bims-pideca Biomed News
on Class IA PI3K signalling in development and cancer
Issue of 2026–01–25
sixteen papers selected by
Ralitsa Radostinova Madsen, MRC-PPU



  1. bioRxiv. 2025 Dec 06. pii: 2025.12.03.691507. [Epub ahead of print]
      Post-zygotic gain-of-function PIK3CA mutations arising during embryonic development cause disorders collectively known as the PIK3CA -related overgrowth spectrum (PROS). This ranges from minor, localized overgrowth to devastating multi-tissue overgrowth. Disease severity is widely attributed to a combination of PIK3CA genotype, affected cell type, and developmental timing of mutation acquisition. However, in PROS this explains neither the biased pattern of overgrowth - disproportionately affecting mesoderm and neuroectoderm- derived tissues - nor the typical low mutation burden within areas of extensive tissue overgrowth. Indeed, growing evidence suggests PROS mutations cause overgrowth non-cell- autonomously, although mechanisms of this are poorly understood. Here, we develop mosaic zebrafish models of PROS with overexpression of orthologous hotspot pik3ca mutations ( pik3ca PROS ) to visualize and examine the effects of mutated cells on early development, in whole live animals. Reminiscent of PROS, we observe a spectrum of embryonic vasculature malformations (VMs), accompanied by larval muscle and bone overgrowth. Surprisingly, VMs only rarely expressed pik3ca PROS in constituent endothelial cells, with pik3ca PROS -expressing cells often closely abutting malformations instead. Single-cell transcriptomics of pik3ca PROS mosaic zebrafish prior to VM onset revealed that most pik3ca PROS cells are relatively immature and developmentally inert or constitute a small minority of mesodermal-derived cell types. Despite this constriction, global changes to cell fate were evident, alongside pervasive, pan- lineage abnormalities of gene expression, and rewiring of predicted ligand-receptor communication between lineages. We propose that targeting signals that indirectly propagate overgrowth through non-cell autonomous mechanisms - as well as PI3K activation itself - is worthy of therapeutic investigation.
    Significance statement: Patchy, or mosaic, activating mutations in PIK3CA cause asymmetric human overgrowth due to aberrant hyperactivation of phosphoinositide 3-kinase (PI3K) signaling. Overgrowth prominently affects blood vessels and may be severely debilitating. While causation by PIK3CA mutations is clear, the explanation for the extent and pattern of associated overgrowth is not. Leveraging the power of zebrafish models for observation of early development, we now provide evidence for widely pervasive developmental effects of PIK3CA mutations extending beyond transcriptionally and phenotypically affected cells and lineages. This suggests potential therapeutic value of targeting secondary effects of PIK3CA activation as well as the activated PI3K itself.
    DOI:  https://doi.org/10.64898/2025.12.03.691507
  2. Cell Commun Signal. 2026 Jan 20.
      The mechanistic target of rapamycin complex 1 (mTORC1) is a central driver of cell growth that is frequently hyperactivated in cancer. While mTORC1 is activated at the lysosomal surface in response to growth factors and amino acids, the processes governing its inactivation are not fully understood. Here, we report that sustained mTORC1 suppression during leucine or arginine starvation requires the translocation of peripheral lysosomes to the perinuclear region. Our data suggest that a pool of mTOR remains active at peripheral lysosomes during starvation, and that increased spatial separation between lysosomes and the plasma membrane attenuates PI3K/Akt signaling-thereby reducing inputs that otherwise maintain mTORC1 activity. Consequently, preventing lysosome translocation and increasing peripheral lysosome levels sustains mTORC1 signaling during prolonged starvation in a PI3K/Akt-dependent manner independently of autophagy. Under these conditions, mTORC1 signaling persists even when lysosomal catabolism is perturbed by chloroquine or concanamycin A. Collectively, these data indicate that the peripheral lysosome pool, even when catabolically impaired, can sustain mTORC1 signaling under nutrient scarcity, by modulating PI3K/Akt signaling input to the pathway. These observations identify peripheral lysosome levels as a critical determinant of mTORC1 inactivation during nutrient stress and may have implications for diseases with aberrant mTORC1 signaling, including cancer.
