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Smith, D. M.

Publications and source records attributed to Smith, D. M..

At least 19 recordsLinked to original sources

Progranulin deficiency promotes neuroinflammation through cathepsin B-mediated activation of the NLRP3 inflammasome

Haploinsufficiency of progranulin (resulting from mutations in the GRN gene) is a major genetic cause of frontotemporal dementia (FTD), which is characterized by profound changes in personality and behavior, progressive impairments in executive function, speech, language and/or movement, TDP-43 pathology, lysosomal dysfunction, and neuroinflammation. Studies in progranulin-deficient mouse models have demonstrated the critical role of neuroinflammation in disease pathogenesis, as deletion of NF-kB or complement factors prevents FTD-associated behavioral deficits. While progranulin is known to be anti-inflammatory, the precise molecular mechanism by which its deficiency triggers inflammatory cascades remain unclear. Here, we investigate the involvement of the NLRP3 inflammasome in progranulin-deficient models, including mice, human microglial cells, and patient fibroblasts. In Grn mice, we found increased levels of several inflammasome-related proteins, including procaspase-1 and cleaved IL-1{beta}. Similarly, GRN knockout (KO) microglia cells showed significant increases in levels of procaspase-1, NLRP3, and cleaved IL-1{beta}. Moreover, KO cells had increased NLRP3 oligomerization, suggesting that progranulin negatively regulates inflammasome assembly. We also investigated the potential link between lysosomal dysfunction and NLRP3 inflammasome activation in progranulin deficiency. We found that pharmacological inhibition of cathepsin B reduced NLRP3 inflammasome oligomerization as well as inflammatory cytokine expression in GRN KO cells. Additionally, siRNA knockdown of cathepsin B reduced levels of procaspase-1 and cleaved IL-1{beta} in GRN KO cells. Finally, we found that heterozygous GRN fibroblasts exhibited similar increases in procaspase-1 and cleaved IL-1{beta} levels, and these increases were corrected by treatment with an antisense oligonucleotide (ASO) that increase progranulin protein levels. Overall, our results demonstrate that progranulin deficiency promotes NLRP3 inflammasome assembly and activity through cathepsin B-mediated signaling, thereby establishing a mechanistic link between lysosomal dysfunction and increased inflammation. The ability of the GRN-targeting ASO to correct NLRP3-mediated inflammation highlights a promising therapeutic strategy for FTD-GRN and inflammation in other neurodegenerative disorders linked to progranulin deficiency.

neuroscience↗

Nonlinear associations between body mass index and brain microstructure across adolescence in the ABCD Study

Importance: Adolescent body mass index (BMI) is linked to brain microstructural alterations, but it is not known if this association is uniform across the BMI range. Objective: To characterize the shape of the association between adolescent BMI and brain microstructure across the BMI range. Design: Baseline, and 2-, 4-, and 6-year follow-up brain imaging and BMI from the Adolescent Brain Cognitive DevelopmentSM Study, analyzed between June 2025 and June 2026. Setting: Multicenter, population-based study including 21 sites distributed across the US. Participants: 10,479 adolescents (5,078 [48.5%] female; aged 9-18 years) from this population-based cohort study were included after quality control of complete data. Exposures: Centers for Disease Control BMI extended percentiles and percent from median BMI. Main Outcome and Measure: The primary outcome was the restricted normalized isotropic (RNI) signal fraction derived from diffusion imaging which indexes water confined within spherical cellular structures and is sensitive to microstructural properties including cellularity. Results: A total of 10,479 participants (5,078 [48.5%] female; aged 9-18 years) contributed 22,049 imaging observations across four timepoints. Higher BMI percentile was associated with greater RNI in bilateral reward- and appetite-related subcortical gray matter and white matter tracts, with effects varying spatially within structures, and with generally greater magnitude in males. Across these structures, the association increased steeply above the 80th percentile. This acceleration reflected compression of the percentile scale at high BMI; when BMI was reparameterized as percent from median, the association with RNI was approximately linear. Conclusions and Relevance: Our results suggest that BMI is associated with brain microstructure in a graded manner within white matter tracts and subcortical gray matter related to reward, executive function, and appetitive control. This indicates that the effect of BMI on microstructure is not confined to weight extremes and should be accounted for when modeling brain-body-behavior relationships during adolescence.

