolecular salt-bridge interactions of Orai subunits as a core element of an opening-permissive Orai channel architecture. Collectively, clearance and synergistic action of all these gating checkpoints is required to allow STIM1 coupling and Orai1 pore opening. Graphical Abstract O_FIG O_LINKSMALLFIG WIDTH=200 HEIGHT=166 SRC="FIGDIR/small/207183v2_ufig1.gif" ALT="Figure 1"> View larger version (76K): org.highwire.dtl.DTLVardef@3f80f1org.highwire.dtl.DTLVardef@12a6a0aorg.highwire.dtl.DTLVardef@197b825org.highwire.dtl.DTLVardef@1bab109_HPS_FORMAT_FIGEXP M_FIG C_FIG

biophysics↗