bims-toxgon Biomed News
on Toxoplasma gondii metabolism
Issue of 2025–08–17
24 papers selected by
Lakesh Kumar, BITS Pilani



  1. Int J Parasitol. 2025 Aug 07. pii: S0020-7519(25)00136-5. [Epub ahead of print]
      Toxoplasma gondii is a zoonotic protozoan pathogen capable of infecting humans and nearly all warm-blooded animals, and causing substantial economic losses to the livestock industry. Developing an effective vaccine against T. gondii remains an urgent priority for controlling the spread of this zoonotic parasite. In this study, we evaluated the protective efficacy of a live-attenuated T. gondii PruΔpp2a-c mutant in both mice and cats. Immunization with PruΔpp2a-c elicited strong cellular (IL-2, IL-4, IL-10, IL-12, and IFN-γ) and humoral (IgG, IgG1, and IgG2a) immune responses in mice, conferring protection against lethal challenge with various T. gondii strains, including highly virulent Type I (RH), mildly virulent ToxoDB#9 (PYS), and less virulent Type II (Pru) strains. While partial protection was observed against virulent strains, almost complete immune protection was achieved against both acute and chronic infections by the less virulent Pru strain, along with a significant reduction in brain cyst burden (P < 0.01). Notably, vaccination of cats with PruΔpp2a-c induced high antibody titers and led to a 94.5% reduction in fecal oocyst shedding (P < 0.001) following homologous challenge, thereby significantly decreasing the potential for environmental transmission. These findings demonstrate that PruΔpp2a-c provides strong cross-protection against various T. gondii strains and substantially limits oocyst shedding. The dual efficacy observed in both intermediate and definitive hosts highlights PruΔpp2a-c as a promising live-attenuated vaccine candidate for preventing transmission of T. gondii by cats.
    Keywords:  PP2A-C; Toxoplasma gondii; cats; immunity; live-attenuated vaccine; mice
    DOI:  https://doi.org/10.1016/j.ijpara.2025.08.002
  2. Pharmacol Ther. 2025 Aug 07. pii: S0163-7258(25)00120-2. [Epub ahead of print] 108908
      Post-translational acetylation of lysine residues is a dynamic and reversible modification that plays a pivotal role in regulating protein structure, function, and interactions. This modification is mediated by central metabolite acetyl-CoA and is tightly controlled by the opposing actions of lysine acetyltransferases (KATs) and lysine deacetylases (KDACs), including the NAD+-dependent sirtuins. As a nutrient-sensing post-translational modification (PTM), acetylation is essential for maintaining cellular homeostasis, particularly by modulating proteostasis and metabolic flexibility-the ability of cells to rewire metabolic pathways in response to fluctuating energy demands and nutrient availability. Dysregulation of acetylation has been implicated in the pathogenesis of metabolic disorders, neurodegenerative diseases, and cancer. Emerging evidence suggests that targeting acetylation-regulating enzymes with small-molecule inhibitors or activators hold promise for elucidating the role of acetylation in metabolic sensing and protein homeostasis, also known as proteostasis. This review examines the regulation of acetylation across various metabolic states, its impact on metabolic adaptability, and its intricate interplay with proteostasis mechanisms. Additionally, it highlights the role of site-specific acetylation dynamics and sirtuin biology shaping metabolic regulation, providing key insights into the mechanisms underlying metabolic disorders and their progression. Understanding the regulatory mechanisms governing acetylation-dependent metabolic sensing could facilitate the development of precision therapeutics to restore metabolic homeostasis.
