Proteins > Dihydroorotate dehydrogenase (quinone), mitochondrial
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Dihydroorotate dehydrogenase (quinone), mitochondrial
A dihydroorotate dehydrogenase (quinone), mitochondrial that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q02127]
Synonyms
DHOdehase;
EC 1.3.5.2;
Dihydroorotate oxidase
Research
Bioassay Publications (48)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 4 (8.33) | 18.2507 |
| 2000's | 9 (18.75) | 29.6817 |
| 2010's | 22 (45.83) | 24.3611 |
| 2020's | 13 (27.08) | 2.80 |
Compounds (30)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Drugs with Other Measurements
Low cytotoxic quinoline-4-carboxylic acids derived from vanillin precursors as potential human dihydroorotate dehydrogenase inhibitors.Bioorganic & medicinal chemistry letters, , 08-15, Volume: 46, 2021
Isoxazolylthioamides as potential immunosuppressants a combinatorial chemistry approach.Bioorganic & medicinal chemistry letters, , Aug-18, Volume: 8, Issue:16, 1998
Pyrazole bioisosteres of leflunomide as B-cell immunosuppressants for xenotransplantation and chronic rejection: scope and limitations.Journal of medicinal chemistry, , Aug-27, Volume: 41, Issue:18, 1998
[no title available]Journal of medicinal chemistry, , 10-13, Volume: 65, Issue:19, 2022
[no title available]Journal of medicinal chemistry, , 09-23, Volume: 64, Issue:18, 2021
Targeting Chikungunya Virus Replication by Benzoannulene Inhibitors.Journal of medicinal chemistry, , 04-22, Volume: 64, Issue:8, 2021
[no title available]Journal of medicinal chemistry, , 05-13, Volume: 64, Issue:9, 2021
N-phenyl ureidobenzenesulfonates, a novel class of promising human dihydroorotate dehydrogenase inhibitors.Bioorganic & medicinal chemistry, , 11-15, Volume: 28, Issue:22, 2020
A carboxylic acid isostere screen of the DHODH inhibitor Brequinar.Bioorganic & medicinal chemistry letters, , 11-15, Volume: 30, Issue:22, 2020
Bifunctional Naphtho[2,3-Journal of medicinal chemistry, , 07-23, Volume: 63, Issue:14, 2020
Dihydroorotate dehydrogenase inhibitors in anti-infective drug research.European journal of medicinal chemistry, , Dec-01, Volume: 183, 2019
Ligand-based design, synthesis and biochemical evaluation of potent and selective inhibitors of Schistosoma mansoni dihydroorotate dehydrogenase.European journal of medicinal chemistry, , Apr-01, Volume: 167, 2019
Targeting Myeloid Differentiation Using Potent 2-Hydroxypyrazolo[1,5- a]pyridine Scaffold-Based Human Dihydroorotate Dehydrogenase Inhibitors.Journal of medicinal chemistry, , Jul-26, Volume: 61, Issue:14, 2018
Design, Synthesis, and Biological Evaluation of 4-Quinoline Carboxylic Acids as Inhibitors of Dihydroorotate Dehydrogenase.Journal of medicinal chemistry, , 06-28, Volume: 61, Issue:12, 2018
Synthesis, structure-activity relationship and binding mode analysis of 4-thiazolidinone derivatives as novel inhibitors of human dihydroorotate dehydrogenase.MedChemComm, , Jun-01, Volume: 8, Issue:6, 2017
Development of ML390: A Human DHODH Inhibitor That Induces Differentiation in Acute Myeloid Leukemia.ACS medicinal chemistry letters, , Dec-08, Volume: 7, Issue:12, 2016
Original 2-(3-alkoxy-1H-pyrazol-1-yl)pyrimidine derivatives as inhibitors of human dihydroorotate dehydrogenase (DHODH).Journal of medicinal chemistry, , Jan-22, Volume: 58, Issue:2, 2015
Original 2-(3-Alkoxy-1H-pyrazol-1-yl)azines Inhibitors of Human Dihydroorotate Dehydrogenase (DHODH).Journal of medicinal chemistry, , Jul-23, Volume: 58, Issue:14, 2015
Benzimidazole derivatives as potential dual inhibitors for PARP-1 and DHODH.Bioorganic & medicinal chemistry, , Aug-01, Volume: 23, Issue:15, 2015
SAR Based Optimization of a 4-Quinoline Carboxylic Acid Analog with Potent Anti-Viral Activity.ACS medicinal chemistry letters, , Jun-13, Volume: 4, Issue:6, 2013
