Loading... PRMT5 The methyltransferase PRMT5 (protein arginine methyl transferase 5) catalyzes the transfer of a methyl group from the co-factor S-adenosylmethione (SAM) to arginine residues in a target protein, thereby regulating the activity of a range of protein substrates, many of which are involved in key cellular processes. PRMT5 is upregulated in a variety of human malignancies. In cancer cell lines, increased PRMT5 expression is correlated with growth rate while in patient-derived primary tumors it is correlated with poor patient survival. In cancer, the main mechanism of action of PRMT5 inhibition is to modulate alternative RNA splicing. Many hematological and solid tumors are known to hijack the cell’s splicing machinery to maintain splicing fidelity and drive tumorigenesis and tumor growth. This renders PRMT5 – a key splicing regulator – an exploitable vulnerability in such tumors. Indeed, in pre-clinical models, pharmacological inhibition of PRMT5 induces robust anti-tumor activity, further highlighting the emergence of PRMT5 as a promising cancer drug target. Back to pipeline RORγt ERRα LXR PRMT5 TH17 © Scicomvisuals | Privacy | Disclaimer

Loading... Our interest Lead Pharma is a research & development company discovering, designing, and delivering innovative small-molecule therapies to treat immune diseases and cancer. Collaborations are a key part of our business strategy. Contact If you are a pharmaceutical company, an investor or a potential strategic partner, we would appreciate you getting in touch to discuss our research projects and strategic ambitions as well as opportunities for collaboration. Please contact us at BD@leadpharma.com Partnerships © Scicomvisuals | Privacy | Disclaimer

Loading... ERRα The estrogen-related receptor α (ERRα) is a nuclear receptor and a transcriptional master regulator of mitochondrial function and flexibility, controlling an intricate network of mitochondrial and metabolic genes. ERRα upregulation and activation is associated with poor prognosis, recurrence of cancer, therapy resistance as well as with metastasis of several tumor types including melanoma, breast and colon cancer. The deregulation of energetics in cancer cells is an emerging hallmark of cancer – a hallmark Lead Pharma is targeting with ERRα inverse agonists. Lead Pharma has developed the very first drug-like series of potent, non-covalent, non-steroidal ERRα inverse agonists. Back to pipeline RORγt ERRα LXR PRMT5 TH17 © Scicomvisuals | Privacy | Disclaimer