    Keywords:  Acetylation; Autophagy; Deacetylation; Metabolic flexibility; Proteastasis; Sirtuins
    DOI:  https://doi.org/10.1016/j.pharmthera.2025.108908
  3. mBio. 2025 Aug 13. e0138925
      One of the defining features of apicomplexan parasites is their cytoskeleton composed of alveolar vesicles, known as the inner membrane complex (IMC) undergirded by an intermediate filament-like protein network and an array of subpellicular microtubules (SPMTs). In Toxoplasma gondii, this specialized cytoskeleton is involved in all aspects of the disease-causing lytic cycle and notably acts as a scaffold for parasite offspring in the internal budding process. Despite advances in our understanding of the architecture and molecular composition, insights pertaining to the coordinated assembly of the scaffold are still largely elusive. Here, T. gondii tachyzoites were dissected by advanced, iterative expansion microscopy (pan-expansion microscopy), revealing new insights into the very early sequential formation steps of the tubulin and IMC scaffold. A comparative study of the related parasite Sarcocystis neurona revealed that different MT bundling organizations of the nascent SPMTs correlate with the number of central and basal alveolar vesicles. In the absence of a so-far identified MT nucleation mechanism, we genetically dissected T. gondii γ-tubulin and γ-tubulin complex proteins 4, 5, and 6 (GCP4/5/6). While γ-tubulin depletion abolished the formation of the tubulin scaffold, a set of MTs still formed that suggests SPMTs are nucleated at the outer core of the centrosome. Depletion of GCP4/5/6 interfered with the correct assembly of nascent SPMTs into the forming daughter buds, further indicating that the parasite utilizes the γ-tubulin ring complex in tubulin scaffold formation.IMPORTANCEApicomplexan protozoan parasites rely on their specialized cytoskeleton to form offspring. The cytoskeleton serves as an essential scaffold for the emerging daughter cells and is formed by the inner membrane complex (IMC) and underlying subpellicular microtubules (SPMTs). In Toxoplasma gondii, the IMC is composed of several membranous sacks and supported by 22 SPMTs, the latter are evenly spaced around the apical end of mature parasites. Although many advances have been made, little is known about the earliest steps of scaffold formation. Here, we gain unprecedented insights into IMC and SPMT establishment via iterative expansion microscopy and comparative cell biology. We show that at the onset of division, SPMTs are grouped and reveal that the number of groups determines the number of IMC sacks that are assembled. We further dissect the parasite's γ-tubulin ring complex and show that it is critically involved in scaffold formation.
    Keywords:  APR; IMC; SFA; Sarcocystis; Toxoplasma; alveoli; microtubules; γ-tubulin; γTuRC
    DOI:  https://doi.org/10.1128/mbio.01389-25
  4. bioRxiv. 2025 Jul 14. pii: 2025.07.14.664749. [Epub ahead of print]
      Some of the longest 5' untranslated regions (UTRs) documented in eukaryotes belong to parasites of the phylum Apicomplexa. Translational regulation plays prominent roles in the development of these parasites, including the agents of toxoplasmosis ( Toxoplasma gondii ) and malaria. To understand the function of 5' UTRs in apicomplexan translation, we performed high-resolution ribosome profiling of T. gondii in human fibroblasts. We show that parasite translation efficiency (TE) is largely controlled by 5' UTR features and tuned by the number of upstream AUGs (uAUGs). Examination of ribosome occupancy reveals that, despite widespread assembly of parasite monosomes on uAUGs, ribosomes seldom translate uORFs. These determinants of translation are reaffirmed in a massively parallel reporter assay examining the effect of more than 30,000 synthetic 5' UTRs in T. gondii . A model trained on these results accurately predicted the TE of newly designed 5' UTRs. Together, this work defines the regulatory language of T. gondii translation, providing a framework to understand the evolution of exceptionally long 5' UTRs in apicomplexans.
    DOI:  https://doi.org/10.1101/2025.07.14.664749
  5. DNA Repair (Amst). 2025 Aug 07. pii: S1568-7864(25)00078-3. [Epub ahead of print]152 103882
      Toxoplasma gondii is an obligate intracellular parasite with a high replication rate that can lead to DNA replicative stress, in turn associated with the generation of DNA double-strand breaks (DSBs). Cells have two main pathways to repair DSBs: non-homologous end joining and homologous recombination repair (NHEJ and HRR respectively). RAD51 is the key recombinase in the HRR pathway. In this work, we achieved endogenous tagging of the RAD51 gene using the Auxin Inducible Degron (AID) system, to generate the clonal line RH RAD51HA-AID. Here we demonstrate that RAD51 is expressed in replicative tachyzoites and establishes damage foci. Auxin-induced knock-down (KD) affects the correct replication of tachyzoites which show loss of synchronization. The use of the RAD51 inhibitor B02 also affects parasite growth, with an IC50 of 4.8 µM. B02 produced alterations in tachyzoite replication and arrest in the S phase of the cell cycle. Additionally, B02 induced tachyzoite to bradyzoite differentiation showing small cyst-like structures. In conclusion, RAD51 is necessary for maintaining proper tachyzoite replication under normal growth conditions, supporting that genome instability occurs during the cell cycle. Our findings also suggest that DNA replication stress can induce bradyzoite differentiation.
    Keywords:  B02; DNA replication stress; Homologous recombination repair; RAD51; Toxoplasma gondii
    DOI:  https://doi.org/10.1016/j.dnarep.2025.103882
  6. Science. 2025 Aug 14. 389(6761): 685-686
      Metabolic immunity contributes to cells' defenses against Toxoplasma gondii.
