DDP-38003 / Rasna Therap - LARVOL DELTA

Metabolic traits shape responses to LSD1-directed therapy in glioblastoma tumor-initiating cells. (PubMed, Sci Adv) - "We demonstrated the therapeutic potential of its pharmacological inhibition in glioblastoma using DDP_38003 (LSD1i), which selectively targets tumor-initiating cells (TICs) by hampering their adaptability to stress...A dropout short hairpin RNA screening identifies postglycosylphosphatidylinositol attachment to proteins inositol deacylase 1 (PGAP1) as a mediator of resistance to LSD1i. Disruptions in ER and mitochondrial balance holds promise for improving LSD1-targeted therapy efficacy and overcoming treatment resistance."

Journal • Brain Cancer • Glioblastoma • Movement Disorders • Oncology • Solid Tumor • KDM1A

Pharmacological inhibition of LSD1 triggers myeloid differentiation by targeting GSE1 oncogenic functions in AML. (PubMed, Oncogene) - "Here, we unraveled a novel mode of action of the LSD1 inhibitors MC2580 and DDP-38003, showing that they can induce differentiation of AML cells through the downregulation of the chromatin protein GSE1...Moreover, we show that LSD1 inhibitors lead to the reduced binding of GSE1 to these promoters, activating transcriptional programs that trigger myeloid differentiation. Our study offers new insights into GSE1 as a novel therapeutic target for AML."

Journal • Acute Myelogenous Leukemia • Hematological Disorders • Hematological Malignancies • Oncology • KDM1A