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Pant, A.

Publications and source records attributed to Pant, A..

At least 19 recordsLinked to original sources

Complementary cytotoxicity of GD2-targeted photoimmunotherapy and 5-aminolevulinic acid photodynamic therapy in neuroblastoma and osteosarcoma

Phototherapy, a light-activated anticancer treatment, enables localized tumor-cell killing with distinct mechanisms of action. Photoimmunotherapy (PIT) produces immunogenic tumor cell death upon near-infrared light activation of a photoabsorber through antigen-specific targeting. Photodynamic therapy (PDT) produces reactive oxygen species through red-light activation of intracellular protoporphyrin IX generated from 5-aminolevulinic acid uptake and metabolism. PIT may have limited activity in antigen-low cells, whereas PDT has less precise tumor selectivity. We combined these modalities to define their interaction, broaden cytotoxicity, and determine whether dual treatment could reduce light-dose requirements. We conjugated dinutuximab, which targets the GD2 antigen, to IRDye 700DX and characterized plasma-membrane localization by confocal and widefield microscopy. PIT and PDT monotherapies were evaluated across agent and light doses in neuroblastoma (NB) and osteosarcoma (OS) cell lines. Combination matrices were tested using interaction, highest-single-agent, and Bliss analyses. Both monotherapies demonstrated significant light-dose-dependent effects in NB and OS. PIT produced no measurable cytotoxicity in antigen-blunted control cells, whereas PDT remained effective, confirming antigen-dependence of PIT and antigen-independence of PDT. The combination interaction was significant in SK-N-BE(2) but not LM7. At selected combinations, however, dual treatment produced greater killing than the more effective matched monotherapy in both SK-N-BE(2) and LM7 (Padj<0.022). Notably, lowest combination of PIT 10 J/cm2 plus PDT 10 J/cm2 achieved 90.3% killing in SK-N-BE(2), exceeding higher light-dose PIT or PDT monotherapy, suggesting a light-dose sparing effect. These findings establish potent and complementary PIT-PDT activity, supporting dual phototherapy to broaden cytotoxicity and reduce light-dose requirements in GD2-expressing tumor phototherapy.

cancer biology↗

Engineering the mechanosensitivity of single DNA molecules via high-throughput microfluidic force spectroscopy

Single-molecule force spectroscopy (SMFS) is a powerful tool to measure how biomolecules respond to mechanical force, but limited sequence throughput constrains its potential. Here, we present a single-molecule, multiplexed, microfluidic force spectroscopy (SM3FS) assay that uses parallelized microfluidics to measure up to 80 sequence variants per experiment. Using SM3FS, we stretched, overstretched, or unzipped 241 different DNA structures and generated 131,847 single-molecule traces from a quarter-million observations. High sequence throughput allowed us to identify DNA structures that are kinetically stable yet mechanically fragile (Frupture < 3 pN at 0.5 pN s-1), revealing how mechanosensitivity can arise as an intrinsic property of multivalent systems. By enabling systematic sequence-function mapping under force, SM3FS opens a path to high-throughput nonequilibrium studies of biomolecules.

biophysics↗

Mast cell extracellular granules are bioactive condensates driven by heparin and polyamine

Biomolecular condensates are membraneless bodies that organize biochemical reactions typically within cells. However, the roles of condensates in extracellular space--where conditions differ substantially from intracellular space--remain poorly understood. Here, we report mast cell extracellular granules (MCEGs), a stable membraneless entity, are condensates assembled via electrostatic interactions between glycosaminoglycans and polyamines. Disrupting polyamine synthesis or trafficking blocks MCEG formation and compromises the storage of proteases and cytokines. Granules reconstituted with heparin and spermine are sufficient to enrich mediators such as CPA3 and TNF, maintaining an elevated pH and higher concentrations of calcium and zinc compared to the extracellular milieu. This unique environment enhances CPA3 enzymatic activity. Furthermore, the granules increase TNF binding and its bioactivity toward endothelial cells. Together, we reveal MCEGs as functionally active biomolecular condensates with distinct biochemical and immunological properties; MCEGs are formed through sugar-metabolite interactions, expanding the mechanisms of condensate assembly beyond classical protein-protein and protein-RNA interactions.

cell biology↗

Discovery and Characterization of a Hydroxypyridone-3-carboxamide Analog as an Antiviral Lead against Orthopoxviruses