neuroscience↗

Limitations of inferring antiviral efficacy of interfering particles from observational natural histories

Recently Hariharan et al.2 reported naturally arising defective HIV genomes capable of conditional replication and interference in humans. While this work makes an important contribution to the field of therapeutic interfering particles (TIPs), particularly with respect to safety and tolerability, it also raises fundamental issues regarding: (i) whether the presented data constitute a valid test of, or support conclusions about, the therapeutic potential of TIPs and (ii) technical issues pertaining to the reported basic reproductive numbers (R0). Hariharan et al. conclude that the findings "raise concerns about the effectiveness of TIPs." However, the data presented do not constitute a valid test of therapeutic efficacy. Here, we (i) clarify that post-hoc observational natural history cannot adjudicate the success or failure of an intervention, (ii) show new analysis highlighting how the reported R0 measurements are internally inconsistent with the within-host viral dynamics reported, and (iii) explain that alternative, well-established mechanisms remain sufficient to explain the reported observations.

microbiology↗

Cell-type specific impact of opioid use disorder and HIV on the human forebrain and cerebellum

Opioid use disorder (OUD), which frequently co-occurs with HIV infection, causes long-term neurological disease, yet the epigenetic and transcriptomic effects of OUD and HIV on specific cell types and regions of the brain are poorly understood. To assess the cell-type specific impacts of OUD and HIV across the human brain, we measured single cell transcriptomes and epigenomes of 580,353 cells in the prefrontal cortex, amygdala and cerebellum of 44 donors. We cataloged over 750k candidate cis-regulatory elements (cCREs) and identified gene regulatory networks (GRNs) of transcription factor activity across 35 neuronal and non-neuronal cell types. We identified specific neuronal and glial populations whose cCREs were significantly enriched for genetic risk of addiction-related traits. In OUD donors, we found evidence for reduced metabolic function in neurons in the PFC and cerebellum as well as increased gene expression related to voltage-gated calcium channel activity in the cerebellum. Using a cerebellar organoid model, fentanyl treatment reduced metabolic activity while increasing neuronal activity. Across brain regions, HIV activated immune-related pathways in glial populations, while comorbid OUD and HIV exacerbated metabolic changes in cortical glial cells. Cerebellum-specific Bergmann glia, in addition to forebrain microglia and astrocytes, showed expansion of reactive state identity in HIV. These results highlight shared and specific changes to immune, synaptic, and metabolic processes in OUD and HIV across brain regions and reveal that cerebellar cell types are distinctly affected by opioid abuse.

genomics↗

A new mRNA antigen vaccine induces potent B and T cell responses and in vivo protection against SARS-CoV-2

The SARS-CoV-2 mRNA vaccine provides effective protection against viral infection and severe disease by inducing efficient adaptive immunity. However, vaccine efficacy is decreased against emerging variants, and immune memory is relatively short-lived. Here, we added new T cell epitopes to the RBD (receptor-binding domain) mRNA vaccine and identified a SARS-CoV-2 membrane epitope that significantly improved vaccine-induced immunity and protection in vivo. That new vaccine, designated G1-C, induced 8.2-fold higher levels of RBD-specific antibodies than did RBD and enhanced spike-specific T cell and B cell responses. Remarkably, the G1-C modulated hematopoietic stem cell (HSC) differentiation and increased levels of B and NK cells by regulating multiple signaling pathways in bone marrow potentially via Fos, Klf4, and Klf6 transcription factors. Altogether, these findings identify a new vaccine candidate to control viral infection by affecting the lymphoid-myeloid lineage bias and suggest the potential role of T cell epitopes in vaccine design and development.

