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Pich, A.

Publications and source records attributed to Pich, A..

8 recordsLinked to original sources

O-mannosylation of fibrocystin and fibrocystin-L expands TMEM260 sequon selectivity and provides a potential link to the renal and auditory phenotypes of SHDRA

Protein O-mannosylation in the endoplasmic reticulum (ER) regulates the maturation and function of extracellular proteins, yet the substrate spectrum and biological functions of individual O-mannosyltransferases remain incompletely understood. TMEM260 is an ER-resident O-mannosyltransferase that modifies immunoglobulin-like, plexins, transcription factors (IPT) domains. Here, we identify fibrocystin and fibrocystin-L, encoded by PKHD1 and PKHD1L1, respectively, as novel TMEM260-mediated O-mannosylated proteins. By combining screening of human proteomic datasets with mass spectrometry-based analysis of IPT domains expressed in TMEM260-deficient HEK293 cells, we demonstrate that multiple IPT domains of fibrocystin and fibrocystin-L are modified by TMEM260. Our findings expand the known substrate requirements of TMEM260 by revealing tolerance of substantial sequon variation and demonstrating serine as an alternative acceptor residue within IPT domains. In humans, loss-of-function variants in TMEM260 cause structural heart defects and renal anomalies (SHDRA) syndrome, whereas pathogenic variants in fibrocystin cause autosomal recessive polycystic kidney disease (ARPKD). Notably, patients with SHDRA and ARPKD share overlapping renal phenotypes, suggesting that impaired TMEM260 function may phenocopy aspects of fibrocystin-associated diseases. Given that fibrocystin is a substrate protein for TMEM260-mediated O-mannosylation, these findings raise the possibility that functional impairment of TMEM260 causes aberrant O-mannosylation of fibrocystin. Thereby fibrocystin function might be compromised leading to the renal phenotype observed in patients with TMEM260 mutations. To directly assess the functional relevance of this modification, we expressed recombinant fibrocystin fragments in TMEM260-deficient cells complemented with either wild-type TMEM260 or a catalytically inactive TMEM260 mutant. Further, we investigate the O-mannosylation of the threonine residue directly C-terminal to the ARPKD-associated patient mutation L1407R. Strikingly, substitution of leucine L1407 by the patient-associated arginine residue, completely abolished O-mannosylation of the adjacent threonine, demonstrating that this disease-associated mutation directly disrupts a TMEM260-dependent O-mannosylation site. Together, our findings establish fibrocystin and fibrocystin-L as TMEM260-dependent O-mannosylated proteins and reveal a potential molecular mechanism linking defective TMEM260-mediated O-mannosylation to the renal phenotype of SHDRA, which overlaps with PKHD1-associated ARPKD.

biochemistry↗

Integrated risk assessment reveals low biological activity of RNA-based crop protection formulations across plant and non-target systems

RNA-based crop protection products are considered promising alternatives to conventional pesticides due to their high target specificity and selectivity profile. While current risk assessments mainly focus on sequence-dependent off-target effects, potential sequence-independent effects of RNA molecules and formulation components remain poorly understood. Here, we assessed the potential of naked and formulated RNA molecules to induce unintended biological responses in plants and non-target organisms using complementary plant stress and cellular toxicity assays. Single-stranded RNA (ssRNA), double-stranded RNA (dsRNA), circular RNA (circRNA), and chitosan-based RNA formulations were evaluated for their ability to induce early stress responses in plants and adverse effects in insect cells. Cytosolic Ca{superscript 2} signaling and reactive oxygen species (ROS) production were monitored in barley and Arabidopsis, while impedance-based phenotypic profiling (ECIS) was used to assess cellular responses in Spodoptera frugiperda (Sf21) cells. Neither naked nor formulated RNA preparations triggered pronounced Ca{superscript 2} influxes or ROS bursts, indicating an absence of substantial activation of early plant defense signaling. Likewise, RNA formulations caused only minor effects on insect cell attachment and spreading as a measure for cell viability. Observable responses occurred primarily at elevated concentrations of RNA formulations and were formulation-dependent rather than RNA-dependent. Overall, the investigated RNA molecules exhibited low biological activity across the tested non-target systems. Our results highlight the importance of evaluating RNA active ingredients and delivery matrices separately and demonstrate the value of integrated screening approaches for the early hazard assessment of RNA-based crop protection products.