Orthopoxviruses remain a persistent global health concern due to the ongoing circulation of mpox, the possibility of the re-emergence of smallpox, and the threats posed by many poxviruses that infect animals and/or humans. The limited availability of antiviral drugs, the unproven efficacy in humans, and the emergence of resistant mutants underscore the need for new and better therapeutics. In this study, we identify and characterize ZW-2038, a hydroxypyridone-3-carboxamide analog, as an antiviral compound against vaccinia virus (VACV), monkeypox virus (MPXV), and cowpox virus (CPXV). Discovered through a focused in-house small-molecule screen, ZW-2038 exhibited low micromolar potency and high selectivity in primary human fibroblasts. The compound also reduced viral replication under physiomimetic conditions including human and monkey intestinal organoids (enteroids) and ex vivo mouse lung tissue models. Mechanistically, ZW-2038 suppresses VACV DNA replication and downstream post-replicative gene expression, albeit without inhibiting MPXV resolvase (Mpr) in vitro. These findings, along with in vitro safety profiling and mice pharmacokinetics studies, characterize ZW-2038 as a promising yet suboptimal antiviral lead against orthopoxviruses warranting future development.

microbiology↗

TFEB activation ameliorates listeriolysin O-mediated subversion of lysosomal and LC3 function during Listeria monocytogenes infection

Xenophagy is a crucial innate subcellular defense mechanism, functioning as a selective autophagy pathway that captures intracellular pathogens within xenophagosomes for subsequent lysosomal degradation. However, many pathogens have evolved strategies to subvert this process, ensuring their intracellular replication and survival within the host cell. Despite its significance, the precise mechanisms by which intracellularly motile xenophagy cargo like Listeria monocytogenes (Lm) circumvent this selective autophagy pathway are not yet completely understood. In this study, we identify a previously unrecognized function of the secreted virulence factor listeriolysin (LLO) in orchestrating a multi-layered disruption of host autophagy-lysosomal machinery. While LLO is classically known for its role in mediating vacuolar escape, our findings reveal that it also contains a functional LIR motif which enables LLO to directly bind LC3 in the cytosol, rendering it unavailable for xenophagosome formation. Concurrently, LLO impairs lysosomal function by reducing its hydrolytic capacity and suppresses nuclear translocation of TFEB, a key transcription factor that governs autophagy and lysosome biogenesis, further compromising host degradative pathways. Using various Lm mutant strains, we show that actin-based motility is dispensable for xenophagy evasion. Instead, the intracellular persistence of Lm primarily stems from two factors: LLO-mediated LC3 binding, which diverts LC3 from its xenophagic functions, and the inhibition of TFEB nuclear translocation. Importantly, pharmacological activation of TFEB or genetic disruption of the LLO-LC3 interaction restores xenophagy and substantially reduces bacterial load. Collectively, our findings position LLO as a multifaceted virulence determinant that employs previously uncharacterized mechanisms to subvert host cell-autonomous defense. This study deepens mechanistic insight into the pathogenesis of Lm and highlights LC3 and TFEB as promising therapeutic targets for host-directed therapies against intracellular infections. Highlights{blacksquare} Listeria monocytogenes (Lm) evades xenophagy independently of its host-actin polymerization ability {blacksquare}Listeriolysin O (LLO) impairs lysosomal degradative potential and suppresses TFEB nuclear translocation {blacksquare}LLO binds LC3 through its LC3-interacting region (LIR) motif, effectively limiting LC3 availability for xenophagosome formation {blacksquare}Restoring LC3 and TFEB function enables intracellular clearance of Lm Graphical abstractThe graphical abstract illustrates how vacuolar ({Delta}hlyA), and cytosolic (WT and {Delta}actA) Listeria monocytogenes differentially engage with host-degradative pathways. Listeriolysin O (LLO), a critical virulence factor, is highlighted as the linchpin determining whether these bacteria get targeted for degradation or successfully evade the host response. In {Delta}hlyA strain infected cells, where LLO is absent, (1) the bacteria remain confined within the phagosome. (2 - 4) The phagosomal compartment then fuse with lysosome, to form phagolysosome that is both acidified and hydrolytically active, enabling effective bacterial degradation while sustaining autophagy flux. (5) This process coincides with nuclear translocation of the master transcription regulator, TFEB, which enhances lysosomal biogenesis and function, boosting bacterial clearance. On the other hand, both WT and {Delta}actA strains produce LLO, (1, 2) which allows them to escape from the phagosome into the host cytosol. (3) WT strain induces polymerization of host cell actin, leading to the formation of actin clouds that mature into actin tails, facilitating bacterial mobility and cell to cell spread. (4) The {Delta}actA strain, despite lacking the ability to interact with host actin, still replicates in the cytosol. LLO plays a multifaceted role in evading host defenses. (5 - 6) It limits LC3 availability for nascent xenophagosome formation by binding to LC3, reducing bacterial capture by the xenophagy machinery. (7 - 8) Furthermore, even when a few bacteria are successfully sequestered within phagosome or xenophagosome, LLO-mediated lysosomal dysfunction impair their maturation into degradative phagolysosome and xenolysosome. (9) Compounding this, LLO suppresses nuclear translocation of TFEB, thereby dampening transcriptional activation of autophagy-lysosomal pathways. Collectively, these mechanisms compromise the host degradative capacity, allowing cytosolic bacteria to replicate and evade clearance. Several unanswered questions remain regarding the structural and mechanistic aspects of the interaction of LLO with LC3. It is still unclear whether LC3 conjugation occurs on single or double membrane vesicles, and whether these vesicular structures are fully sealed. Additionally, it is not yet determined if LLO binds LC3 specifically at sites of omegasome or phagophore formation. The aggregation behavior of LLO also raises intriguing possibilities: could these aggregates play a protective role in shielding LLO from its degradation? Furthermore, it remains to be clarified whether LLO exists freely in the cytosol or is associated with specific membrane-bound compartments. Finally, the precise mechanism by which LLO interferes with TFEB nuclear translocation is another critical open question requiring further investigation. O_FIG O_LINKSMALLFIG WIDTH=165 HEIGHT=200 SRC="FIGDIR/small/691302v1_ufig1.gif" ALT="Figure 1"> View larger version (50K): org.highwire.dtl.DTLVardef@21c235org.highwire.dtl.DTLVardef@553714org.highwire.dtl.DTLVardef@932e53org.highwire.dtl.DTLVardef@c686ef_HPS_FORMAT_FIGEXP M_FIG C_FIG