immunology↗

Age associations with cortical and subcortical brain structure in adolescents age 9-17

IntroductionAdolescence is a pivotal period in brain structural development and maturation. However, investigation of cortical and subcortical brain changes during this time have been limited by small sample size and have generally examined the brain at the level of predetermined regions of interest. The recently developed Fast Efficient Mixed-Effects Algorithm (FEMA) allows for increased computational speed using mixed-effects models applied at the voxel or vertex level, as well as across multiple regions of interest. MethodsWe extended the existing FEMA framework to represent predictors using natural spline basis functions, enabling us to model nonlinear trajectories of brain structure as a function of age. We then applied this model to the The Adolescent Brain Cognitive DevelopmentSM Study (22,651 observations from 10,521 unique subjects aged 9.00-17.77) to study the age-related trajectories of tabulated cortical and subcortical volumes, vertexwise cortical thickness and surface area, and voxelwise volume assessed using the Jacobian. Models are reported separately in males and females. ResultsGlobal volume variables, including total subcortical gray matter volume, peaked near 13 years in females and 15 years in males. Vertexwise cortical surface area followed an inverted U-shaped curve, whereas vertexwise cortical thickness followed a monotonic decrease during the age range studied. Voxelwise imaging analysis revealed regional differences in age trajectories at the subregional level. DiscussionThe results of this work replicate and extend prior findings related to adolescent brain development, and illustrate distinct spatiotemporal patterns of structural changes in subcortical regions. The updated FEMA framework is publicly available for use in similar large datasets.

neuroscience↗

Precision fMRI reveals densely interdigitated network patches with conserved motifs in the lateral prefrontal cortex

Dominant models of human lateral prefrontal cortex (LPFC) organization emphasize broad domain-general zones and smooth functional gradients. However, these models rely heavily on group-averaged neuroimaging, which can obscure fine-scale cortical features - especially in highly inter-individually variable regions like the LPFC. To address this limitation, we collected a new precision fMRI dataset from 10 individuals, each with approximately 2 hours of resting-state and 6 hours of task data. We mapped individual-specific LPFC networks using resting-state fMRI and tested network-level functional preferences using task fMRI. We found that individual LPFC organization differed markedly from group-averaged estimates. Individual maps showed more fragmented and interdigitated networks - especially in anterior LPFC - including novel conserved motifs present across individuals. Task fMRI revealed that distinct but adjacent networks support domain-specific processes (i.e., language, social cognition, episodic projection) versus domain-general control. Sharp functional boundaries were visible at the individual level that could not be observed in group data. These findings uncover previously hidden organizational principles in the LPFC and offer a framework for understanding how the LPFC supports flexible, complex cognition through a finely organized architecture.

neuroscience↗

FEMA-Long: Modeling unstructured covariances for discovery of time-dependent effects in large-scale longitudinal datasets