    Keywords:  Amino acid deprivation; Catabolically impaired lysosomes; Lysosome positioning; MTORC1; PI3K-Akt signaling; Rab7; Rap1
    DOI:  https://doi.org/10.1186/s12964-026-02659-9
  3. ACS Synth Biol. 2026 Jan 19.
      Cancer is known to be a disease of altered cellular signaling; however, the relationship between mutation-specific changes to signal transduction and the phenotypic consequences produced remains poorly understood. Here, we investigate two common breast cancer driver mutations, the PIK3CAH1047R mutation and the ErbB2 amplification, both of which activate the PI3K-Akt pathway but paradoxically drive distinct cellular outcomes. Indeed, in nontransformed mammary epithelial cells, PI3KH1047R expression induced features of epithelial-mesenchymal transition (EMT), while ErbB2amp cells exhibited a hyperproliferative phenotype. Characterization of PI3K axis signaling revealed that ErbB2amp cells display prolonged, stimulus-dependent PI3K activation, whereas PI3KH1047R cells show constitutive, ligand-independent signaling. To test whether these distinct dynamics contribute to the phenotypic responses, we employed an iLID-based optogenetic system that enables precise, tunable control of endogenous PI3K activity. Using this tool to mimic the mutation-specific dynamics in MCF10A mammary epithelial cells, we found that PI3K signaling patterns alone were sufficient to reproduce key features of the PIK3CA H1047R-associated EMT phenotype but not the ErbB2-associated proliferative phenotype. These findings suggest that the temporal encoding of pathway activity, not merely its magnitude, can drive some phenotypic changes in oncogenic progression, explain how distinct mutations within a common signaling pathway can produce divergent cellular phenotypes, and provide a workflow for interrogating the functional consequences of changes in signaling dynamics.
    Keywords:  EMT; PI3K-signaling; breast cancer; optogenetics; signaling dynamics; temporal dynamics
    DOI:  https://doi.org/10.1021/acssynbio.5c00651
  4. Brain. 2026 Jan 19. pii: awag017. [Epub ahead of print]
      Cerebral cavernous malformations are common vascular anomalies in the central nervous system that predispose individuals to seizures and hemorrhagic stroke. Familial forms are linked to germline loss-of-function mutations in CCM1-3, and sporadic lesions frequently harbor somatic gain-of-function mutations in MAP3K3 and PIK3CA. However, the mechanisms by which these somatic mutations drive lesion development remain incompletely understood, and no medical therapies are currently available. Here, we investigated the cooperative effects of MAP3K3I441M and PIK3CAH1047R mutations using transgenic neonatal and adult mouse model, supported by histology, micro-CT, bulk and single-cell RNA sequencing, and human cerebral cavernous malformations samples. MAP3K3 I441M activated inflammatory and angiogenic transcriptional programs in brain endothelial cells, whereas PIK3CAH1047R enhanced cell cycle and DNA replication pathways. Notably, MAP3K3I441M and PIK3CAH1047R double mutations synergistically amplified PI3K-AKT-mTOR signaling, inducing an "angiogenic switch" reminiscent of tumor neovascularization. This interaction promoted endothelial angiogenesis and lesion development in mouse brains. Transcriptomic analyses of human cerebral cavernous malformations confirmed enrichment of angiogenesis-related gene signatures in double mutations-related lesions. Treatment with the PI3Kα-selective inhibitor alpelisib suppressed lesion formation and reversed pro-angiogenic signaling in both mouse models and patient-derived cerebral cavernous malformations organoids. These findings uncover a convergent mechanism involving MAPK and PI3K pathway activation in cerebral cavernous malformations pathogenesis and demonstrate that PI3Kα inhibition may offer a viable therapeutic strategy for a disease that currently lacks effective pharmacological treatment.
