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Biology subjects

Fedele, C.

Publications and source records attributed to Fedele, C..

6 recordsLinked to original sources

Viscoelasticity driven deformation dynamics of the substrate affect mechanically induced Ca2+ signals

The viscoelastic properties of the substrate are known to affect many aspects of cellular behavior from migration to differentiation. Cells are also known to sense deformations in the extracellular matrix (ECM). However, these mechanotransduction events have mostly been studied separately, and the emphasis has been on purely elastic materials although most tissues in the body are viscoelastic. We wanted to understand how the viscosity and elasticity of the substrate affect cells mechanosensation, i.e., how cells integrate passive (substrate viscoelasticity) and active cues (dynamic substrate deformation) into calcium transients. We used a light-controllable Disperse Red 1-glass (DR1-glass) coating together with a thin polyacrylamide (PAA) hydrogel with controllable viscoelasticity. This allowed us to generate local deformations in the cell-substrate interface on substrates with different viscoelastic properties. Inspecting the resulting calcium transients in a Madin Darby canine kidney type II (MDCK II) monolayer with the genetically encoded calcium indicator jRCaMP1b revealed that cells responded to deformation differently depending on the viscoelasticity of the substrate. On stiff elastic gels cells exhibited all in all the largest calcium responses as well as increased sensitivity to the magnitude of deformation, with larger deformations leading to stronger calcium signals, whereas on soft elastic and soft viscoelastic gels the magnitudes of deformation had less effect on the degree of calcium signals. Indeed, immunostainings showed that cells formed the strongest focal adhesions (FA) on stiff gels, albeit differences were surprisingly small. Instead, computational modeling revealed that forces generated at FAs were strongly dependent on the viscoelasticity of the substrate, with increased elasticity and decreased viscosity leading to larger forces. Moreover, viscoelasticity affected the dynamics of the force generation. On stiff elastic gels force increased in fast steps, whereas on soft gels the buildup was gradual and was further slowed down by increased viscosity. Surprisingly, experiments with PIEZO1 KO cells showed that the calcium responses to the substrate deformation did not require PIEZO1 channels. Instead, depleting the ER with thapsigargin (TG), depolymerizing the actin cytoskeleton with cytochalasin D (cyto D) and latrunculin A (Lat A), and inhibiting actomyosin II with y-27632, showed that the calcium was mainly released from the ER in an actin, but not actomyosin, dependent mechanism. The data therefore suggests that the forces subjected to FAs could be directly transmitted to the ER via an actin mediated tension that results in the opening of ER residing calcium release channels. Our results illustrate that the viscoelasticity of the cell niche controls cell behavior in two ways. Firstly, it affects how cells build adhesions to the ECM and thus the accumulation of mechanosensitive proteins. Secondly, it affects the dynamics of the deformations and forces that are sensed by FAs. In line with our previous findings, we show that the mechanically induced calcium responses are dependent on dynamics, with fast mechanical cues resulting in larger calcium responses. Moreover, our research suggests that cells may possess distinct response mechanisms that are selectively activated depending on the mechanical properties of their niche, and the type and dynamics of the mechanical stimulation.

cell biology↗

Prospective isolation according to melanin pigment content of melanoma cells with heterogeneous potentials for disease propagation

Functional variation between cancer cells (intra-tumoral heterogeneity) poses a major challenge to treating and managing cancer patients. Melanomas are typically composed of cancer cells with heterogeneous content of melanin pigment. Pigment production is a hallmark of normal melanocytic differentiation, however the functional consequences of melanin production in melanoma cells remains poorly understood owing to a lack of experimental approaches for detection of pigment in unfixed cells. Here, we describe a novel flow cytometric method for high purity separation of viable melanoma cells based on their content of melanin pigment, exploiting the infrared light scattering properties of melanin. By fluorescence-activated cell sorting, we show that melanoma cells with low-pigment content (LPCs) in culture and in patient tumors are far more abundant than high-pigment cells (HPCs), and have substantially increased potentials for colony formation in vitro and for tumor formation in vivo. RNAseq analysis revealed activation of P53 in HPCs associated with perturbed cell cycling, whereas LPCs displayed upregulation of MYC-associated transcription and activated ribosome biogenesis. The latter was reduced by topoisomerase 2 beta targeting with CX-5461, which also induced senescent HPC phenotypes and irreversible loss of clonogenic activity. These data illuminate an inverted pyramid hierarchical model of melanoma cell propagation wherein abundant LPCs frequently renew their own malignant potential to propagate disease, but also rarely generate HPCs that lose this ability in a manner that may be promoted as an anti-melanoma strategy.

cancer biology↗

Light-induced nanoscale deformation in azobenzene thin film triggers rapid intracellular Ca2+ increase via mechanosensitive cation channels

Epithelial cells are in continuous dynamic biochemical and physical interaction with their extracellular environment. Ultimately, this interplay guides fundamental physiological processes. In these interactions, cells generate fast local and global transients of Ca2+ ions, which act as key intracellular messengers. However, the mechanical triggers initiating these responses have remained unclear. Light-responsive materials offer intriguing possibilities to dynamically modify the physical niche of the cells. Here, we use a light-sensitive azobenzene-based glassy material that can be micropatterned with visible light to undergo spatiotemporally controlled deformations. The material allows mechanical stimulation of single cells or multicellular assemblies, offering unique opportunities for experimental mechanobiology. Real-time monitoring of consequential rapid intracellular Ca2+ signals reveal that Piezo1 is the key mechanosensitive ion channel generating the Ca2+ transients after nanoscale mechanical deformation of the cell culture substrate. Furthermore, our studies indicate that Piezo1 preferably responds to lateral material movement at cell-material interphase rather than to absolute topographical change of the substrate. Finally, experimentally verified computational modeling of the signaling kinetics suggests that the lateral mechanical stimulus triggers multiplexed intercellular signaling that involves Na+, highlighting the complexity of mechanical signaling in multicellular systems. These results give mechanistic understanding on how cells respond to material dynamics and deformations.