cell biology↗

Ciclopirox suppresses poxvirus replication by targeting iron metabolism

Poxviruses remain a significant global health concern, necessitating the development of novel antiviral strategies. Through high-throughput screening, we previously identified ciclopirox (CPX), an FDA-approved antifungal, as a hit that inhibits vaccinia virus (VACV) replication. Here, we further characterized its antiviral activity and mechanism of action using human primary fibroblasts. CPX significantly reduced VACV titers without reducing host cell viability, with an EC50 in the sub-micromolar range and a CC50 >500 M. Rescue experiments demonstrated that CPX inhibits viral replication primarily through chelation of intracellular Fe3+ and, to a lesser extent, Fe2+, as evidenced by partial restoration of viral replication with ferric ammonium citrate supplementation. Furthermore, overexpression of the iron-dependent enzymes RRM2 and the VACV-encoded F4L reduced the inhibitory effect of CPX, indicating that these host and viral proteins are affected by CPX treatment. Moreover, CPX treatment also suppressed cowpox virus and monkeypox (mpox) virus replication in vitro. It also reduced VACV titers in ex vivo mouse lung tissue. These findings highlight host iron metabolism as a critical determinant of poxvirus replication and support repurposing CPX as a broad-spectrum orthopoxvirus antiviral candidate.

microbiology↗

Molecular grammars of intrinsically disordered regions that span the human proteome

Intrinsically disordered regions (IDRs) of proteins are defined by functionally relevant molecular grammars. This refers to IDR-specific non-random amino acid compositions and non-random patterning of distinct pairs of amino acid types. Here, we introduce GIN (Grammars Inferred using NARDINI+) as a resource, which we have used to extract the molecular grammars of all human IDRs and classified them into thirty distinct clusters. Unbiased analyses of IDRome-spanning grammars reveals that specialized IDR grammar features direct biological processes, cellular localization preferences, and molecular functions. IDRs with exceptional grammars, defined as sequences with high-scoring non-random features, are harbored in proteins and complexes that enable spatial and temporal sorting of biochemical activities. Protein complexes within the nucleus recruit specific factors through top-scoring IDRs. These IDRs are frequently disrupted via cancer-associated mutations and fusion oncoproteins. Overall, GIN enables the decoding of sequence-function relationships of IDRs and can be deployed in IDR-specific and IDRome-wide analyses.

