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Shubbar, A.

Publications and source records attributed to Shubbar, A..

2 recordsLinked to original sources

Protonation- and substrate-regulated dimer opening couples brain-type creatine kinase to vesicular and actin-remodeling membranes

Brain-type creatine kinase (CK-BB) buffers local ATP demand through reversible phosphotransfer between ATP and phosphocreatine, yet how this soluble metabolic enzyme engages membrane compartments is unknown. Here, we combine fluorescence microscopy, DEER spectroscopy, hydrogen-deuterium exchange and native mass spectrometry, DEER- and AlphaFold-guided modeling, and long-timescale molecular dynamics to define the pH- and substrate-regulated conformational landscape governing CK-BB membrane association. Acidification promotes curvature-sensitive membrane binding and redistributes endogenous and recombinant CK-BB from diffuse cytosolic pools to punctate vesicular structures and membrane ruffles. Substrates independently promote curvature-sensitive association at neutral pH. DEER and modeling reveal an asymmetric dimer in which the convex surface remains restrained, whereas the concave catalytic-regulatory surface samples pH- and substrate-dependent intermediates. We identify progressive dimer opening as a novel regulatory mechanism whereby acidification and substrate binding increase dynamics across the convex surface and N-terminal dimer interface, generating membrane-competent conformations that facilitate curvature sensing and membrane association. Substrate binding buffers acid-induced deprotection while preserving dynamics near the His191/Ser199 regulatory interface. These findings establish CK-BB as a previously unrecognized curvature-sensitive metabolic enzyme and define dimer dynamics as a molecular switch coupling protonation and substrate occupancy to curved-membrane recognition and localized ATP regeneration, with potential relevance to neurodegeneration and cellular stress.

biophysics↗

Structural dynamics of sphingosine kinase 1 regulation and inhibition

Sphingosine kinase 1 (SK1) generates sphingosine-1-phosphate, a bioactive lipid implicated in cancer and other diseases. Despite its clinical importance, the structural and dynamic basis of SK1 regulation and inhibition remains poorly understood. Using integrated spectroscopic and computational approaches, we uncover conformational transitions that govern substrate entry, catalysis, and inhibitor binding. Phosphorylation of Ser225 reconfigures the regulatory loop and reshuffles salt bridges, priming SK1 for membrane engagement and catalytic activity. We identify a previously uncharacterized catalytic intermediate with a distinct conformation and a highly dynamic lipid-binding loop 1 (LBL-1), sensitive to potent inhibitors such as PF-543. These inhibitors not only stabilize non-catalytic states but also induce LBL-mediated dimerization, blocking membrane binding and substrate access. Our findings reveal a multilayered regulatory mechanism driven by structural flexibility and establish a novel inhibitory paradigm. This framework provides critical insight into SK1 regulation and a foundation for developing next-generation SK1-targeted therapeutics.

biophysics↗