bioengineering↗

Combined Inhibition of SHP2 and CXCR1/2 Promotes Anti-Tumor T Cell Response in NSCLC

Clinical trials of SHP2 inhibitors (SHP2i) alone and in various combinations are ongoing for multiple tumors with over-activation of the RAS/ERK pathway. SHP2 plays critical roles in normal cell signaling; hence, SHP2is could influence the tumor microenvironment. We found that SHP2i treatment depleted alveolar and M2-like macrophages and promoted B and T lymphocyte infiltration in Kras- and Egfr-mutant non-small cell lung cancer (NSCLC). However, treatment also increased intratumor gMDSCs via tumor-intrinsic, NF-kB-dependent production of CXCR2 ligands. Other RAS/ERK pathway inhibitors also induced CXCR2 ligands and gMDSC influx in mice, and CXCR2 ligands were induced in tumors from patients on KRASG12C-inhibitor trials. Combined SHP2(SHP099)/CXCR1/2(SX682) inhibition depleted a specific cluster of S100a8/9high gMDSCs, generated Klrg1+ CD8+ effector T cells with a strong cytotoxic phenotype but expressing the checkpoint receptor NKG2A, and enhanced survival in Kras-and Egfr-mutant models. Our results argue for testing RAS/ERK pathway/CXCR1/2/NKG2A inhibitor combinations in NSCLC patients. Statement of SignificanceOur study shows that inhibiting the SHP2/RAS/ERK pathway triggers NF-kB-dependent up-regulation of CXCR2 ligands and recruitment of S100A8high gMDSCs, which suppress T cells in NSCLC. Combining SHP2 and CXCR2 inhibitors blocks this gMDSC immigration, resulting in enhanced Th1 polarization, induction of CD8+ KLRG1+ effector T cells with high cytotoxic activity and improved survival in multiple NSCLC models.

cancer biology↗

SHP2 Inhibition Abrogates Adaptive Resistance to KRASG12C-Inhibition and Remodels the Tumor Microenvironment of KRAS-Mutant Tumors

KRAS is the most frequently mutated oncogene in human cancer, and KRAS inhibition has been a longtime therapeutic goal. Recently, inhibitors (G12C-Is) that bind KRASG12C-GDP and react with Cys-12 were developed. Using new affinity reagents to monitor KRASG12C activation and inhibitor engagement, we found that, reflecting its action upstream of SOS1/2, SHP2 inhibitors (SHP2-Is) increased KRAS-GDP occupancy, enhancing G12C-I efficacy. SHP2-Is abrogated feedback signaling by multiple RTKs and blocked adaptive resistance to G12C-Is in vitro, in xenografts, and in syngeneic KRASG12C-mutant pancreatic ductal adenocarcinoma (PDAC) and non-small cell lung cancer (NSCLC) models. Biochemical analysis revealed enhanced suppression of ERK-, MYC-, anti-apoptotic-, and cell-cycle genes, and increased pro-apoptotic gene expression in tumors from combination-treated mice. SHP2-I/G12C-I also evoked favorable changes in the immune microenvironment, decreasing myeloid suppressor cells, increasing CD8+ T cells, and sensitizing tumors to PD-1 blockade. Experiments using cells expressing inhibitor-resistant SHP2 showed that SHP2 inhibition in PDAC cells is required for tumor regression and remodeling of the immune microenvironment, but also revealed direct inhibitory effects on angiogenesis resulting in decreased tumor vascularity. Our results demonstrate that SHP2-I/G12C-I combinations confer a substantial survival benefit in PDAC and NSCLC and identify additional combination strategies for enhancing the efficacy of G12C-Is.

cancer biology↗

SHP2 Inhibition Abrogates MEK inhibitor Resistance in Multiple Cancer Models

Adaptive resistance to MEK inhibitors (MEK-Is) typically occurs via induction of genes for different receptor tyrosine kinases (RTKs) and/or their ligands, even in tumors of the same histotype, making combination strategies challenging. SHP2 (PTPN11) is required for RAS/ERK pathway activation by most RTKs, and might provide a common resistance node. We found that combining the SHP2 inhibitor SHP099 with a MEK-I inhibits proliferation of multiple cancer cells in vitro. PTPN11 knockdown/MEK-I had similar effects, while expressing SHP099-binding mutants conferred resistance, demonstrating that SHP099 was on-target. This combination was efficacious in xenograft and/or genetically engineered models of KRAS-mutant pancreas cancer and ovarian cancer and in wild-type RAS-expressing triple negative breast cancer. Biochemical studies show that SHP099 impedes SOS/RAS/MEK/ERK1/2 reactivation in response to MEK-Is and blocks ERK1/2-dependent transcriptional programs. SHP099 alone also inhibited RAS activation in some, but not all, KRAS-mutant lines. Hence, SHP099/MEK-I combinations could have therapeutic utility in multiple malignancies.\n\nSIGNIFICANCEMEK inhibitors have shown limited efficacy as single agents because of the rapid development of adaptive resistance. We find that combining SHP2 and MEK inhibition abrogates adaptive resistance in multiple cancer models, expressing mutant and wild-type KRAS.

cancer biology↗