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Bechard, A.

Publications and source records attributed to Bechard, A..

2 recordsLinked to original sources

Protein co-scientist aided simulations of the structural and functional impact of O-GlcNAc Transferase TPR domain deletions and amino acid substitutions associated with X-Linked Intellectual Disability

O-GlcNAc transferase (OGT) is an essential glycosyltransferase that regulates cellular processes through the addition of O-linked {beta}-N-acetyglucosamine (O-GlcNAc) to target proteins. Substrate recognition and protein-protein interactions are mediated by the tetratricopeptide repeat (TPR) domain, yet the contributions of individual TPR repeats to structural stability and function remain poorly understood. Here, we employed an integrated computational framework combining an AI protein co-scientist, Speak to a Protein, which incorporates Boltz-2 for structure prediction and rDock for ligand binding evaluation, with external tools including AlphaFold3 for more advanced structure prediction and the HDOCK server for protein-protein docking. This framework was used to investigate how deletions of TPR domains and disease-associated amino acid substitutions within the TPR domain affect OGT structure and function. Five synthetic truncation OGT isoforms, thirteen single-TPR deletion variants, and five X-linked intellectual disability (XLID)-associated amino acid substitutions were modeled and aligned to wild-type OGT for comparison. Structural perturbations were quantified using backbone root mean square deviation (RMSD), while functional effects were assessed through docking analyses with UDP-GlcNAc, Host Cell Factor 1 (HCF1), and Tet methylcytosine dioxygenase 1 (TET1). Variation in TPR length altered global protein structure and induced long-range conformational changes within the catalytic domain despite no sequence modifications in that region. Single TPR deletions showed that individual repeats contribute unequally to structural stability, with deletions in mid-to-late TPR domains producing the largest structural disruptions. Disease-associated amino acid substitutions also generated conformational changes and reduced predicted ligand binding, consistent with known reductions in enzymatic activity in XLID. Protein-protein docking analyses demonstrated substrate-specific effects, as domain deletion and amino acid substitution variants of OGT had different interactions with TET1 and HCF1. Collectively, these findings identify the TPR domain as a regulatory domain that governs structure, ligand recognition, and protein interactions. More broadly, this work demonstrates how the integration of a protein co-scientist with protein structure modeling tools can be used to predict the structural and functional consequences of domain deletions or natural amino acid variants.

bioinformatics↗

The divergent effects of CDPPB and cannabidiol on fear extinction and anxiety in a predator scent stress model of PTSD in rats.

Post-traumatic stress disorder (PTSD) is a disorder with no clear FDA-approved treatments that reduce symptoms in the majority of patients. PTSD individuals possess an impaired capacity for extinguishing fear memory associations. As such, considerable focus has been given to the development of extinction-enhancing pharmacological agents to be used in combination with PTSD treatments. Here we use a predator-threat animal model of PTSD to test the ability of two compounds to enhance contextual fear extinction and reduce anxiety. Mirroring the heterogeneity observed in human response to trauma, an exposure to predator threat, including the fox odor TMT, have been shown to induce long-term changes in anxiety behavior in only subsets of susceptible rats. Here, two weeks following a ten-minute exposure to a predator odor, rats were classified into stress-Susceptible (Sus) and stress-Resilient (Res) phenotypes using cut-off behavioral criteria for elevated plus maze and acoustic startle response performance. One week following classification, Sus rats underwent three days of context fear extinction. We found that Sus rats increased freezing from day one to day two. Treatment with the mGlu5 positive allosteric modulator CDPPB, but not the phytocannabinoid cannabidiol (CBD), prior to sessions resulted in reduced freezing. CDPPB administration resulted in an increase of Fos immunoreactive cells in the medial prefrontal cortex, indicative of increased neuronal activity. Finally, we used the light-dark box test to measure phenotypic differences and the effects of CDPPB and CBD on unconditioned anxiety two weeks after classification. We found that Res rats showed less anxiety compared to Sus rats, and that CBD, but not CDPPB, administered prior to testing was anxiolytic in Sus rats. Taken together, the present data indicate that mGlu5 PAMs such as CDPPB hold promise for treating human PTSD patients as they enhance extinction of fear without increasing general anxiety. Polytherapy with medications such as CBD may be necessary in order to attenuate general anxiety and future directions will explore this hypothesis.

neuroscience↗