    Keywords:  PI3K pathway activation; endothelial cell remodeling; organoid disease models; somatic mutations; targeted therapy; vascular malformations
    DOI:  https://doi.org/10.1093/brain/awag017
  5. Elife. 2026 Jan 21. pii: RP107794. [Epub ahead of print]14
      Cells process dynamic signaling inputs to regulate fate decisions during development. While oscillations or waves in key developmental pathways, such as Wnt, have been widely observed, the principles governing how cells decode these signals remain unclear. By leveraging optogenetic control of the Wnt signaling pathway in both HEK293T cells and H9 human embryonic stem cells, we systematically map the relationship between signal frequency and downstream pathway activation. We find that cells exhibit a minimal response to Wnt at certain frequencies, a behavior we term anti-resonance. We developed both detailed biochemical and simplified hidden variable models that explain how anti-resonance emerges from the interplay between fast and slow pathway dynamics. Remarkably, we find that frequency directly influences cell fate decisions involved in human gastrulation; signals delivered at anti-resonant frequencies result in dramatically reduced mesoderm differentiation. Our work reveals a previously unknown mechanism of how cells decode dynamic signals and how anti-resonance may filter against spurious activation. These findings establish new insights into how cells decode dynamic signals with implications for tissue engineering, regenerative medicine, and cancer biology.
    Keywords:  HEK 293T; Wnt; computational biology; developmental biology; hESC; human; mesoderm; systems biology
    DOI:  https://doi.org/10.7554/eLife.107794
  6. Commun Biol. 2026 Jan 19.
      Phosphoinositide-3 kinase (PI3K) is a central regulator of cellular metabolism and survival, and its dysregulation is implicated in major human diseases, particularly cancer. The p85 regulatory subunit of PI3K uses its C-terminal domains to stabilise the catalytic p110 subunit in an inhibited state. Certain Src homology 3 (SH3) domains activate p110 by binding to the proline-rich (PR) 1 motif at the N-terminus of p85. How this interaction leads to PI3K activation remains unclear. Moreover, the low specificity of SH3 domains raises the question about how they can selectively control PI3K activation. Combining structural, biophysical, and functional methods, we demonstrate that both questions are linked: PI3K-activating SH3 domains form additional 'tertiary' interactions with the C-terminal domains of p85, relieving p110 inhibition. SH3 domains lacking these tertiary contacts may bind p85 with similar affinity but fail to activate PI3K. Thus, p85 employs a selection mechanism that discriminates based on binding mode rather than binding strength, preventing nonspecific activation rather than nonspecific binding. This mechanism conveys a functional selectivity to SH3 domains that are otherwise considered promiscuous. These insights establish a mechanistic framework that will help to predict, modulate, and therapeutically target SH3-driven PI3K activation in disease.
    DOI:  https://doi.org/10.1038/s42003-026-09540-y
  7. EMBO Rep. 2026 Jan 20.
      Mechanistic target of rapamycin complex 1 (mTORC1) integrates signals from nutrients, growth factors, and cellular stress to regulate biosynthesis and maintain homeostasis. Dysregulated mTORC1 disrupts stem cell homeostasis and impairs cell fate transitions in vivo and in vitro. Previous studies have shown that mTORC1 hyperactivation promotes nuclear translocation of TFE3, blocking pluripotency exit in both mouse and human naïve embryonic stem cells. Similarly, our earlier work has demonstrated that sustained mTORC1 activation impedes somatic cell reprogramming via the transcriptional coactivator PGC1α. This raises the question of how mTORC1 coordinates gene transcription across distinct transitions in pluripotent cells. Here, we show that TFE3 mediates the transcriptional blockade induced by mTORC1 hyperactivation during reprogramming. Notably, during both pluripotency exit and reprogramming, TFE3 recruits the NuRD corepressor complex to repress genes essential for cell fate transitions. These findings uncover a shared mechanism by which mTORC1 and TFE3 regulate stem cell identity, highlighting the dual regulatory role of TFE3 and its potential implications in development, aging, and tumorigenesis.