Plant Biology↗

Collagen Rope Trick: Cell-Laden Fibre Assembly at 1 Liquid Interfaces

Summary ParagraphTissues and organs in living organisms represent centimeter-scale hierarchical architectures comprising nano-to microscale, uniaxially aligned extracellular matrix (ECM) fibres with high mechanical strength, integrated with cellular components, as exemplified in tendon, skin, cartilage, bone, and blood vessels1. Here, we present a liquid-liquid interfacial spinning method to produce highly uniaxially aligned, centimeter-scale collagen fibres. The dried fibres exhibit exceptional mechanical properties, with fracture strength of 280 MPa, Youngs modulus of 6 GPa, and toughness of 17 MJ m-3, comparable to spider silk and tendon collagen, and exceeding supramolecular and double-network hydrogels1. Incorporating living cells into the collagen solution yielded centimeter-scale, cell-laden aligned fibres, with densely adherent, uniaxially aligned cells and over 80% viability. Myoblast-laden fibres recapitulate biological features of fibrotic muscle tissues, as observed in type II diabetes2. Interfacial collagen assembly further enables fabrication of dimension-controlled constructs, like 2D sheets, 0D capsules, and 1D tubes, thus providing modular building blocks for centimeter-scale 3D tissues and organ-like structures. This approach offers a versatile platform to engineer mechanically robust, cell-laden tissues with controlled hierarchical architecture.

bioengineering↗

METTL3 regulates exocytosis independently of m6A

RNA modification pathways are often mis-regulated in various cancers, with N6-methyladenosine (m6A) having a pivotal role in cancer progression and metastasis. Methyltransferase-like 3 (METTL3), a core component of the m6A methyltransferase complex, functions not only as an m6A writer but also promotes tumorigenesis through m6A-independent mechanisms. Here, we show that METTL3 is mislocalized to the cytoplasm in breast cancer tumors from patients, contributing to the oncogenic phenotype. Cytoplasmic METTL3 interacts with EXOC7, a key regulator of exocytosis, promoting its stabilization. Additionally, METTL3 regulates m6A-dependent alternative splicing of EXOC7. Silencing METTL3 impairs vesicle trafficking and the breast cancer secretome - effects that do not rely on its enzymatic activity but instead involve METTL3-mediated stabilization of EXOC7 and potentially other exocyst components. Furthermore, METTL3 knockdown impairs invadopodia formation, collagen matrix invasion, and focal adhesion morphology in vitro, while inhibition of METTL3 catalytic activity does not. Our findings uncover non-catalytic roles of METTL3 in regulating exocytosis and the cancer secretome.

molecular biology↗

Sorafenib induces muscle wasting by disrupting the activity of distinct chromatin regulators

Adverse effects of chemotherapies can outweigh the benefits in cancer patients. Various chemotherapeutics are linked to muscle wasting or cachexia, drastically reducing the chance of survivability of cancer patients. Insights into the molecular basis of chemotherapy-induced cachexia is an unmet need to improve the treatment strategies. Here, we investigated the tyrosine kinase inhibitor class of chemotherapeutic agents for their effects on muscle function. Sorafenib, but not Nilotinib and Imatinib, triggered cachexia. System-wide transcriptome and proteome analyses revealed that Sorafenib alters the global transcriptional program and proteostasis in muscle cells. Mechanistically, Sorafenib treatment reduced active epigenetic mark H3K4 methylation on distinct muscle-specific genes due to the defective chromatin association of SET1/A, a catalytic component of the SET1/MLL complex. It favored transcriptionally incompetent chromatin, characterized by diminished association with RNA polymerase II. The transcriptional reorientation led to disrupted sarcomere organization, calcium homeostasis, and mitochondrial respiration. Consequently, the contractile ability of muscle cells was severely compromised. Collectively, we identified an unanticipated transcriptional mechanism underlying Sorafenib-induced cachexia. Our findings hold the potential to strategize therapy regimens to minimize chemotherapy-induced cachexia and improve treatment outcomes.

cell biology↗

SGLT2 inhibitors attenuate endothelial to mesenchymal transition and cardiac fibroblast activation