bioinformatics↗

Nuclear speckle proteins form intrinsic and MALAT1-dependent microphases

Nuclear speckles are enriched in serine / arginine rich splicing factors (SRSFs), such as SRSF1. Splicing factors and proteins such as TDP-43 concentrate into distinct speckle territories to enable pre-mRNA processing. We have discovered that SRSFs and TDP-43 are block copolymers and the protein-specific interplay of inter-block repulsions and attractions drives spontaneous microphase separation. This gives rise to size-limited, ordered assemblies, that are 30 - 45 nm in diameter. Depending on the protein, each microphase comprises several tens to hundreds of molecules. The sub-micron scale territories observed in cells are shown to be clusters of microphases. The regulatory lncRNA MALAT1 binds preferentially to SRSF1 microphases to enhance microphase separation and alter microphase structures. Microphase separation enables the concentration of finite numbers of splicing factors into assemblies with distinct nanoscale structures that can be modulated by MALAT1. Our findings provide a structural framework for the functional organization of splicing factors.

biophysics↗

JNK2 pathway in colonocytes enhances gut barrier integrity in response to microbial acetate.

Weaning involves a nutritional shift from fat-rich milk to carbohydrate-based solid food, reshaping metabolism, microbiota, and gut immune tolerance. While dairy remains a component of the human diet beyond weaning, the impact of continued milk supplementation on gut epithelial homeostasis remains poorly understood. Here, using a mouse model, we show that continued milk-based feeding post-weaning promotes intestinal barrier function by enriching the commensal bacterium Dubosiella newyorkensis, which produces acetate to activate epithelial JNK2 signaling. This pathway enhances barrier integrity and suppresses inflammation induced by mild Dextran Sodium Sulphate (DSS) treatment. In contrast, feeding a lard-based high-fat diet or transient pharmacologic inhibition of JNK2 induces epithelial P38 activation, resulting in barrier disruption and inflammation. Importantly, the beneficial effects of milk were observed only if initiated during the weaning period, when the microbiome is in a metastable transitional state. Initiation of the same intervention two weeks after weaning led to P38 activation and inflammatory responses. These findings highlight the microbiome-dependent, stage-specific effects of diet and underscore the importance of early-life nutritional interventions for long-term gut health.

physiology↗

Genome-wide in vivo dynamics of cohesin-mediated loop extrusion and its role in transcription activation

The organization of the genome in three-dimensional space is highly dynamic, yet how these dynamics are regulated and the role they play in genome function is poorly understood. Here, we utilized acute depletion of NIPBL to characterize the role of cohesin-mediated loop extrusion in vivo. Using this approach, we found that many chromatin loops are rapidly diminished upon loss of NIBPL, consistent with recent single locus imaging studies showing that chromatin loops are transient. However, we also identified cohesin-dependent chromatin loops that are associated with distinct chromatin states and may be "long-lived", given that they require NIPBL for their establishment upon mitotic exit, but are persistent when NIPBL is depleted from interphase cells. In addition to the reformation of 3D genome structures, mitotic exit coincides with widespread transcriptional activation. We found that NIPBL is essential for establishing the expression of lineage-defining genes during the M-G1 transition but has diminished impact on the steady-state maintenance of their expression. At genes sensitive to its depletion, NIPBL supports a unique local genome organization defined by greater spatial proximity to nearby super-enhancers and weaker transcription start site insulation of genomic contacts. Overall, we show that NIPBL-mediated loop extrusion is critical to genome organization and transcription regulation in vivo.

molecular biology↗

Adaptive Nesting Strategies of Dusky Crag Martins in desert ecoregions: Implications for Conservation and Bioinspired Innovations

Understanding the adaptive strategies of species in extreme environments is crucial for biodiversity conservation. This study is the first to explore the nesting behavior of the Dusky Crag Martin Ptyonoprogne concolor in the Thar Desert, Rajasthan. It examined the birds site selection, nesting frequency, and construction methods. Soil samples from nest sites and source locations were analyzed to identify structural and elemental properties. The bird adopts several strategies, such as aligning its nesting period with the monsoon, reusing nests, and utilizing both macro and micro-level additive construction techniques. Detailed analysis revealed a preference for cohesionless sand with low moisture and higher Soil Organic Carbon (SOC) content. The bird strategically alternates light and dark soil layers in its nest. Structural and elemental analyses using optical microscopy and Scanning Electron Microscopy (SEM), and X-ray Fluorescence (XRF), shows the light layers is rich in calcium oxide and fibrous material, and dark layers containing higher iron oxide and partially decomposed litter from Prosopis cineraria. The study concludes that alternating calcium-rich and iron-rich layers enhances energy efficiency, structural integrity, and pathogen resistance in nest construction. his behavior underscores the evolutionary adaptations of P. concolor to the extreme desert environment. These findings highlight the importance of conserving desert habitats and provide bio-inspired insights for sustainable building and agricultural practices in arid regions.