    DOI:  https://doi.org/10.1126/science.aea0875
  7. Eur J Med Chem. 2025 Aug 09. pii: S0223-5234(25)00822-0. [Epub ahead of print]299 118057
      Toxoplasma gondii, an obligate intracellular parasite, infects approximately one-third of the global population, making toxoplasmosis a significant public health concern. The current treatment - typically a combination of pyrimethamine and sulfadiazine - is limited to the acute phase of infection, and it often causes allergic reactions and severe side effects. Marinoquinolines (MQs), a class of compounds originally isolated from marine microorganisms, have exhibited promising pharmacological properties including anti-T. gondii activity in both in vitro and in vivo models. Addressing the need for more effective and safer therapies, this study investigated novel synthetic MQ derivatives for their inhibitory effects against the parasite. Seventeen MQs were synthesized with indole moieties incorporated into the marinoquinoline scaffold. All compounds were evaluated for half-maximal effective concentration (EC50) against intracellular T. gondii tachyzoites (RH strain) and half-maximal cytotoxic concentration (CC50) in human foreskin fibroblasts (HFFs). Selectivity indices (SICC50/EC50) were calculated. Two derivatives showed outstanding selectivity with SI values of 516 and 751 along with favourable in silico ADMET profiles including high gastrointestinal absorption, blood-brain barrier permeability, and no predicted toxicity. These findings support the potential of indole-based MQs as promising candidates for further preclinical development in the treatment of toxoplasmosis.
    Keywords:  Antiparasitic drug discovery; Blood-brain barrier permeability in vitro and in silico evaluation; Marinoquinoline derivatives; Toxoplasma gondii
    DOI:  https://doi.org/10.1016/j.ejmech.2025.118057
  8. bioRxiv. 2025 Jul 16. pii: 2025.07.16.665172. [Epub ahead of print]
      Chromatin remodeling complexes dynamically modify DNA accessibility to mediate changes in gene expression during eukaryotic cell cycle progression, developmental transitions, and environmental adaptation. Higher eukaryotes have multiple remodeler subtypes based on the incorporation of different ATPases; however, the coordination and functional specificity of these diverse complexes is not well understood. Apicomplexan parasites such as Toxoplasma gondii have a limited set of chromatin remodelers offering a divergent setting in which to explore the function of homologous complexes. These parasites have selectively retained the Myb domain-containing proteins with homology to chromatin-associated regulators like SNF2H and SWI3. Here, a comprehensive analysis of the Myb protein family in Toxoplasma defines the composition of two SWI3 complexes defined by mutually exclusive ATPases with homology to the widely conserved BRG1 and BRM. Integrating transcriptomics with a custom chromatin-profiling strategy, we show that BRG1 is essential for the timely transcription of genes during mitosis and cytokinesis, while BRM ensures global transcriptional competency and fidelity throughout the cell cycle and developmental transitions. Our findings demonstrate that BRG1 and BRM perform distinct yet interdependent regulatory roles shaped by their chromatin context. This work uncovers ancestral principles of chromatin regulation and offers new insight into the functional diversification of SWI/SNF complexes across eukaryotes.
    DOI:  https://doi.org/10.1101/2025.07.16.665172
  9. Nanomedicine (Lond). 2025 Aug 13. 1-12
       AIM: Toxoplasma gondii dense granule antigen 7 (GRA7) is a membrane-associated protein expressed across parasite life cycle and represents a promising vaccine target. This study aimed to develop a GRA7-based virus-like particle (VLP) vaccine and assess its protective efficacy.
    MATERIALS & METHODS: GRA7 VLPs were constructed using an influenza M1 scaffold via the baculovirus expression system. Female BALB/c mice were immunized intranasally three times and orally challenged with lethal T. gondii ME49 cysts. Humoral and cellular immune responses, brain inflammation, and parasite burden were evaluated at 40 days post-infection. Body weight reduction and survival rate were monitored after challenge.
    RESULTS: GRA7 VLPs induced robust T. gondii-specific IgG in serum after immunization. Following challenge with cysts, elevated antibody levels were detected in intestinal, fecal, and brain tissues, accompanied by enhanced activation of IgG-secreting cells, germinal center B cells, memory B cells, as well as CD4+ and CD8+ T cells in antigen-restimulated splenocytes of vaccinated mice. Notably, vaccinated mice exhibited 100% survival and sustained body weight, alongside a marked reduction in cerebral pro-inflammatory cytokines and parasite cyst burden.
    CONCLUSION: GRA7 VLPs confer strong systemic and mucosal immunity and significant protection against chronic toxoplasmosis, underscoring their potential as a promising vaccine platform.
