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Biology subjects

Jarolimek, W.

Publications and source records attributed to Jarolimek, W..

3 recordsLinked to original sources

LOX inhibition disrupts a collagen-integrin-MYC axis as a translatable targeting strategy in invasive lobular carcinoma

Invasive lobular carcinoma (ILC) accounts for 15% of breast cancers yet lacks specific therapy because ILCs are underrepresented in clinical trials and preclinical models are lacking. We established intraductal xenograft models to test whether the clinical pan-lysyl-oxidase PXS-5505, now in phase trials for myelofibrosis can exploit the collagen-rich matrix dependency created by CDH1 loss. PXS-5505 remodels fibrillar collagen, and halts tumor expansion and metastatic seeding across ER+ and triple negative models without systemic toxicity. Genome-wide CRISPR screens reveal ITGAV and ITGB5 as synthetic lethal partners of CDH1 and LOX inhibition downregulates their expression together with MYC, NF-{kappa}B, and AP-1 transcriptional programmes. Collagen fibre density/alignment, and MYC/AP-1 gene signatures serve as pharmacodynamic readouts of drug activity. These data uncover a tractable ECM-integrin-MYC axis in ILC and nominate PXS-5505, alone or with endocrine therapy, for window of opportunity trials in this understudied breast cancer subtype. One Sentence SummaryTargeting matrix remodelling in ILC inhibits ILC progression and alters multiple molecular endpoints, providing a translatable therapeutic strategy for this understudied subtype that requires better treatments.

cancer biology↗

Matrix structure and microenvironment dynamics correlate with chemotherapy response in ovarian cancer

Elevated extracellular matrix (ECM) in the tumor microenvironment (TME) is associated with chemoresistance and poor prognosis. We hypothesized that modifying the ECM may enhance response to chemotherapy. We measured chemotherapy-induced changes in the TME of two mouse models of high-grade serous ovarian cancer (HGSOC) that differed in chemotherapy response. Treatment of the chemo-sensitive tumors triggered dynamic transcriptional ECM and immune changes and structural modifications of ECM proteins. These changes, observed over twenty-days post-chemotherapy, had relevance to HGSOC patient responses to chemotherapy. Integrating transcriptomics with ECM structure metrics, we identified ECM targets, including lysyl oxidase (LOX), that might enhance chemotherapy in less responsive mouse tumors. Given alone or in combination with chemotherapy, a pan-LOX inhibitor (PXS-5505) modulated fibroblast and immune cell distribution and reduced tumor stiffness in HGSOC chemo-resistant mouse tumors. Moreover, pre-treatment with PXS-5505 improved response to chemotherapy. We conclude that pretreatment with ECM targeting agents may improve response to chemotherapy, by altering ECM structure and immune responses.

cancer biology↗

Accurate quantification of lysyl oxidase concentration in human tissue

The family of Lysyl oxidase enzymes play fundamental roles in the formation of the extracellular matrix, through catalyzing the crosslinking of collagen and elastin fibers. Lysyl oxidase (LOX) -- one of the 5 family members (LOX, LOXL1-4), is a disease biomarker, with blood concentration positively correlating with progression of fibrosis or cancer. An accurate quantification of LOX concentration can support diagnosis, monitoring of disease progression or treatment success. However, reported LOX concentrations in human blood are inconsistent. Therefore, a novel, high-throughput and sensitive digital enzyme-linked immunosorbent assay was developed using two validated and selective human anti-LOX antibodies and single molecule array technology. Both, the 56 kDa pro-form and the 32 kDa active form can be accurately measured from recombinant and native protein. The serum LOX concentration correlated with LOX activity measured in the same platform using a bio-probe. The usefulness of this technology was demonstrated in serum from bladder cancer patients wherein LOX concentration was significantly higher compared to the healthy subjects. This study demonstrates the validation and use of a sensitive and accurate method for measuring LOX concentration in human samples. This novel method may be superior than some commercially available enzyme-linked immunosorbent assay kits for accurate measurement of LOX concentrations in clinical settings.

molecular biology↗