Fig. 2. The PHD2-HIF-VHL-EPO axis and its dysregulation.
(A) Scheme depicting the distinctive oxygen-sensing mechanism that regulates EPO transcription. In the presence of oxygen, PHD2 site-specifically hydroxylates HIF-2α, thereby targeting it for degradation by VHL. Little HIF-2α remains to bind the HRE of the EPO gene, so activation is modest. ARNT is the stable subunit of HIF-2.
(B) Loss-of-function mutations in PHD2, denoted by PHD2*, cause an increase in HIF-2α and increased (or inappropriately normal) EPO gene activation, designated erythrocytosis type 3 (ECYT3) in the OMIM classification.
(C) In gain-of-function mutations in HIF-2α, denoted by HIF-2α*, hydroxylation is deceased and VHL binding is reduced, leading to increased EPO gene activation, ECYT4.
(D) Loss-of-function mutations in VHL, denoted by VHL*, reduce binding to hydroxylated HIF-2α leading to increased EPO gene activation, ECYT2.
(E) A mutation in EPO, denoted by EPO* causes a frameshift that initiates excess production of EPO from a normally noncoding EPO mRNA, ECYT5.