    Keywords:  GRA7; Toxoplasma gondii; immune protection; vaccine; virus-like particles
    DOI:  https://doi.org/10.1080/17435889.2025.2546769
  10. mSphere. 2025 Aug 11. e0023125
      Li-av Segev Zarko studies the nanomachines that apicomplexan parasites deploy to break into host cells. In this mSphere of Influence article, she reflects on how breakthrough cryo-electron microscopy studies published between 2018 and 2021 reshaped her view of what the ever-advancing field of structural biology can reveal about molecular and cellular parasitology.
    Keywords:  apicomplexan parasites; cryo-EM; resolution revolution
    DOI:  https://doi.org/10.1128/msphere.00231-25
  11. Acta Trop. 2025 Aug 11. pii: S0001-706X(25)00251-7. [Epub ahead of print] 107780
      Toxoplasmosis, which is caused by the protozoan parasite Toxoplasma gondii, represents a global health concern for both humans and animals. This study evaluates the immunogenic potential and protective efficacy of a recombinant T. gondii DDX3X protein (rTgDDX3X; gene accession: TGGT1_226250) as a vaccine candidate. A gene fragment encoding residues 25-232 of TgDDX3X was amplified and inserted into the pET30α vector for expression in Escherichia coli BL21 (DE3) cells. The purified recombinant protein (∼30.1 kDa) was validated using SDS-PAGE and immunoblotting, which revealed specific reactivity with sera from T. gondii-infected mice. Antiserum produced in rTgDDX3X-immunized rats selectively recognized native TgDDX3X in tachyzoite lysates, and immunofluorescence analysis localized the protein primarily to the parasite cytoplasm. Vaccination elicited robust T cell activation, with progressive increases in CD4⁺ and CD8⁺ populations over 6 weeks. Elevated titers of anti-rTgDDX3X IgG antibodies were observed, predominantly of the IgG1 isotype (IgG1/IgG2a >1), indicating a Th2-skewed immune response. In challenge models, mice immunized with rTgDDX3X exhibited prolonged survival following infection with the virulent RH strain (mean: 12 days vs. 10 days in controls) and a reduced brain cyst burden after PRU infection (410 vs. 616 cysts/brain). Neutralization assays demonstrated that polyclonal antibodies against rTgDDX3X suppressed T. gondii proliferation In vitro and enhanced survival In vivo. Collectively, these findings indicate that rTgDDX3X induces measurable immune responses and confers partial protection, supporting its potential as a foundational antigen for toxoplasmosis vaccine development.
    Keywords:  DEAD-box; Toxoplasma gondii; immunogenicity; protective efficacy; recombinant subunit vaccine
    DOI:  https://doi.org/10.1016/j.actatropica.2025.107780
  12. Microbiol Spectr. 2025 Aug 13. e0107425
      Toxoplasmosis is caused by infection with Toxoplasma gondii and is one of the most prevalent food-borne parasitic disease worldwide. T. gondii disseminates through the host organism and forms a latency-specific structure called bradyzoite cysts, found primarily in muscle and neuronal cells. In mice, Toxoplasma leads to sustained brain microvascular abnormalities, including capillary rarefaction, microglial activation, and blood-brain barrier (BBB) breakdown, resulting in synaptic and neuronal loss, behavioral and cognitive damages. We hypothesized that cyst-bearing neurons could signal distinct classes of molecules that would orchestrate neurovascular and neuroinflammatory processes. Primary mouse cortical neurons were infected with T. gondii (ME49 strain) tachyzoites, which, 7 days post infection, generated cysts. We determined angiogenic-regulating factors from the neuronal conditioned media (nCM) using a proteome array and found nine molecules, belonging to four main functional clusters: (i) angiogenic signaling (VEGFA); (ii) endothelial-regulating growth factors (IGFBP-2, -3, -9 and PDGF-AA), (iii) chemoattractants (CCL-2, CCL-3, and CXCL12), and (iv) fractalkine signaling (CX3CL1). The main targets were validated in neuronal culture samples and in brain cortices by ELISA, RT-qPCR, or immunoblotting. CX3CL1 secretion was reduced in infected cultures and accumulated on neuronal surface. In vivo, the CX3CL1 receptor (CX3CR1) was upregulated, whereas the CX3CL1 soluble fraction was decreased. Recombinant CX3CL1 decreased arginase-1 and increased iNOS expression in nCM-treated microglial cells, indicating that CX3CL1 polarizes microglia to a pro-resolutive state. Our data suggest that CX3CL1 plays a key role in regulating neuroinflammatory signaling in acquired Toxoplasmosis, highlighting its potential to prevent the neurocognitive damage observed in infected individuals.