Beneficial effects of sodium glucose co-transporter 2 inhibitors (SGLT2is) in cardiovascular diseases have been extensively reported leading to the inclusion of these drugs in the treatment guidelines for heart failure. However, molecular actions especially on non-myocyte cells remain uncertain. We observed dose-dependent inhibitory effects of two SGLT2is, dapagliflozin (DAPA) and empagliflozin (EMPA), on inflammatory signaling in human umbilical vein endothelial cells (HUVECs). Proteomics analyses and subsequent enrichment analyses discovered profound effects of these SGLT2is on proteins involved in mitochondrial respiration and actin cytoskeleton. Validation in functional oxygen consumption measurements as well as tube formation and migration assays revealed strong impacts of DAPA. Considering that most influenced parameters played central roles in endothelial to mesenchymal transition (EndMT), we performed in vitro EndMT assays and identified substantial reduction of mesenchymal and fibrosis marker expression as well as changes in cellular morphology upon treatment with SGLT2is. In line, human cardiac fibroblasts (HCFs) exposed to DAPA showed less proliferation, reduced ATP production, and decelerated migration capacity while less extensive impacts were observed upon EMPA. Mechanistically, sodium proton exchanger 1 (NHE1) as well as sodium-myoinositol cotransporter (SMIT) and sodium-multivitamin cotransporter (SMVT) could be identified as relevant targets of SGLT2is in non-myocyte cardiovascular cells as validated by individual siRNA-knockdown experiments. In summary, we found comprehensive beneficial effects of SGLT2is on human endothelial cells and cardiac fibroblasts. The results of this study therefore support a distinct effect of selected SGLT2i on non-myocyte cardiovascular cells and grant further insights into potential molecular mode of action of these drugs.

pharmacology and toxicology↗

Pharmacological inhibition of bromodomain and extra-terminal proteins induces NRF-2-mediated inhibition of SARS-CoV-2 replication and is subject to viral antagonism

Inhibitors of bromodomain and extra-terminal proteins (iBETs), including JQ-1, have been suggested as potential therapeutics against SARS-CoV-2 infection. However, molecular mechanisms underlying JQ-1-induced antiviral activity and its susceptibility to viral antagonism remain incompletely understood. iBET treatment transiently inhibited infection by SARS-CoV-2 variants and SARS-CoV, but not MERS-CoV. Our functional assays confirmed JQ-1-mediated downregulation of ACE2 expression and multi-omics analysis uncovered induction of an antiviral NRF-2-mediated cytoprotective response as an additional antiviral component of JQ-1 treatment. Serial passaging of SARS-CoV-2 in the presence of JQ-1 resulted in predominance of ORF6-deficient variants. JQ-1 antiviral activity was transient in human bronchial airway epithelial cells (hBAECs) treated prior to infection and absent when administered therapeutically. We propose that JQ-1 exerts pleiotropic effects that collectively induce a transient antiviral state that is ultimately nullified by an established SARS-CoV-2 infection, raising questions on their clinical suitability in the context of COVID-19.

microbiology↗

Ena/VASP clustering at microspike tips involves Lamellipodin but not I-BAR proteins, and absolutely requires unconventional Myosin-X

Sheet-like membrane protrusions at the leading edge, termed lamellipodia, drive 2D-cell migration using active actin polymerization. Microspikes comprise actin-filament bundles embedded within lamellipodia, but the molecular mechanisms driving their formation and their potential functional relevance have remained elusive. Microspike formation requires the specific activity of clustered Ena/VASP proteins at their tips to enable processive actin assembly in the presence of capping protein, but the factors and mechanisms mediating Ena/VASP clustering are poorly understood. Systematic analyses of B16-F1 melanoma mutants lacking potential candidate proteins revealed that neither inverse BAR-domain proteins, nor lamellipodin or Abi are essential for clustering, although they differentially contribute to lamellipodial VASP accumulation. In contrast, unconventional myosin-X (MyoX) identified here as proximal to VASP was obligatory for Ena/VASP clustering and microspike formation. Interestingly, and despite the invariable distribution of other relevant marker proteins, the width of lamellipodia in MyoX-KO mutants was significantly reduced as compared to B16-F1 control, suggesting that microspikes contribute to lamellipodium stability. Consistently, MyoX removal caused marked defects in protrusion and random 2D-cell migration. Strikingly, Ena/VASP-deficiency also uncoupled MyoX cluster dynamics from actin assembly in lamellipodia, establishing their tight functional association in microspike formation. Significance StatementUnlike filopodia that protrude well beyond the cell periphery and are implicated in sensing, morphogenesis and cell-to-cell communication, the function of microspikes consisting of actin-filament bundles fully embedded within lamellipodia is less clear. Microspike formation involves specific clustering of Ena/VASP family members at filament-barbed ends to enable processive actin polymerization in the presence of capping protein, but the factors and mechanisms mediating Ena/VASP clustering have remained unknown. Here, we systematically analyzed these processes in genetic knockout mutants derived from B16-F1 cells and show that Ena/VASP clustering at microspike tips involves Lamellipodin, but not inverse BAR-domain proteins, and strictly requires unconventional Myosin-X. Complete loss of microspikes was confirmed with CRISPR/Cas9-mediated MyoX knockout in Rat2 fibroblasts, excluding cell type-specific effects.

cell biology↗