DFN-529 / CervoMed - LARVOL DELTA

[VIRTUAL] Evaluation of Cytotoxicity of Anti-VEGF Molecules on Vascular Endothelial Growth Factor Enriched Choroidal Vascular Endothelial Cells (ARVO 2021) - "This includes combination of various anti- VEGF molecules such as Pazopanib, Palomid 529 and Bevacizumab (avastin) for targeting vascular endothelial growth factor (VEGF). Although anti-VEGF molecules are effective in controlling the proliferation and cell viability rates of VEGF-enriched CVECs, a combination of these anti-VEGF molecules are more effective in inhibiting the cell proliferation rates than any one anti-VEGF molecule alone in comparison to control."

Ophthalmology • CASP3

Chronic treatment with the (iso-)glutaminyl cyclase inhibitor PQ529 is a novel and effective approach for glomerulonephritis in chronic kidney disease. (PubMed, Naunyn Schmiedebergs Arch Pharmacol) - "These results suggest that PQ529 suppresses the progression of inflammation-induced renal dysfunction by inhibiting the CCL2/CCR2 axis. Inhibition of QC/isoQC may thus be a viable alternative therapeutic approach for treating glomerulonephritis and CKD patients."

Journal • Chronic Kidney Disease • Glomerulonephritis • Immunology • Inflammation • Lupus Nephritis • Nephrology • Renal Disease • CCL2 • CD68 • CLU • KIM1

DNA ligase I variants fail in the ligation of mutagenic repair intermediates with mismatches and oxidative DNA damage. (PubMed, Mutagenesis) - "Moreover, we found that the presence of all possible 12 non-canonical base pairs variously impacts the ligation efficiency by P529L and R771W depending on the architecture at the DNA end, whereas E566K exhibits no activity against all substrates tested. Our results contribute to the understanding of the substrate specificity and mismatch discrimination of LIG1 for mutagenic repair intermediates and the effect of non-synonymous mutations on ligase fidelity."

Journal • Immunology

The cytotoxicity and synergistic potential of aspirin and aspirin analogues towards oesophageal and colorectal cancer. (PubMed, Curr Clin Pharmacol) - "These findings indicate the potential and limitations of aspirin and aspirin analogues as chemotherapeutic agents against OC and CRC when combined with platins."

Journal • Colorectal Cancer • Esophageal Cancer • Gastrointestinal Cancer • Oncology • Solid Tumor • Squamous Cell Carcinoma

Stratus Media Group acquires Paloma Pharmaceuticals, Inc. and VasculoMedics, Inc (GlobeNewswire) - "Stratus Media Group...announced today the acquisition, through merger, of two biotechnology companies, Paloma Pharmaceuticals, Inc. and VasculoMedics, Inc. With these acquisitions, Stratus, which will be renamed RestorGenex, plans to create a world-class pharmaceutical company with an initial focus on dermatology, ocular diseases and women's health."

M&A • Fibrosis • Oncology • Psoriasis

The Brain Penetrating and Dual TORC1/TORC2 Inhibitor, RES529, Elicits Anti-Glioma Activity and Enhances the Therapeutic Effects of Anti-Angiogenetic Compounds in Preclinical Murine Models. (PubMed, Cancers (Basel)) - "Here, we determined the sensitizing effects of the small molecule and oral available dual TORC1/TORC2 dissociative inhibitor, RES529, alone or in combination with the anti-VEGF blocking antibody, bevacizumab, or the tyrosine kinase inhibitor, sunitinib, in human GBM models. Conclusions. In summary, RES529, the first dual TORC1/TORC2 dissociative inhibitor, lacking affinity for ABCB1/ABCG2 and having good brain penetration, was active in GBM preclinical/murine models giving credence to its use in clinical trial for patients with GBM treated in association with anti-angiogenetic compounds."

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