    IMPORTANCE: Toxoplasma gondii is a widespread parasite that forms latent cysts in neurons during chronic brain infection. How these infected neurons contribute to long-term brain damage is not well understood. In this study, we used a neuron-specific culture system and a mouse model to show that T. gondii infection alters the release of key signaling molecules by neurons. We found that infected neurons reduce secretion of fractalkine, a molecule that normally helps keep brain immune cells (microglia) in a resting state. At the same time, infected neurons showed increased expression of inflammatory and vascular-related genes, but not always matching increases in protein levels, pointing to complex regulation. These changes may contribute to blood-brain barrier dysfunction and persistent inflammation seen in chronic infection. Our findings highlight the role of neuron-derived signals in driving T. gondii-induced brain pathology and identify fractalkine as a potential target to reduce inflammation.
    Keywords:  Toxoplasma gondii; angiogenesis; blood-brain barrier; fractalkine; neuroinflammation
    DOI:  https://doi.org/10.1128/spectrum.01074-25
  13. R Soc Open Sci. 2025 Aug;12(8): 250159
      Toxoplasma gondii infection has been linked to dampening hosts anti-predator behaviour particularly in laboratory conditions with rodents. Little is known about the role of T. gondii within more complex ecological contexts involving large mammals. Therefore, we aimed to determine the prevalence of T. gondii infection in a population of free-living fallow deer (Dama dama). In addition, we assessed whether there was a link between deer seropositivity and space use where deer may be more likely to be exposed to T. gondii (e.g. closer to human infrastructure). Finally, we determined whether infection with T. gondii was linked to deer risk-taking behaviour. To achieve our goals, we estimated seropositivity and combined it with spatial distribution and behavioural data of individually recognizable deer ranging from those that avoid humans (risk avoiders) to those who beg for food (risk takers). We found T. gondii to be quite widespread in this population with a seropositivity rate of approximately 20%. We found no correlation between T. gondii seropositivity and space use in the park, therefore we were unable to determine how the deer were exposed. We did however find that seropositive deer were also more likely to take risks, opening new avenues to explore T. gondii's dynamics in the wild.
    Keywords:  Dama dama; Toxoplasma gondii; animal behaviour; host manipulation; parasitology; risk taking; serology; toxoplasmosis
    DOI:  https://doi.org/10.1098/rsos.250159
  14. Acc Chem Res. 2025 Aug 13.
      ConspectusProtein acetylation is a pervasive and reversible post-translational modification (PTM) that impacts various protein features including stability, localization, and interactions and regulates diverse cellular functions, including transcription, signal transduction, and metabolism. This process is orchestrated by "writer" lysine acetyltransferases (KATs) and "eraser" deacetylases (KDACs), and its dysregulation is implicated in a broad spectrum of diseases including cancer, metabolic syndromes, and immune disorders. However, dissecting the roles of specific acetylation events in live cells remains a challenge due to the lack of tools that enable precise, rapid, and reversible acetylation at defined protein sites.To begin addressing these challenges, we recently developed AceTAG (acetylation tagging), a chemically induced proximity (CIP) platform for targeted protein acetylation in live cells. AceTAG molecules are heterobifunctional ligands that recruit endogenous KATs─such as p300/CBP or PCAF/GCN5─to a tagged protein of interest, enabling selective, tunable, and dynamic acetylation. We demonstrated the utility of AceTAG across diverse proteins, including histone H3.3, p65/RelA, and p53. We further show that chemically induced acetylation of p53, including multiple hotspot p53 mutants, leads to enhanced stability and transcriptional activation, underscoring the potential of AceTAG for functional investigations and the potential for therapeutic exploration.In this Account, we provide an overview of protein acetylation and survey chemical biology technologies for its manipulation, with a focus on AceTAG. We describe the conceptual motivation of AceTAG, applications, technical considerations, and recent efforts to expand this concept to endogenous proteins. Finally, we offer a forward-looking perspective of targeted acetylation as a chemical tool to investigate the biology of this PTM, as well as its potential as a therapeutic modality.
    DOI:  https://doi.org/10.1021/acs.accounts.5c00326
  15. Science. 2025 Aug 14. 389(6761): eadr6326
      As major consumers of cellular metabolites, mitochondria are poised to compete with invading microbes for the nutrients that they need to grow. Whether cells exploit mitochondrial metabolism to protect from infection is unclear. In this work, we found that the activating transcription factor 4 (ATF4) activates a mitochondrial defense based on the essential B vitamin folate. During infection of cultured mammalian cells with the intracellular pathogen Toxoplasma gondii, ATF4 increased mitochondrial DNA levels by driving the one-carbon metabolism processes that use folate in mitochondria. Triggered by host detection of mitochondrial stress induced by parasite effectors, ATF4 limited Toxoplasma access to folates required for deoxythymidine monophosphate synthesis, thereby restricting parasite growth. Thus, ATF4 rewires mitochondrial metabolism to mount a folate-based metabolic defense against Toxoplasma.