On dihydroorotate dehydrogenases and their inhibitors and uses.Journal of medicinal chemistry, , Apr-25, Volume: 56, Issue:8, 2013
Discovery of novel inhibitors for DHODH via virtual screening and X-ray crystallographic structures.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 20, Issue:6, 2010
Dual binding mode of a novel series of DHODH inhibitors.Journal of medicinal chemistry, , Feb-23, Volume: 49, Issue:4, 2006
Biphenyl-4-ylcarbamoyl thiophene carboxylic acids as potent DHODH inhibitors.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 16, Issue:2, 2006
Bifunctional Naphtho[2,3-Journal of medicinal chemistry, , 07-23, Volume: 63, Issue:14, 2020
Dihydroorotate dehydrogenase inhibitors in anti-infective drug research.European journal of medicinal chemistry, , Dec-01, Volume: 183, 2019
Ligand-based design, synthesis and biochemical evaluation of potent and selective inhibitors of Schistosoma mansoni dihydroorotate dehydrogenase.European journal of medicinal chemistry, , Apr-01, Volume: 167, 2019
On dihydroorotate dehydrogenases and their inhibitors and uses.Journal of medicinal chemistry, , Apr-25, Volume: 56, Issue:8, 2013
Design and synthesis of potent inhibitors of the malaria parasite dihydroorotate dehydrogenase.Journal of medicinal chemistry, , Jan-25, Volume: 50, Issue:2, 2007
High-throughput screening for potent and selective inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase.The Journal of biological chemistry, , Jun-10, Volume: 280, Issue:23, 2005
Recent advances of human dihydroorotate dehydrogenase inhibitors for cancer therapy: Current development and future perspectives.European journal of medicinal chemistry, , Mar-15, Volume: 232, 2022
Cerpegin-derived furo[3,4-c]pyridine-3,4(1H,5H)-diones enhance cellular response to interferons by de novo pyrimidine biosynthesis inhibition.European journal of medicinal chemistry, , Jan-15, Volume: 186, 2020
Biphenyl-4-ylcarbamoyl thiophene carboxylic acids as potent DHODH inhibitors.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 16, Issue:2, 2006
SAR, species specificity, and cellular activity of cyclopentene dicarboxylic acid amides as DHODH inhibitors.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 15, Issue:21, 2005
Cerpegin-derived furo[3,4-c]pyridine-3,4(1H,5H)-diones enhance cellular response to interferons by de novo pyrimidine biosynthesis inhibition.European journal of medicinal chemistry, , Jan-15, Volume: 186, 2020
Synthesis of 2-,4,-6-, and/or 7-substituted quinoline derivatives as human dihydroorotate dehydrogenase (hDHODH) inhibitors and anticancer agents: 3D QSAR-assisted design.Bioorganic & medicinal chemistry letters, , 04-01, Volume: 29, Issue:7, 2019
Design, synthesis and pharmacological evaluation of novel substituted quinoline-2-carboxamide derivatives as human dihydroorotate dehydrogenase (hDHODH) inhibitors and anticancer agents.European journal of medicinal chemistry, , Jul-23, Volume: 82, 2014
Structure-activity relationships (SAR) of some tetracyclic heterocycles related to the immunosuppressive agent Brequinar Sodium.Bioorganic & medicinal chemistry letters, , Feb-03, Volume: 8, Issue:3, 1998
Heteroatom- and carbon-linked biphenyl analogs of Brequinar as immunosuppressive agents.Bioorganic & medicinal chemistry letters, , Jul-07, Volume: 8, Issue:13, 1998
In vitro resistance selections for Plasmodium falciparum dihydroorotate dehydrogenase inhibitors give mutants with multiple point mutations in the drug-binding site and altered growth.The Journal of biological chemistry, , Jun-27, Volume: 289, Issue:26, 2014
Fluorine modulates species selectivity in the triazolopyrimidine class of Plasmodium falciparum dihydroorotate dehydrogenase inhibitors.Journal of medicinal chemistry, , Jun-26, Volume: 57, Issue:12, 2014