ecology↗

Driving forces for condensation of synapsin are governed by sequence-encoded molecular grammars

Multiple biomolecular condensates coexist at the pre- and post-synapse to enable vesicle dynamics and controlled neurotransmitter release in the brain. In pre-synapses, intrinsically disordered regions (IDRs) of synaptic proteins are drivers of condensation that enable clustering of synaptic vesicles (SVs). Using computational analysis, we show that the IDRs of SV proteins feature evolutionarily conserved non-random compositional biases and sequence patterns. Synapsin-1 is essential for condensation of SVs, and its C-terminal IDR has been shown to be a key driver of condensation. Focusing on this IDR, we dissected the contributions of two conserved features namely the segregation of polar and proline residues along the linear sequence, and the compositional preference for arginine over lysine. Scrambling the blocks of polar and proline residues weakens the driving forces for forming micron-scale condensates. However, the extent of clustering in subsaturated solutions remains equivalent to that of the wild-type synapsin-1. In contrast, substituting arginine with lysine significantly weakens both the driving forces for condensation and the extent of clustering in subsaturated solutions. Co-expression of the scrambled variant of synapsin-1 with synaptophysin results in a gain-of-function phenotype in cells, whereas arginine to lysine substitutions eliminate condensation. We report an emergent consequence of synapsin-1 condensation, which is the generation of interphase pH gradients realized via differential partitioning of protons between coexisting phases. This pH gradient is likely to be directly relevant for vesicular ATPase functions and the loading of neurotransmitters. Our study highlights how conserved IDR grammars serve as drivers of synapsin-1 condensation. Research HighlightsO_LIDistinct biomolecular condensates formed by pre-synaptic proteins contain a unique bias of sequence grammars within their IDRs. C_LIO_LIThe IDR of synapsin-1, the essential protein for the clustering of synaptic vesicles, has a conserved compositional bias for Arg and blockiness of proline/polar residues. C_LIO_LIUsing sequence designs, we uncovered how conserved sequence features of the driver IDR of synapsin-1 affect condensation in vitro and in cells. C_LIO_LISynapsin-1 condensates are defined by a measurable interphase pH gradient. C_LI

biochemistry↗

Biomolecular condensates are characterized by interphase electric potentials

Biomolecular condensates form via processes that combine phase separation and reversible associations of multivalent macromolecules. Condensates can be two- or multi-phase systems defined by coexisting dense and dilute phases. Here, we show that solution ions can partition asymmetrically across coexisting phases defined by condensates formed by intrinsically disordered proteins or homopolymeric RNA molecules. Our findings were enabled by direct measurements of the activities of cations and anions within coexisting phases of protein and RNA condensates. Asymmetries in ion partitioning between coexisting phases vary with protein sequence, condensate type, salt concentration, and ion type. The Donnan equilibrium set up by asymmetrical partitioning of solution ions generates interphase electric potentials known as Donnan and Nernst potentials. Our measurements show that the interphase potentials of condensates are of the same order of magnitude as membrane potentials of membrane-bound organelles. Interphase potentials quantify the degree to which microenvironments of coexisting phases are different from one another. Importantly, and based on condensate-specific interphase electric potentials, which are membrane-like potentials of membraneless bodies, we reason that condensates are mesoscale capacitors that store charge. Interphase potentials lead to electric double layers at condensate interfaces. This helps explain recent observations of condensate interfaces being electrochemically active.

biophysics↗

Role of vaccinia virus growth factor in stimulating the mTORC1-CAD axis of the de novo pyrimidine pathway under different nutritional cues