    DOI:  https://doi.org/10.1126/science.adr6326
  16. bioRxiv. 2025 Jul 14. pii: 2025.07.14.664716. [Epub ahead of print]
      SIRT5, one of the human sirtuins, catalyzes the removal of acyl substitutions from lysine residues in a NAD + -dependent manner. In addition to the deacetylase activity, SIRT5 also demonstrates strong desuccinylase, demalonylase, and deglutarylase activity. Through deacylating a broad spectrum of cellular proteins and enzymes, SIRT5 is heavily involved in the regulation of energy metabolism, reactive oxygen species (ROS) reduction, and ammonia detoxification. Accumulating evidence also suggest SIRT5 as a potential therapeutic target for the treatment of neurodegenerative diseases, metabolic disorders, and cancer. In the current study, we report the identification and characterization a SIRT5 modulator, reduced nicotinic acid riboside (NARH). It shows differential regulation of the distinct activities of SIRT5: activates desuccinylation, but mildly suppresses deacetylation. NARH binds to SIRT5 in the absence of NAD + , and demonstrates cellular target engagement and activity. The potential NARH binding site is further investigated using a suite of biochemical and computational approaches. The current study provides greatly-needed mechanistic understanding of SIRT5 regulation, as well as a novel chemical scaffold for further activator development.
    DOI:  https://doi.org/10.1101/2025.07.14.664716
  17. Cardiovasc Toxicol. 2025 Aug 11.
      Cardiac fibrosis is a pathological condition marked by the excessive accumulation of extracellular matrix (ECM) components, which leads to impaired cardiac function and heart failure. Despite its significant contribution to cardiovascular morbidity and mortality, no effective therapeutic drugs specifically target the inhibition of cardiac fibrosis, largely due to the complex etiological heterogeneity and pathogenesis of this disease. Sirtuins (SIRTs), a family of NAD + -dependent deacetylases, play a critical role in cellular processes such as oxidative stress, inflammation, energy metabolism, mitochondrial function, epithelial-to-mesenchymal transition (EMT), and ECM homeostasis, all of which are implicated in cardiac fibrosis. Growing clinical and experimental evidence suggests that SIRTs regulate the cellular and molecular mechanisms of cardiomyocytes through various biological pathways. Emerging evidence indicates that sirtuin activators, including resveratrol and NAD + precursors, hold therapeutic potential in mitigating cardiac fibrosis. However, the complex and context-dependent roles of sirtuins necessitate further research to fully elucidate their mechanisms and translational applications. As the role of SIRTs in relation to cardiac fibrosis and its associated mechanisms is rarely discussed in the literature, this review comprehensively addresses the roles of the seven mammalian sirtuins (SIRT1-SIRT7) in the pathogenesis and progression of cardiac fibrosis. It highlights the key role of SIRTs as molecular targets for innovative anti-fibrotic therapies, offering new avenues for the treatment of cardiac fibrosis and associated cardiovascular diseases.
    Keywords:  Cardiac fibrosis; Extracellular matrix; Myofibroblasts; Oxidative stress; Sirtuins
    DOI:  https://doi.org/10.1007/s12012-025-10052-0
  18. Cell Rep. 2025 Aug 12. pii: S2211-1247(25)00918-0. [Epub ahead of print]44(8): 116147
      Mitochondria-driven histone lysine succinylation is emerging as a critical signaling system that links cellular metabolism to the pathogenesis of diseases, including cancer. Here, we report that a global increase in protein/histone succinylation is associated with mitochondrial tricarboxylic acid cycle defects in acute myeloid leukemia (AML). Depletion of the succinyl-coenzyme A (CoA) synthetase alpha subunit SUCLG1 causes protein/histone hypersuccinylation in leukemia cells, which impairs cell proliferation and leukemia progression in xenograft models. Mechanistically, increased histone succinylation, which could compete with acetylation, attenuates the interaction of the bromodomain-containing protein 4 (BRD4) bromodomain with chromatin, hence disrupting BRD4-mediated leukemogenic gene transcription and restoring BRD4-dependent fine-tuned gene regulatory circuits. Our study uncovers the crucial role of metabolism-controlled histone succinylation in cancer development and highlights it as an innovative therapeutic approach.
