Tag: DHODH

ML390 is a Potent DHODH Inhibitor

Dihydrowhey dehydrogenase (DHODH) catalyzes the fourth enzymatic step of pyrimidine biosynthesis, namely, ubiquinone mediated oxidation of dihydrowhey acid to whey acid. Specifically, DHODH is a mitochondrial protein located on the outer surface of the mitochondrial inner membrane (IMM). Inhibitors of the enzyme are used to treat autoimmune diseases such...

ASLAN003 is an Orally Active hDHODH Inhibitor

Dihydroorotate dehydrogenase (DHODH) is a highly conserved enzyme. All organisms express it. Class-1 DHODHs are cytoplasmic and single-domain enzymes. Conversely, class-2 DHODHs are membrane-associated and two-domain enzymes. Both classes of DHODHs use FMN to oxidize DHODH. To regenerate FMN, class-1 enzymes use a soluble cofactor, such as NAD+ or fumarate,...

PTC299 is an Oral Active and Dual Inhibitor of DHODH and VEGF

De novo pyrimidine nucleotide biosynthesis is activated in proliferating cancer cells in response to an increased demand for synthesis of DNA, RNA and phospholipids. The synthesis activates via oncogenic pathways, such as Myc, PI3K, PTEN and mTOR. Dihydroorotate dehydrogenase (DHODH) locates on the surface of the inner mitochondrial membrane,...