While linear mixed-effects (LME) models are common for analyzing longitudinal data, most users rely on random intercepts or simple stationary covariance, due to unavailability of computationally tractable solutions. Here, we extend the Fast and Efficient Mixed-Effects Algorithm (FEMA) and present FEMA-Long, a computationally tractable approach to flexibly modeling longitudinal covariance suitable for high-dimensional data. FEMA-Long can: i) model unstructured covariance, ii) model covariates as smooth functions using splines, iii) discover time-dependent effects of covariates with spline interactions, and iv) use these flexible longitudinal modeling strategies to perform longitudinal genome-wide association studies and discover time-dependent genetic effects, in a computationally scalable manner, suitable for high-dimensional data. Through extensive simulations, we show that estimates from FEMA-Long are accurate, while being up to several thousand times faster and with minimal carbon footprint. To show the utility of FEMA-Long for discovering novel biological signal, using data from the Norwegian Mother, Father and Child Cohort Study (MoBa), we performed a longitudinal genome-wide association study with non-linear SNP-by-time interaction on length, weight, and BMI of 68,273 infants with up to six measurements in the first year of life. We found dynamic patterns of random effects including time-varying heritability and genetic correlations, as well as several genetic variants showing time-dependent effects, highlighting the applicability of FEMA-Long to enable novel discoveries. FEMA-Long is available at: https://github.com/cmig-research-group/cmig_tools. Author summaryMost large-scale datasets have complexities such as repeated measures, related individuals, or other dependencies across samples, preventing the use of standard regression approaches for analysis. In such circumstances, linear mixed-effects modeling is often employed. However, for high-dimensional datasets, fitting these models is quite challenging. Further, most standard uses of linear mixed-effects modeling focus on simpler covariance models, which may not hold. Here, we introduce FEMA-Long, a novel computationally efficient analytical framework for fitting linear mixed-effects models with time-varying random effects, as well as allowing the effect of the covariates to change smoothly over time by using splines. This is particularly relevant when, for example, studying the effect of genetic variants on phenotypes, where the effects could be non-linear over time. The FEMA-Long framework allows time-varying heritability as well as discovery of genetic variants that show time-dependent effects. By performing a genome-wide association study on data from the Norwegian Mother, Father and Child Cohort Study (MoBa) using FEMA-Long, we show the discovery of genetic variants with time-dependent effects on infant length, weight, and BMI during the first year of life. Our results highlight the potential of using FEMA-Long to make novel discoveries that can lead to biological insights on the genetics of complex traits as well as improve the potential of using genetics for personalized prediction.

genetics↗

Immunomodulation by AZD1656 reverses cardiac dysfunction, metabolic remodelling and reduces infarct size in type 2 diabetic cardiomyopathy

Type 2 diabetes (T2D) precipitates diabetic cardiomyopathy (dbCM), a condition characterized by chronic inflammation, metabolic dysregulation and impaired cardiac performance. Here we show that the glucokinase activator AZD1656, originally developed for glycaemic control but later identified to have immunomodulatory effects, reverses cardiac dysfunction and metabolic remodelling in dbCM. In obese, hyperglycaemic db/db mice with diastolic dysfunction, six weeks of AZD1656 treatment improved myocardial performance, reduced infarct size and enhanced post-ischaemic recovery. Integrated metabolic, functional and histological analyses revealed restoration of mitochondrial metabolism and attenuation of fibrosis. Mechanistically, AZD1656 remodelled the cardiac immune landscape by promoting regulatory T-cell infiltration. These findings demonstrate a link between cardiac inflammation and metabolic remodelling in dbCM and highlight that modulation of immune cells and metabolism can protect the diabetic heart. Targeting immunometabolic pathways may therefore offer a therapeutic strategy to alleviate cardiac dysfunction and reduce infarct vulnerability in T2D

physiology↗

GALILEO Generatively Expands Chemical Space and Achieves One-Shot Identification of a Library of Novel, Specific, Next Generation Broad-Spectrum Antiviral Compounds at High Hit Rates