    Keywords:  BRD4; CP: Cancer; CP: Metabolism; SUCLG1; acute myeloid leukemia; histone succinylation
    DOI:  https://doi.org/10.1016/j.celrep.2025.116147
  19. bioRxiv. 2025 Jul 15. pii: 2025.07.15.665002. [Epub ahead of print]
      Malate dehydrogenase (MDH: EC:1.1.1.37) catalyzes a key NAD + -dependent redox reaction integral to cellular metabolism. In humans, the cytosolic (hMDH1) and mitochondrial (hMDH2) isoforms operate in distinct compartments, suggesting potential differences in regulation. Here, we present a comparative analysis of hMDH1 and hMDH2 under physiologically relevant conditions, integrating enzymatic assays, ligand binding studies, small-angle X-ray scattering (SAXS), and molecular modeling. Our findings reveal that hMDH2 activity is inhibited by α-ketoglutarate, glutamate, NAD + , ATP, and citrate at concentrations consistent with mitochondrial metabolic states characterized by elevated amino acid catabolism or redox stress. Conversely, hMDH1 exhibits minimal impact by these metabolites, with only modest inhibition observed in the presence of ATP and ADP. SAXS analyses confirm that both isoforms maintain stable dimeric structures upon ligand binding, indicating that regulation is not mediated by global conformational changes. Structural modeling and normal mode analyses identify increased flexibility in hMDH1, particularly within the active site loop, thumb loop, and a partially disordered C-terminal helix. In contrast, hMDH2 displays a more rigid architecture and a more electropositive active site environment, correlating with its heightened sensitivity to anionic metabolites. Fluorescence quenching experiments further support these distinctions, demonstrating stronger binding affinities for nucleotide-based ligands in hMDH2 compared to hMDH1. Collectively, these results suggest that isoform-specific regulation of human MDH arises from differences in local structural dynamics and electrostatics, rather than large-scale structural rearrangements. hMDH2 appears adapted to integrate mitochondrial metabolic signals, modulating malate oxidation in response to cellular conditions, while hMDH1 maintains consistent cytosolic function across diverse metabolic states.
    DOI:  https://doi.org/10.1101/2025.07.15.665002
  20. Life Med. 2025 Aug;4(4): lnaf019
      Mitochondrial dysfunction is a hallmark of aging, characterized by a decline in mitochondrial biogenesis and quality control, compromised membrane integrity, elevated ROS production, damaged mitochondrial DNA (mtDNA), impaired mitochondrial-nuclear crosstalk, and deregulated metabolic balance. Among the key longevity regulators, sirtuin family members SIRT3, SIRT4, and SIRT5 are predominantly localized to mitochondria and play crucial roles in maintaining mitochondrial function and homeostasis. This review explores how mitochondrial sirtuins mitigate aging-related mitochondrial dysfunctions and their broader implications in aging-related diseases. By elucidating the intricate interplay between mitochondrial dysfunction and mitochondrial sirtuins, we aim to provide insights into therapeutic strategies for promoting healthy aging and combating age-related pathologies.
    Keywords:  aging; mitochondrial dysfunction; mitochondrial sirtuins
    DOI:  https://doi.org/10.1093/lifemedi/lnaf019
  21. bioRxiv. 2025 Jul 14. pii: 2025.07.14.664770. [Epub ahead of print]
      Heme is an essential molecule for most organisms, yet some parasites, like Trypanosoma cruzi , the causative agent of Chagas disease, cannot synthesize it. These parasites must acquire heme from their hosts, making this process critical for their survival. In the midgut of the insect vector, T. cruzi epimastigotes are exposed to both hemoglobin (Hb) and free heme resulting from its degradation. Despite the importance of this nutrient, how different heme sources influence parasite gene expression remains poorly understood. Here, we showed that heme restitution either as hemin or Hb to heme-starved parasites induces an early and distinct transcriptional response in T. cruzi epimastigotes. Using RNA sequencing at 4- and 24-hours post-supplementation, we identified gene subsets commonly or uniquely regulated by each heme source, including genes putatively linked to heme acquisition and metabolism. We also presented here the first studies focused on CRAL/TRIO domain-containing protein ( Tc CRAL/TRIO), a novel heme responsive hemoprotein identified from this study. Our results provide a more detailed picture of T. cruzi biology and highlights heme acquisition as a promising point of vulnerability. These findings may ultimately contribute to the identification of potential molecular targets for the development of new therapeutic strategies against Chagas disease.
