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Jagessar, K. L.

Publications and source records attributed to Jagessar, K. L..

2 recordsLinked to original sources

Proton-coupled alternating access in a versatile Spns drug efflux pump from Mycobacterium smegmatis

Spns transporters are a mechanistically distinct branch of the major facilitator superfamily that regulate lipid transport, lysosomal homeostasis, immunity and disease. How the conserved Spns fold integrates protonation, substrate binding and alternating access to support chemically and directionally diverse transport remains unresolved. Here we combine DEER spectroscopy in lipid nanodiscs with DEER-and AlphaFold-guided modeling and protonation-mimetic mutagenesis to define the conformational landscape of the Mycobacterium smegmatis homolog MsSpns. Protonation shifts MsSpns toward an inward-facing state, whereas deprotonation favors a broader outward-facing ensemble through remodeling of intracellular and extracellular gates. Protonation-mimetic substitutions identify Glu126 as a switch that stabilizes an inward-facing, substrate-entry-competent conformation, while Asp38 and Asp57 favor outward-facing states and tune the extracellular proton-sensing network. The substrate-binding cavity displays distinct proton sensitivity and weaker cooperativity than gating networks. Hydrophilic cationic substrates stabilize the outward-facing state, consistent with efflux antiport, whereas lipophilic compounds favor the inward-facing state, suggesting uptake or allosteric stabilization. Thus, conserved proton-coupling elements can power opposing transport modes, revealing the mechanistic versatility of the Spns fold and its therapeutic potential.

biophysics↗

Sequence and Structural Determinants of Ligand-dependent Alternating Access of a MATE Transporter

MATE transporters are ubiquitous ion-coupled antiporters that extrude structurally- and chemically-dissimilar molecules and have been implicated in conferring multidrug resistance. Here, we integrate Double Electron Electron Resonance (DEER) in conjunction with functional assays and site-directed mutagenesis of conserved residues to illuminate principles of ligand-dependent alternating access of PfMATE, a proton-coupled MATE from the hyperthermophilic archaeon Pyrococcus furiosus. Pairs of spin labels monitoring the two sides of the transporter reconstituted into nanodiscs reveal large amplitude movement of helices that alter the orientation of a putative substrate binding cavity. We found that acidic pH favors formation of an inward-facing (IF) conformation, whereas elevated pH (>7) and the substrate rhodamine 6G stabilizes an outward-facing (OF) conformation. PfMATE isomerization between outward-facing and inward-facing conformations is driven by protonation of a previously unidentified intracellular glutamate residue that is critical for drug resistance. Our results can be framed in a mechanistic model of transport that addresses central aspects of ligand coupling and alternating access.

biophysics↗