    Keywords:  NuRD Complex; Pluripotency Exit; Somatic Cell Reprogramming; TFE3; mTORC1
    DOI:  https://doi.org/10.1038/s44319-025-00544-z
  8. Mol Syst Biol. 2026 Jan 19.
      Oncogenic mutations shape colorectal cancer (CRC) biology, yet their impact on transcriptional phenotypes remains incompletely understood, and their individual prognostic value is limited. Here, we perform a pooled single-cell transcriptomic screen of over 100,000 CRC cells with a comprehensive barcoded library of oncogenic variants across genetically diverse CRC lines. Using a variational autoencoder-based interpretable factor model, we identify ten conserved oncogene-driven transcriptional modules (TMOs) representing core cancer phenotypes such as cellular plasticity, inflammatory response, replicative stress, and epithelial-to-mesenchymal transition. Engagement of these modules can be context-dependent, reflecting interactions between oncogene-induced driver pathways and background genetics. TMO activity in patient tumors stratifies CRC cohorts into high- and low-risk groups, improving relapse-free survival prediction beyond existing classification systems. Our study systematically links oncogenic signaling to transcriptional states and clinical outcomes, establishing a functional framework for module-based patient stratification in precision oncology.
    Keywords:  Colorectal Cancer; Oncogenes; Signatures; Single Cell Screening; Transcriptional Modules
    DOI:  https://doi.org/10.1038/s44320-025-00186-2
  9. Lymphat Res Biol. 2026 Jan 23. 15578585251391569
       BACKGROUND: Vascular anomalies are a group of common endothelial disorders that manifest a wide range of overlapping phenotypes, which complicate diagnosis. Next-generation sequencing (NGS) has led to the ability to detect low-frequency somatic variants, which may aid in the correct diagnosis and treatment of patients. Our goal was to identify the pathogenic variants in affected tissue taken from a cohort of 58 unrelated patients with various clinically diagnosed vascular anomalies.
    METHODS: DNA was extracted from fresh/frozen affected tissue samples and evaluated using a custom 735 vascular anomaly/cancer gene NGS panel down to 1% somatic mosaicism.
    RESULTS: Pathogenic or likely pathogenic variants were identified in 47% (27/58) of vascular anomaly tissue biopsies, including 61.5% (16/26) of lymphatic malformation (LM), 15% (3/20) of hemangioma (congenital and infantile), and 67% (8/12) of other various vascular anomalies. Two novel variants, PIK3CA c.3205_3206insTTTT (p.*1069Pheext*4) and PIK3R1 c.1384_1395del (p.Glu462_Arg465del), were identified in LM tissue. In addition, we report a likely pathogenic variant GNA14 c.512C>T (p.Thr171Ile) identified in a GLUT-1 positive infantile hemangioma lesion. The majority (52%) of the negative results were in infantile hemangioma tissue, for which a genetic cause has not yet been established.
    CONCLUSIONS: The 735 gene vascular anomaly/cancer NGS panel is an effective way to detect low levels of somatic mosaicism in these lesions. Given the challenge that many vascular anomalies present to diagnose, genetic testing is an invaluable tool for clinicians to utilize in the process of diagnosis and determining treatment.
    Keywords:  GNA14; PIK3CA; PIK3R1; hemangioma; lymphatic malformation; next-generation sequencing; vascular anomalies
    DOI:  https://doi.org/10.1177/15578585251391569
  10. Nat Commun. 2026 Jan 20. 17(1): 614
      UFMylation, a ubiquitin-like modification, is crucial for cellular processes and is linked to human diseases, including cancer. However, its role in cancer remains unclear. Here, we report that UFL1 promotes breast tumor growth by remodeling lipid metabolism. Mechanistically, UFL1 interacts with and UFMylates AKT, enhancing its localization at the endoplasmic reticulum and phosphorylation by PDK1 and mTORC2, thereby increasing AKT-mediated lipid synthesis. Moreover, AKT phosphorylates UFL1, boosting its activity. Thus, UFL1 and AKT form a positive feedback loop, accelerating lipid synthesis and breast tumor growth. Clinically, UFL1 levels are increased in human breast tumors and are associated with poor clinical outcomes in breast cancer patients. Importantly, UFMylation inhibitors sensitize breast cancer cells to AKT inhibitors and anticancer drugs. Our findings reveal a critical role for UFMylation in lipid metabolism and identify the UFL1-AKT axis as a potential therapeutic target in breast cancer.