The COVID-19 pandemic (2019-2023) demonstrated the need for safe and effective, stockpiled broad-spectrum antiviral drugs to suppress unexpected viral outbreaks. The inability of the pharmaceutical industry to create such a therapeutic in the 6 years since the onset of COVID-19 demonstrates antiviral drug development must undergo a paradigm shift for this to occur. AI-based target and medicinal chemistry discovery platforms such as GALILEO and its geometric graph convolutional network tool ChemPrint, which we recently published, hold promise in accelerating and reimagining the drug development process. GALILEO identified the Thumb-1 site (an allosteric subdomain of the viral RNA polymerase) to be structurally conserved across numerous viral species and MDL-001 (an orally available therapeutic with a favorable pharmacokinetics and safety profile in humans) to be a potent inhibitor thereof. Published preclinical proof-of-concept studies demonstrated MDL-001 as a first-in-class broad-spectrum antiviral drug. This study leverages GALILEOs generative and multimodal discovery tools to create trillions of new chemical entities (NCEs) from MDL-001s pharmacophoric scaffold and select a library of highly specific and optimized compounds for next-generation broad-spectrum antiviral development. Specifically, ChemPrints one-shot predictions identified 12 NCEs with predicted affinity to Thumb-1 and significantly reduced, or no, affinity to MDL-001s original target. In vitro bioassays demonstrated a 100% hit rate, with all 12 NCEs having antiviral activity against Hepatitis C Virus (HCV) and/or human Coronavirus 229E. In vitro studies also demonstrated reduced activity of 800-fold to greater than 15,000-fold relative to MDL-001s originally designed mechanism of action (MoA). In Tanimoto similarity plots, the 12 NCEs lacked chemical relatedness to known antiviral drugs, including MDL-001 (average Tanimoto coefficient: 0.38) and Beclabuvir, (average Tanimoto coefficient: 0.13) a HCV Thumb-1 ligand that lacks broad-spectrum activity. This study showcases GALILEOs ability to generate vast NCE libraries and ChemPrints extrapolative capabilities to discover large, potent NCE libraries of compounds, specific to a complex target that are novel to known chemistry at high hit-rates.

bioinformatics↗

MDL-001: An Oral, Safe, and Well-Tolerated Broad-Spectrum Inhibitor of Viral Polymerases

Endemic viral respiratory illnesses caused by influenza, RSV, and coronaviruses impose a global disease burden of hundreds of millions of infections and hundreds of thousands of deaths annually. Chronic hepatitis B and C infections persist in 254 million and 58 million people worldwide, respectively. No approved therapy addresses these viruses simultaneously. MDL-001 is an oral, direct-acting, broad-spectrum antiviral targeting the Thumb-1 allosteric site of viral polymerases. Here, we report MDL-001 inhibits influenza A/B, RSV, SARS-CoV-2, endemic human coronaviruses, and hepatitis B/C/D viruses with nanomolar EC90 potency in vitro. MDL-001 demonstrated equivalent in vivo efficacy to oseltamivir against mouse-lethal influenza A virus infection, reducing lung viral load by 2.6 log10 and preventing weight loss and mortality. MDL-001 demonstrated equivalent symptom reduction to subcutaneous remdesivir after SARS-CoV-2 infection. MDL-001 treatment reduced SARS-CoV-2 lung viral titers by 2.9 log10, superior to literature reported 1.4 log10 and 1.0 log10 reductions for nirmatrelvir and molnupiravir, respectively. MDL-001 reduced HCV viremia by 3.3 log10, equivalent to sofosbuvir. Oral MDL-001 reduced plasma HBV surface antigen by 2.5 log10, exceeding tenofovir alafenamide from Day 8 through Day 21. MDL-001 demonstrated an in vitro EC50 of 79.4 nM against infection with RSV strain A2, a 416-fold improvement over literature-reported ribavirin. Oral pharmacokinetics studies demonstrate MDL-001 is rapidly absorbed and partitioned into Lung (Kp=39-52) and Liver (Kp=71-104) tissues. MDL-001 produced no treatment-related adverse events across 376 animals and showed no hERG, Ames genotoxicity, or micronucleus safety issues. These findings support MDL-001 as a broad-spectrum, direct-acting non-nucleoside antiviral clinical candidate.

pharmacology and toxicology↗

The infralimbic, but not the prelimbic cortex is needed for a complex olfactory memory task.

