Publications by authors named "E Gilardoni"
OncoFAP is an ultrahigh affinity ligand of fibroblast activation protein (FAP), a tumor-associated antigen overexpressed in the stroma of the majority of solid tumors. OncoFAP has been previously implemented as a tumor-homing moiety for the development of small molecule drug conjugates (SMDCs). In the same context, the glycine--proline dipeptide was included with the aim to selectively undergo cleavage only in the presence of the target FAP, triggering the consequent release of the cytotoxic payload in the tumor microenvironment.
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- The study investigated the effects of inhaled carnosine on mice exposed to cigarette smoke, simulating chronic obstructive pulmonary disease (COPD), by administering various doses (10, 50, or 100 mg/kg/day).
- It was found that inhaled carnosine reduced lung inflammation and oxidative stress caused by cigarette smoke, with the most significant effects observed at the highest dose (100 mg/kg), particularly affecting specific inflammatory cytokines.
- A deeper analysis revealed that carnosine notably reversed many COPD-related pathways and upregulated key enzymes involved in cellular defense mechanisms, emphasizing its potential therapeutic role in managing oxidative stress and inflammation in lung tissue.
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- Fibroblast activation protein (FAP) is commonly found in the stroma of human tumors, making it a target for cancer detection using radiolabeled ligands, such as the newly discovered OncoFAP, which shows rapid tumor accumulation and low healthy tissue uptake.
- A trimerized version called OncoFAP-23 has improved binding affinity and was tested in tumor-bearing mice, demonstrating a favorable biodistribution profile with significant tumor retention and minimal healthy tissue accumulation.
- Combining OncoFAP-23 with the interleukin 2 treatment shows increased anti-tumor effects and a strong immune response, while also displaying a good safety profile with no observed toxicity.
Article Synopsis
- Anti-PD-1 antibodies have transformed cancer treatment by achieving lasting remission in some patients, leading researchers to seek ways to enhance their effectiveness with new biomarkers and drugs.
- This study introduces F8(scDb)-IL7, a novel fusion protein targeting EDA-FN, which is present in most tumors but rare in healthy tissue, potentially improving cancer therapy at the disease site.
- F8(scDb)-IL7 was shown to boost T Cell Factor 1 expression in CD8+T cells and effectively eradicates sarcoma lesions when used alongside anti-PD-1 treatment, suggesting a promising combination for cancer patients.
DNA-Encoded Libraries (DELs) allow the parallel screening of millions of compounds for various applications, including discovery or affinity maturation campaigns. However, library construction and HIT resynthesis can be cumbersome, especially when library members present an unknown stereochemistry. We introduce a permutational encoding strategy suitable for the construction of highly pure single-stranded single-pharmacophore DELs, designed to distinguish isomers at the sequencing level (e.
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