    DOI:  https://doi.org/10.1038/s41467-026-68492-3
  11. Nature. 2026 Jan 21.
      Plasticity-the ability of cells to undergo phenotypic transitions-drives cancer progression and therapy resistance1-3. Recent studies have suggested that plasticity in solid tumours is concentrated in a minority subset of cancer cells4-6, yet functional studies examining this high-plasticity cell state (HPCS) in situ are lacking. Here we develop mouse models enabling the detection, longitudinal lineage tracing and ablation of the HPCS in autochthonous lung tumours in vivo. Lineage tracing reveals that the HPCS cells possess a high capacity for cell state transitions, giving rise to both early neoplastic (differentiated) and progressed lung cancer cell states in situ. Longitudinal lineage tracing using secreted luciferases reveals that HPCS-derived cells have a high capacity for growth compared with bulk cancer cells or another cancer cell state with features of differentiated lung epithelium. Ablation of HPCS cells in early neoplasias abrogates benign-to-malignant transition, whereas ablation in established tumours by suicide gene or chimeric antigen receptor (CAR) T cells robustly reduces tumour burden. We further demonstrate that the HPCS gives rise to therapy-resistant cell states, whereas HPCS ablation suppresses resistance to chemotherapy and oncoprotein-targeted therapy. Notably, an HPCS-like state is ubiquitous in regenerating epithelia and in carcinomas of multiple other tissues, revealing a convergence of plasticity programs. Our work establishes the HPCS as a critical hub enabling reciprocal transitions between cancer cell states. Targeting the HPCS in lung cancer and in other carcinomas may suppress cancer progression and eradicate treatment resistance.
    DOI:  https://doi.org/10.1038/s41586-025-09985-x
  12. bioRxiv. 2025 Dec 03. pii: 2025.12.01.691331. [Epub ahead of print]
       Background and aims: Hepatic insulin action is essential for whole body glucose homeostasis. Insulin's inhibition of glycogen breakdown, suppression of gluconeogenesis, and activation of glycogen synthesis are critical for postprandial glucose disposal. AKT, a serine-threonine kinase and well-established insulin signaling target, regulates hepatic glucose metabolism through transcriptional and posttranslational mechanisms. However, current knowledge about AKT's regulation of hepatic glucose metabolism largely stems from genetic loss of function models, precluding observation of rapid, transcription-independent effects.
    Methods: Stable isotope tracing using [U- 13 C]-glucose was coupled with pharmacological inhibition of AKT using MK-2206 in primary rat hepatocytes. Bulk metabolomics was performed on AKT knockout livers and primary rat hepatocytes treated with MK-2206. Radiolabeled glucose was used to quantify short-term changes to glycogen synthesis.
    Results: MK-2206 treatment decreased glucose contribution to glucose 6-phosphate and uridine diphosphate glucose within minutes without significantly affecting total metabolite pool sizes or changes to glucokinase protein levels. This was accompanied by a decrease in glucose contribution to glycogen, independent of changes to glycogen breakdown or glycogen synthase phosphorylation.
    Conclusions: Together, these results demonstrate that AKT acutely regulates glucose contribution to glycogen and its upstream precursors, suggesting a transcription-independent, glucokinase-centered mechanism for glycogen synthesis through the direct pathway.
    DOI:  https://doi.org/10.64898/2025.12.01.691331
  13. Mol Oncol. 2026 Jan 20.
      PIK3R1, a regulatory subunit of class IA phosphoinositide-3-kinase (PI3K), undergoes alternative splicing to generate multiple isoforms, primarily p85α and p55α. The canonical isoform p85α associates with the catalytic subunit p110α to form the active PI3K complex, which regulates key cellular functions such as growth, proliferation, survival, and metabolism. In this study, we performed a comprehensive pan-cancer analysis integrating transcriptomic, proteomic, and genomic data to investigate the expression patterns of p85α and its splicing variant, p55α, and their associations with clinical outcomes. Our findings reveal that while p85α expression is significantly reduced, p55α is elevated in tumors as compared to normal samples. These alterations are linked to poor prognosis across multiple cancer types. Notably, we observed racial disparities in expression patterns, with African American patients exhibiting more pronounced downregulation of p85α and upregulation of p55α than European Americans, potentially contributing to differential clinical outcomes. This is the first study to systematically evaluate p85α and p55α expression across diverse cancers and populations, highlighting the role of alternative splicing in PI3K pathway dysregulation and its relevance to cancer progression and health disparities.