    DOI:  https://doi.org/10.1101/2025.07.14.664770
  22. FEBS Lett. 2025 Aug 13.
      The pyruvate dehydrogenase complex (PDHc) is a crucial metabolic enzyme complex found in all aerobic organisms. It catalyzes the conversion of pyruvate, the product of glycolysis, into acetyl-CoA, a key substrate for the citric acid cycle and fatty acid synthesis. This multienzyme complex uses multiple cosubstrates and tethered reaction intermediates to efficiently channel substrates through its catalytic steps. With a total size of 5-12 MDa, PDHc is among the largest biomolecular assemblies. It consists of three enzymatic components acting sequentially: E1 (pyruvate dehydrogenase), E2 (dihydrolipoamide acetyltransferase), and E3 (dihydrolipoamide dehydrogenase). In eukaryotes, an additional E3-binding protein (E3BP) recruits E3 to the complex. E2 (and E3BP) subunits form the structural core, typically exhibiting octahedral or icosahedral symmetry, while E1 and E3 bind to the core as peripheral subunits. Advances in structural biology, particularly cryo-EM, X-ray crystallography, and nuclear magnetic resonance (NMR), have provided valuable insights into PDHc organization, assembly principles, and species-specific variation. Here, we review diverse PDHc architectures across phylogenetic groups. Understanding these structural and functional adaptations is essential for fully deciphering PDHc regulation and its role in metabolism.
    Keywords:  PDHc; X‐ray crystallography; cryo‐EM; metabolism; multienzyme; polyhedral symmetry; pyruvate dehydrogenase complex; stoichiometry; structural biology
    DOI:  https://doi.org/10.1002/1873-3468.70140
  23. J Chem Inf Model. 2025 Aug 11. 65(15): 8229-8237
      AlphaFold has proven to be a valuable tool for predicting protein structures with unprecedented speed and accuracy. Extensive research from multiple groups has demonstrated that manipulating the multiple sequence alignment used for structure prediction can enhance AlphaFold2's ability to explore protein conformational landscapes, yielding reliable models of proteins capable of switching between alternative conformations. The release of the thoroughly reengineered AlphaFold3, which promises even greater prediction accuracy and efficiency, raises the question of whether such alternative conformational states can be modeled-either natively or by tuning the multiple sequence alignment used for prediction. In this work, we use a family of green fluorescent proteins engineered through alternate frame folding to assess AlphaFold3's prediction accuracy and uncover an unexpected role of disordered regions in driving the conformational preferences of the models.
    DOI:  https://doi.org/10.1021/acs.jcim.5c00906
  24. Mol Pharmacol. 2025 Jul 17. pii: S0026-895X(25)15322-4. [Epub ahead of print]107(8): 100062
      The development of isoform-selective histone deacetylase (HDAC) inhibitors offers a promising approach to minimize the adverse effects of nonselective HDAC inhibitors. HDAC6, due to its unique structural and functional properties, regulates critical cellular processes like gene expression, proliferation, senescence, and apoptosis. Inspired by a tryptoline-derived natural product, callophycin A, a series of compounds were synthesized and evaluated for HDAC6 selectivity. In the HDAC enzyme assay, compound 6a stood out as the lead, demonstrating 21-fold higher potency against HDAC6 compared with HDAC1 (HDAC6 IC50 = 83.6 ± 1.1 nM vs HDAC1 IC50 = 1790 ± 1.0 nM). In dose-dependent western blot experiments using H1975 lung cancer cells, a lower concentration of compound 6a (3 μM) induced significantly greater acetylation of α-tubulin compared with histone H3, indicating preferential inhibition of cytoplasmic HDAC6 over the nuclear HDAC1 isoform. Molecular docking of compound 6a at the HDAC6 active site (PDB code: 5EDU) revealed key interactions including π-alkyl contacts via the cap group, π-π stacking through the linker, hydrogen bonding involving the zinc-binding group, and Zn2+ chelation by the hydroxamic acid moiety that support its strong and selective binding, consistent with its HDAC6 inhibitory profile. Overall, compound 6a represents a promising prototype for the rational design of selective HDAC6 inhibitors, offering a structural framework for developing safer and more effective therapeutics aimed at HDAC6-driven cancers, thereby advancing targeted drug development in oncology. SIGNIFICANCE STATEMENT: Selective histone deacetylase 6 (HDAC6) inhibitors provide a safer alternative to nonselective HDAC inhibitors, with potential applications in cancer. This study identifies compound 6a as a promising lead with remarkable HDAC6 specificity, offering a foundation for developing targeted and efficient therapeutics.
    Keywords:  Anticancer drugs; Epigenetics; Histone deacetylase inhibitor; Tryptoline
    DOI:  https://doi.org/10.1016/j.molpha.2025.100062