Based on the important roles of HS in cancer, several anti-tumor therapeutic strategies targeting HS and its modifying enzymes have been under investigation: (i) heparanase inhibitors (e.g., Roneparstat, a chemically modified 100% N-desulfated, N-reacetylated, and 25% glycol-split heparin with very low anticoagulant activity) have shown promise in preclinical clinical studies [88]; (ii) HS mimetics can competitively inhibit interactions between HS and growth factors [89]; and (iii) sulfatase inhibitors are being explored for their role in normalizing abnormal HS sulfation patterns. The gene discussed is HPSE; the disease is cancer.