    Keywords:  PIK3R1; cancer; p55α; p85α; race; splicing variant
    DOI:  https://doi.org/10.1002/1878-0261.70205
  14. Nat Genet. 2026 Jan 20.
      Spatial transcriptomics aims to elucidate how cells coordinate within tissues by connecting cellular states to their native microenvironments. Imaging-based assays are especially promising, capturing molecular and cellular features at subcellular resolution in three dimensions. Interpretation of such data, however, hinges on accurate cell segmentation. Assigning individual molecules to the correct cells remains challenging. Here we re-analyze data from multiple tissues and platforms to find that segmentation errors currently confound most downstream analysis of cellular state, including differential expression, neighbor influence and ligand-receptor interactions. The extent to which misassigned molecules impact the results can be striking, frequently dominating the results. Thus, we show that matrix factorization of local molecular neighborhoods can effectively identify and isolate such molecular admixtures, thereby reducing their impact on downstream analyses, in a manner analogous to doublet filtering in single-cell RNA sequencing. As the applications of spatial transcriptomics assays become more widespread, accounting for segmentation errors will be important for resolving molecular mechanisms of tissue biology.
    DOI:  https://doi.org/10.1038/s41588-025-02497-4
  15. Nat Commun. 2026 Jan 20. 17(1): 613
      Triple-negative breast cancer (TNBC) is an aggressive and highly lethal disease with limited therapies. While UFL1-mediated UFMylation has been implicated in various diseases, its role in TNBC remains not fully understood. Here, we demonstrate that AKT1 directly interacts with UFL1 and undergoes UFMylation at Lys189/276/297. This modification enhances AKT phosphorylation and activation, promoting tumor growth and chemoresistance in TNBC. In turn, AKT phosphorylates UFL1 at Thr426, establishing a positive feedback loop that sustains high activity of both pro-oncogenic regulators in TNBC. Disrupting the UFL1-AKT interaction using the specific peptide PDAU-TAT significantly inhibits TNBC progression both in vitro and in vivo. Clinically, elevated pT426 UFL1 correlates with high pAKT in TNBC specimens. These findings uncover a crucial UFL1-AKT positive feedback loop that drives TNBC progression and suggest that targeting this axis could offer a promising therapeutic strategy for TNBC and potentially other aggressive cancers characterized by upregulated UFL1 and AKT activation.
    DOI:  https://doi.org/10.1038/s41467-026-68493-2
  16. iScience. 2026 Jan 16. 29(1): 114548
      The vasculature is essential for tissue function and pathology. Spheroid co-cultures of endothelial and marrow/mesenchymal stromal/stem cells (MSCs) form consistent structures, but the vascular components are short-lived. iPSC-derived vascular organoids can establish complex vasculature but often have variable cell maturation and low reproducibility. This article presents consistently formed, free-floating, long-term vascularized mesenchymal organoids (VMOs), by co-culturing human umbilical vein endothelial cells (HUVECs) and MSCs in a pre-gelled minimal Matrigel scaffold. VMOs support 60-day stable vasculature, exhibiting tissue maturation involving inflammation, extracellular matrix remodeling, and endothelial development. Compared to traditional spheroids, VMOs showed enhanced vascular complexity, sustained extracellular matrix production, and higher cell viability. The system preserved MSC heterogeneity including perivascular cell types, offering physiological relevance. Engraftment of breast cancer cells revealed stromal-tumor niches, enabling modeling of bone marrow metastasis. This robust platform offers an alternative model for studying vascular biology, stromal dynamics, and cancer progression, with potential applications in drug testing.
    Keywords:  Stem cells research; Tissue Engineering; Vascular remodeling
    DOI:  https://doi.org/10.1016/j.isci.2025.114548