Structural basis for the function and inhibition of dihydroorotate dehydrogenase from Schistosoma mansoni

RM de Mori, MAA Aleixo, LCC Zapata… - The FEBS …, 2021 - Wiley Online Library
Schistosomiasis is a serious public health problem, prevalent in tropical and subtropical
areas, especially in poor communities without access to safe drinking water and adequate …

Antimalarial activity of single-dose DSM265, a novel plasmodium dihydroorotate dehydrogenase inhibitor, in patients with uncomplicated Plasmodium falciparum or …

A Llanos-Cuentas, M Casapia… - The Lancet Infectious …, 2018 - thelancet.com
Background DSM265 is a novel, long-duration inhibitor of plasmodium dihydroorotate
dehydrogenase (DHODH) with excellent selectivity over human DHODH and activity against …

A triazolopyrimidine-based dihydroorotate dehydrogenase inhibitor with improved drug-like properties for treatment and prevention of malaria

MA Phillips, KL White, S Kokkonda, X Deng… - ACS infectious …, 2016 - ACS Publications
The emergence of drug-resistant malaria parasites continues to hamper efforts to control this
lethal disease. Dihydroorotate dehydrogenase has recently been validated as a new target …

Structure of Plasmodium falciparum dihydroorotate dehydrogenase with a bound inhibitor

DE Hurt, J Widom, J Clardy - Acta Crystallographica Section D …, 2006 - journals.iucr.org
Membrane-associated dihydroorotate dehydrogenase (DHODH) is an antimalarial
therapeutic target without an effective inhibitor. Studies on human DHODH (HsDHODH) led …

Identification of New Human Malaria Parasite Plasmodium falciparum Dihydroorotate Dehydrogenase Inhibitors by Pharmacophore and Structure-Based Virtual …

E Pavadai, F El Mazouni, S Wittlin… - Journal of chemical …, 2016 - ACS Publications
Plasmodium falciparum dihydroorotate dehydrogenase (Pf DHODH), a key enzyme in the de
novo pyrimidine biosynthesis pathway, which the Plasmodium falciparum relies on …

Deciphering Interactions between Potential Inhibitors and the Plasmodium falciparum DHODH Enzyme: A Computational Perspective

AH Lima Costa, KS Bezerra… - The Journal of …, 2023 - ACS Publications
Malaria is a parasitic disease that, in its most severe form, can even lead to death. Insect-
resistant vectors, insufficiently effective vaccines, and drugs that cannot stop parasitic …

Brequinar derivatives and species-specific drug design for dihydroorotate dehydrogenase

DE Hurt, AE Sutton, J Clardy - Bioorganic & medicinal chemistry letters, 2006 - Elsevier
Therapeutic agents brequinar sodium and leflunomide (Arava™) work by binding in a
hydrophobic tunnel formed by a highly variable N-terminus of family 2 dihydroorotate …

Natural products as inhibitors of Leishmania major dihydroorotate dehydrogenase

LA Chibli, TJ Schmidt, MC Nonato, FA Calil… - European journal of …, 2018 - Elsevier
The flavoenzyme dihydroorotate dehydrogenase (DHODH) catalyzes the fourth reaction of
the de novo pyrimidine biosynthetic pathway, which exerts vital functions in the cells …

Analysis of Flavin Oxidation and Electron-Transfer Inhibition in Plasmodium falciparum Dihydroorotate Dehydrogenase

NA Malmquist, R Gujjar, PK Rathod, MA Phillips - Biochemistry, 2008 - ACS Publications
Plasmodium falciparum dihydroorotate dehydrogenase (pf DHODH) is a flavin-dependent
mitochondrial enzyme that provides the only route to pyrimidine biosynthesis in the parasite …

Fragment-based drug design, 2D-QSAR and DFT calculation: Scaffolds of 1, 2, 4, triazolo [1, 5-a] pyrimidin-7-amines as potential inhibitors of Plasmodium falciparum …

O Iwaloye, OO Elekofehinti, F Olawale… - Letters in Drug …, 2023 - ingentaconnect.com
Background: Plasmodium falciparum dihydroorotate dehydrogenase (PfDODH) is one of the
enzymes currently explored in the treatment of malaria. Although there is currently no …