The medial prefrontal cortex (mPFC) plays a key role in memory and behavioral flexibility, and a growing body of evidence suggests that the prelimbic (PL) and infralimbic (IL) subregions contribute differently to these processes. Studies of fear conditioning and goal-directed learning suggest that the PL promotes behavioral responses and memory retrieval, while the IL inhibits them. Other studies have shown that the mPFC is engaged under conditions of high interference. This raises the possibility that the PL and IL play differing roles in resolving interference. To examine this, we first used chemogenetics (DREADDs) to suppress mPFC neuronal activity and tested subjects on a conditional discrimination task known to be sensitive to muscimol inactivation. After confirming the effectiveness of the DREADD procedures, we conducted a second experiment to examine the PL and IL roles in a high interference memory task. We trained rats on two consecutive sets of conflicting odor discrimination problems, A and B, followed by test sessions involving a mid-session switch between the problem sets. Controls repeatedly performed worse on Set A, suggesting that learning Set B inhibited the rats ability to retrieve Set A memories (i.e. retroactive interference). PL inactivation rats performed similarly to controls. However, IL inactivation rats did not show this effect, suggesting that the IL plays a critical role in suppressing the retrieval of previously acquired memories that may interfere with retrieval of more recent memories. These results suggest that the IL plays a critical role in memory control processes needed for resolving interference.

neuroscience↗

GDF3 promotes adipose tissue macrophage-mediated inflammation via altered chromatin accessibility during aging

Age-related susceptibility to sepsis and endotoxemia is poorly defined, although hyperactivation of the immune system and the expansion of the visceral adipose as an immunological reservoir are underlying features. Macrophages from older organisms exhibit substantial changes, including chronic NLRP3 inflammasome activation, genomic remodeling and a dysfunctional, amplified inflammatory response upon new exposure to pathogen. However, the mechanisms by which old macrophages maintain their inflammatory phenotype during endotoxemia remains elusive. We previously identified Gdf3, a TGF{beta} superfamily cytokine, as a top-regulated gene by age and the NLRP3 inflammasome in adipose tissue macrophages (ATMs). Here, we demonstrate that endotoxemia increases inflammatory (CD11c+) ATMs in a Gdf3- dependent manner in old mice. Lifelong systemic or myeloid-specific deletion of Gdf3 leads to reduced endotoxemia- induced inflammation, with decreased CD11c+ ATMs and inflammatory cytokines, and protection from hypothermia. Moreover, acute blockade of Gdf3 using JQ1, a BRD4 inhibitor, phenocopies old mice with lifelong Gdf3-deficiency. We show that GDF3 promotes the inflammatory phenotype in ATMs by phosphorylating SMAD2/3. Mechanistically, the differential chromatin landscape of ATMs from old mice with or without myeloid-driven Gdf3 indicates that GDF3- SMAD2/3 signaling axis shifts the chromatin accessibility of ATMs towards an inflammatory state during aging. Furthermore, pharmaceutical inhibition of SMAD3 with a specific inhibitor of SMAD3 (SIS3) mimics Gdf3 deletion. SIS3 reduces endotoxemia-mediated inflammation with fewer CD11c+ ATMs and less severe hypothermia in old, but not young mice, as well as reduced mortality. In human adipose tissue, age positively correlates with GDF3 level, while inflammation correlates with pSMAD2/3 level. Overall, these results highlight the importance of GDF3-SMAD2/3 axis in driving inflammation in older organisms and identify this signaling axis as a promising therapeutic target for mitigating endotoxemia-related inflammation in the aged.

immunology↗

Divergent Immediate and Delayed Effects of Juvenile Exposure to Doxorubicin on the Thymus in C57BL/6 Mice