Vaccinia virus (VACV), the prototype poxvirus, actively reprograms host cell metabolism upon infection. However, the nature and molecular mechanisms remain largely elusive. Given the diverse nutritional exposures of cells in different physiological contexts, it is essential to understand how VACV may alter various metabolic pathways in different nutritional conditions. In this study, we established the importance of de novo pyrimidine biosynthesis in VACV infection. We elucidated the significance of vaccinia growth factor (VGF), a viral early protein and a homolog of cellular epidermal growth factor, in enabling VACV to phosphorylate the key enzyme CAD of the de novo pyrimidine pathway at serine 1859, a site known to positively regulate CAD activity. While nutrient-poor conditions typically inhibit mTORC1 activation, VACV activates CAD via mTORC1-S6K1 signaling axis, in conditions where glutamine and asparagine are absent. However, unlike its cellular homolog, epidermal growth factor (EGF), VGF peptide alone in the absence of VACV infection has minimal ability to activate CAD, suggestive of the involvement of other viral factor(s) and differential functions to EGF acquired during poxvirus evolution. Our research provides a foundation for understanding the regulation of a significant metabolic pathway, namely, de novo pyrimidine synthesis during VACV infection, shedding new light on viral regulation under distinct nutritional environments. This study not only has the potential to contribute to the advancement of antiviral treatments but also improve the development of VACV as an oncolytic agent and vaccine vector. ImportanceOur research provides new insights into how VACV alters the mTORC1-CAD signaling axis under different nutritional cues. The identification of how VACV regulates a major enzyme, CAD, within the de novo pyrimidine synthesis pathway, establishes a molecular mechanism for determining how VACV reshapes this essential pathway, necessary for facilitating efficient VACV replication. We further emphasize that, despite nutrient-poor conditions, which typically inhibit mTORC1 activation, VACV can stimulate mTORC1. We identify its early growth factor, VGF, as an important factor for this stimulation of mTORC1 and its downstream effector CAD, revealing a new mechanism for how VACV sustains mTORC1-CAD axis activation under these nutrient deficient conditions. This work provides fresh insights into the molecular mechanisms of mTORC1-CAD regulation, which has the potential to be utilized to enhance VACV as an oncolytic tool, vaccine vector and aid in the development of antiviral drugs.

microbiology↗

Nrf2 regulates the activation-driven expansion of CD4+ T-cells by differentially modulating glucose and glutamine metabolism

SUMMARYUpon antigenic stimulation, CD4+T-cells undergo clonal expansion, elevating their bioenergetic demands and utilization of nutrients like glucose and glutamine. The nuclear factor erythroid 2-related factor 2 (Nrf2) is a well-known regulator of oxidative stress, but its involvement in modulating the metabolism of CD4+T-cells remains unexplored. Here, we elucidate the role of Nrf2 beyond the traditional antioxidation, in modulating activation-driven expansion of CD4+T-cells by influencing their nutrient metabolism. T-cell-specific activation of Nrf2 enhances early activation and IL-2 secretion, upregulates TCR-signaling, and increases activation-driven proliferation of CD4+T-cells. Mechanistically, high Nrf2 inhibits glucose metabolism through glycolysis but promotes glutamine metabolism via glutaminolysis to support increased T-cell proliferation. Further, Nrf2 expression is temporally regulated in activated CD4+T-cells with elevated expression during the early activation, but decreased expression thereafter. Overall, our findings uncover a novel role of Nrf2 as a metabolic modulator of CD4+T-cells, thus providing a framework for improving Nrf2-targeting therapies and T-cell immunotherapies.

immunology↗

Upregulation of ATP Citrate Lyase Phosphorylation and Neutral Lipid Synthesis through Viral Growth Factor Signaling during Vaccinia Virus Infection

