EGLN1 inhibitor

EGLN1 inhibitors, also known as Prolyl Hydroxylase Domain 2 (PHD2) inhibitors, are a class of therapeutic agents that target the oxygen-sensing enzyme EGLN1. By inhibiting EGLN1, these drugs prevent the hydroxylation and subsequent proteasomal degradation of Hypoxia-Inducible Factor alpha (HIF-α) subunits. This leads to the stabilization and accumulation of HIF, which translocates to the nucleus to activate the transcription of genes involved in erythropoiesis (such as erythropoietin), iron metabolism, and angiogenesis. While primarily developed and approved for the treatment of anemia associated with chronic kidney disease (CKD), recent research suggests potential applications in oncology, particularly in KRAS-mutated lung adenocarcinoma, where EGLN1 may support tumor growth through both HIF-dependent and HIF-independent mitochondrial modulation.

Other names

PHD2 inhibitorPHD-2 inhibitorPHD 2 inhibitorHIF prolyl hydroxylase inhibitorHIF-PH inhibitorProlyl hydroxylase domain 2 inhibitor