BackgroundThe understanding of alterations within the immune system following doxorubicin (DOX) chemotherapy, and subsequent restoration, in childhood cancer survivors remains limited. This investigation endeavors to elucidate the immediate and delayed changes in thymic immune cell populations and their phenotypes in response to clinically relevant low doses of DOX in a juvenile mouse model. MethodsMale mice underwent a regimen of repeated low-dose DOX intraperitoneal injections at 4 mg/kg/week for three consecutive weeks. One week after the last dose of DOX, a subset of mice was euthanized to assess the immediate effects of DOX administration. A second subset of mice was euthanized five weeks after the last DOX dose to evaluate the delayed effects. Thymic samples were collected for multiparameter flow cytometry analysis to evaluate alterations in immune cell composition and phenotype. Additionally, quantitative real-time polymerase chain reaction (qRT-PCR) was employed to measure gene expression of- cytokines and senescence markers. ResultsOne week following DOX administration, DOX treatment resulted in significant decline in thymus weight, with notable alterations in immune cell subpopulations. Reduced frequencies of mature CD3+CD4+ and CD3+CD8+ T cells were observed, along with changes in proliferation and exhaustion markers. Gene expression analysis revealed upregulation of Foxn, Pax1, Ifn{gamma}, and Il7 alongside decreased Il6 and Il17 expression. Furthermore, Cdkn1a (p21Cip1) expression was elevated, suggesting immunosenescence. Five weeks following DOX administration, delayed effects of DOX treatment manifested in rebound increase in thymus weight and altered frequencies of CD4+ and CD8+ T cell subsets, with distinct patterns of proliferation and exhaustion observed. Notably, central memory CD4+ T cells exhibited significant decrease in frequency, while naive and effector memory CD4+ T cells showed reduced proliferation (Ki67+) and PD1 expression. Similar trends were observed in CD8+ T cell subsets, indicating selective effects of DOX on T cell differentiation and function. Although expression of thymus-related genes was normalized, p21Cip1 gene expression remained elevated. ConclusionDOX treatment elicits a multifaceted influence on immune cell subsets and thymic weight. Immediate effects included thymic atrophy and reductions in mature T cell populations, while delayed effects showed rebound thymic hyperplasia and selective changes in CD4+ and CD8+ T cell subsets. Notably, both central memory and effector memory T cells exhibited reduced proliferation and exhaustion, suggesting unique impacts of DOX on immune cell function. The enduring elevation in p21Cip1 gene expression 5 weeks after DOX treatment suggests an immunosenescent phenotype. These observations collectively illuminate the formidable task of preserving immune competence and overall well-being in childhood cancer survivors subjected to DOX therapy.

pharmacology and toxicology↗

Retrosplenial cortex encodes both local and global space in connected environments

In everyday life, mammals navigate through environments composed of multiple interconnected spaces. Understanding how the brain encodes space in such complex settings is essential to uncover the mechanisms that support flexible navigation in the real world. In this study, we investigated how the retrosplenial cortex (RSC) and the hippocampus (HPC) encode spatial information in multi-room environments by recording neuronal activity in rats exploring environments composed of two or four connected rooms. These environments varied both in their structural layout and in their sensory features, allowing us to disentangle the influence of environmental geometry from that of local sensory cues. We found that two types of directional coding coexist within the RSC: classical head direction cells maintained a stable preferred firing direction across all rooms, while multidirectional cells expressed room-specific directional tuning that followed the geometric structure of the environment (e.g., 180{degrees} or 90{degrees} rotations). In addition, non-directional RSC neurons displayed room-specific spatial firing patterns that repeated across rooms following geometric transformations, similar to the activity observed in multidirectional cells. In contrast, hippocampal place cells either remapped between rooms or showed simple translational repetition, without preserving any geometric alignment. Taken together, these findings reveal a functional dissociation between retrosplenial and hippocampal spatial codes. The RSC supports a structured, multi-scale representation of space, segmenting the environment into locally anchored reference frames embedded within a coherent global geometry. The HPC, by contrast, encodes room-specific representations independently for each compartment. This division may support flexible navigation in complex environments by integrating geometry-based spatial segmentation and unification in the RSC with context-specific encoding in the HPC, thereby enabling multi-level spatial coding across interconnected spaces.

neuroscience↗

Compromised chronic efficacy of a Glucokinase Activator AZD1656 in mouse models for common human GCKR variants