Like all other viruses, poxviruses rely on host cells to provide metabolites and energy. Vaccinia virus (VACV), the prototype poxvirus, induces profound metabolic alterations in host cells. We previously showed that VACV infection increases the tricarboxylic acid (TCA) cycle intermediates, including citrate, that can be transported to the cytosol to be converted to acetyl-CoA for de novo fatty acid biosynthesis. ATP citrate lyase (ACLY) is a pivotal enzyme converting citrate to acetyl-CoA. Here, we report that VACV infection stimulates the S455 phosphorylation of ACLY, a post-translational modification that stimulates ACLY activity. We demonstrate that the chemical and genetic inhibition of ACLY severely suppresses VACV replication. Remarkably, we found that virus growth factor (VGF)-induced signaling is essential for the VACV-mediated upregulation of ACLY phosphorylation. Furthermore, the upregulation of ACLY phosphorylation during VACV infection is dependent on the activation of the cellular Akt kinase that phosphorylates ACLY. Finally, we report that VGF-induced ACLY phosphorylation via the EGFR-Akt pathway is important for VACV stimulations of neutral lipid droplet synthesis. These findings identified a previously unknown way of rewiring cell metabolism by a virus and a novel function for VGF in the governance of virus-host interactions through the induction of a key enzyme at the crossroads of the TCA cycle and fatty acid de novo biosynthesis. Our study also provides a mechanism for the role played by VGF and its downstream signaling cascades in the modulation of lipid metabolism in VACV-infected cells. ImportanceATP citrate lyase is a key metabolic enzyme that sits at the crossroads of glucose, glutamine, and lipid metabolism. However, how virus infection affects this protein is unclear. Using chemical, genetic, and metabolic approaches we show that VACV, the prototype poxvirus, increases the phosphorylation of ACLY in primary human fibroblasts in a VGF-dependent manner. We further show that the VGF-EGFR-Akt signaling pathway is vital for VACV-induced lipid droplet synthesis. Our findings identified ACLY as a potential target for novel antiviral development against pathogenic poxviruses. Our study also expands the role of growth factor signaling in boosting VACV replication by targeting multiple metabolic pathways.

microbiology↗

Antiviral activities of two nucleos(t)ide analogs against vaccinia and mpox viruses in primary human fibroblasts

Many poxviruses are significant human and animal pathogens, including viruses that cause smallpox and mpox. Identification of inhibitors of poxvirus replication is critical for drug development to manage poxvirus threats. Here we tested two compounds, nucleoside trifluridine and nucleotide adefovir dipivoxil, for antiviral activities against vaccinia virus (VACV) and mpox virus (MPXV) in physiologically relevant primary human fibroblasts. Both trifluridine and adefovir dipivoxil potently inhibited replication of VACV and MPXV (MA001 2022 isolate) in a plaque assay. Upon further characterization, they both conferred high potency in inhibiting VACV replication with half maximal effective concentrations (EC50) at low nanomolar levels in our recently developed assay based on a recombinant VACV secreted Gaussia luciferase. Our results further validated that the recombinant VACV with Gaussia luciferase secretion is a highly reliable, rapid, non-disruptive, and simple reporter tool for identification and chracterization of poxvirus inhibitors. Both compounds inhibited VACV DNA replication and downstream viral gene expression. Given that both compounds are FDA-approved drugs, and trifluridine is used to treat ocular vaccinia in medical practice due to its antiviral activity, our results suggest that it holds great promise to further test trifluridine and adefovir dipivoxil for countering poxvirus infection, including mpox.

microbiology↗

Interleukin-6 Drives Key Pathologic Outcomes in Experimental Acetaminophen-induced Liver Failure

Background and AimsIn severe cases of acetaminophen (APAP) overdose, acute liver injury rapidly progresses to acute liver failure (ALF), producing life-threatening complications including, hepatic encephalopathy (HE) and multi-organ failure (MOF). Systemic levels of interleukin-6 (IL-6) and IL-10 are highest in ALF patients with the most severe complications and the poorest prognosis. The mechanistic basis for dysregulation of these cytokines, and their association with outcome in ALF, remain poorly defined. MethodsTo investigate the impact of IL-6 and IL-10 in ALF, we used an experimental setting of failed liver repair after APAP overdose in which a high dose of APAP is administered (i.e., 500-600 mg/kg). Mice were treated with neutralizing antibodies to block IL-6 and IL-10. ResultsIn mice with APAP-induced ALF, high levels of IL-10 reduced monocyte recruitment and trafficking in the liver resulting in impaired clearance of dead cell debris. Kupffer cells in these mice, displayed features of myeloid-derived suppressor cells, including high level expression of IL-10 and PD-L1, which were increased in an IL-6-dependent manner. Similar to ALF patients with HE, cerebral blood flow was reduced in mice with APAP-induced ALF. Remarkably, although IL-6 is hepatoprotective in mice treated with low doses of APAP (i.e., 300 mg/kg), IL-6 neutralization in mice with APAP-induced ALF fully restored cerebral blood flow and reduced mortality. ConclusionCollectively, these studies demonstrate that exaggerated production of IL-6 in APAP-induced ALF triggers immune suppression (i.e., high levels of IL-10 and PD-L1), reduces cerebral blood flow (a feature of hepatic encephalopathy), disrupts liver repair (i.e., failed clearance of dead cells), and increases mortality.

pathology↗