Glucokinase activators (GKAs) have been developed as blood glucose lowering drugs for type 2 diabetes. Despite good short-term efficacy, several GKAs showed a decline in efficacy chronically during clinical trials. The underlying mechanisms remain incompletely understood. We tested the hypothesis that deficiency in the liver glucokinase regulatory protein (GKRP) as occurs with common human GCKR variants affects chronic GKA efficacy. We used a Gckr-P446L mouse model for the GCKR exonic rs1260326 (P446L) variant and the Gckr-del/wt mouse to model transcriptional deficiency to test for chronic efficacy of the GKA, AZD1656 in GKRP-deficient states. In the Gckr-P446L mouse, the blood glucose lowering efficacy of AZD1656 (3 mg/kg body wt) after 2 weeks was independent of genotype. However after 19 weeks, efficacy was maintained in wild-type but declined in the LL genotype, in conjunction with raised hepatic glucokinase activity and without raised liver lipids. Sustained blood glucose lowering efficacy in wild-type mice was associated with qualitatively similar but more modest changes in the liver transcriptome compared with the P446L genotype, consistent with GKA therapy representing a more modest glucokinase excess than the P446L genotype. Chronic treatment with AZD1656 in the Gckr-del/wt mouse was associated with raised liver triglyceride and hepatocyte microvesicular steatosis. The results show that in mouse models of liver GKRP deficiency in conjunction with functional liver glucokinase excess as occurs in association with common human GCKR variants, GKRP-deficiency predisposes to declining efficacy of the GKA in lowering blood glucose and to GKA induced elevation in liver lipids.

pharmacology and toxicology↗

The Retrosplenial Cortical Role in Delayed Spatial Alternation.

The retrosplenial cortex (RSC) plays an important role in spatial cognition. RSC neurons exhibit a variety of spatial firing patterns and lesion studies have found that the RSC is necessary for spatial working memory tasks. However, little is known about how RSC neurons might encode spatial memory during a delay period. In the present study, we trained control rats and rats with excitotoxic lesions of the RSC on spatial alternation task with varying delay durations and in a separate group of rats, we recorded RSC neuronal activity as the rats performed the alternation task. We found that RSC lesions significantly impaired alternation performance, particularly at the longest delay duration. We also found that RSC neurons exhibited reliably different firing patterns throughout the delay periods preceding left and right trials, consistent with a working memory signal. These differential firing patterns were absent during the delay periods preceding errors. We also found that many RSC neurons exhibit a large spike in firing rate leading up to the start of the trial. Many of these trial start responses also differentiated left and right trials, suggesting that they could play a role in priming the go left or go right behavioral responses. Our results suggest that these firing patterns represent critical memory information that underlies the RSC role in spatial working memory.

neuroscience↗

ProEnd: A Comprehensive Database for Identifying HbYX Motif-Containing Proteins Across the Tree of Life

The proteasome plays a crucial role in cellular homeostasis by degrading misfolded, damaged, or unnecessary proteins. Understanding the regulatory mechanisms of proteasome activity is vital, particularly the interaction with activators containing the hydrophobic-tyrosine-any amino acid (HbYX) motif. Here, we present ProEnd, a comprehensive database designed to identify and catalog HbYX motif-containing proteins across the tree of life. Using a simple bioinformatics pipeline, we analyzed approximately 73 million proteins from 22,000 reference proteomes in the UniProt/SwissProt database. Our findings reveal the widespread presence of HbYX motifs in diverse organisms, highlighting their evolutionary conservation and functional significance. Notably, we observed an interesting prevalence of these motifs in viral proteomes, suggesting strategic interactions with the host proteasome. As validation two novel HbYX proteins found in this database were tested and found to directly interact with the proteasome. ProEnds extensive dataset and user-friendly interface enable researchers to explore the potential proteasomal regulator landscape, generating new hypotheses to advance proteasome biology. This resource is set to facilitate the discovery of novel therapeutic targets, enhancing our approach to treating diseases such as neurodegenerative disorders and cancer. Link: http://proend.org/

cell biology↗