Identification of a metabolically stable triazolopyrimidine-based dihydroorotate dehydrogenase inhibitor with antimalarial activity in mice.Journal of medicinal chemistry, , Apr-09, Volume: 52, Issue:7, 2009
A novel series of teriflunomide derivatives as orally active inhibitors of human dihydroorotate dehydrogenase for the treatment of colorectal carcinoma.European journal of medicinal chemistry, , Aug-05, Volume: 238, 2022
[no title available]Journal of medicinal chemistry, , 01-13, Volume: 65, Issue:1, 2022
[no title available]Journal of medicinal chemistry, , 09-23, Volume: 64, Issue:18, 2021
Lead Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series for the Treatment of Malaria.Journal of medicinal chemistry, , 05-14, Volume: 63, Issue:9, 2020
Cerpegin-derived furo[3,4-c]pyridine-3,4(1H,5H)-diones enhance cellular response to interferons by de novo pyrimidine biosynthesis inhibition.European journal of medicinal chemistry, , Jan-15, Volume: 186, 2020
Dihydroorotate dehydrogenase inhibitors in anti-infective drug research.European journal of medicinal chemistry, , Dec-01, Volume: 183, 2019
Ligand-based design, synthesis and biochemical evaluation of potent and selective inhibitors of Schistosoma mansoni dihydroorotate dehydrogenase.European journal of medicinal chemistry, , Apr-01, Volume: 167, 2019
Targeting Myeloid Differentiation Using Potent 2-Hydroxypyrazolo[1,5- a]pyridine Scaffold-Based Human Dihydroorotate Dehydrogenase Inhibitors.Journal of medicinal chemistry, , Jul-26, Volume: 61, Issue:14, 2018
Design, synthesis and inhibitory activity against human dihydroorotate dehydrogenase (hDHODH) of 1,3-benzoazole derivatives bearing amide units.Bioorganic & medicinal chemistry letters, , 07-01, Volume: 26, Issue:13, 2016
Novel Diketopiperazine Dihydroorotate Dehydrogenase Inhibitors Purified from Traditional Tibetan Animal Medicine Osteon Myospalacem Baileyi.Chemical biology & drug design, , Volume: 86, Issue:4, 2015
Original 2-(3-alkoxy-1H-pyrazol-1-yl)pyrimidine derivatives as inhibitors of human dihydroorotate dehydrogenase (DHODH).Journal of medicinal chemistry, , Jan-22, Volume: 58, Issue:2, 2015
Design, synthesis, X-ray crystallographic analysis, and biological evaluation of thiazole derivatives as potent and selective inhibitors of human dihydroorotate dehydrogenase.Journal of medicinal chemistry, , Feb-12, Volume: 58, Issue:3, 2015
Original 2-(3-Alkoxy-1H-pyrazol-1-yl)azines Inhibitors of Human Dihydroorotate Dehydrogenase (DHODH).Journal of medicinal chemistry, , Jul-23, Volume: 58, Issue:14, 2015
Fluorine modulates species selectivity in the triazolopyrimidine class of Plasmodium falciparum dihydroorotate dehydrogenase inhibitors.Journal of medicinal chemistry, , Jun-26, Volume: 57, Issue:12, 2014
Novel selective and potent inhibitors of malaria parasite dihydroorotate dehydrogenase: discovery and optimization of dihydrothiophenone derivatives.Journal of medicinal chemistry, , Oct-24, Volume: 56, Issue:20, 2013
Discovery of diverse human dihydroorotate dehydrogenase inhibitors as immunosuppressive agents by structure-based virtual screening.Journal of medicinal chemistry, , Oct-11, Volume: 55, Issue:19, 2012
Biaryl analogues of teriflunomide as potent DHODH inhibitors.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 21, Issue:24, 2011
Structure-based design, synthesis, and characterization of inhibitors of human and Plasmodium falciparum dihydroorotate dehydrogenases.Journal of medicinal chemistry, , May-14, Volume: 52, Issue:9, 2009
Design and synthesis of potent inhibitors of the malaria parasite dihydroorotate dehydrogenase.Journal of medicinal chemistry, , Jan-25, Volume: 50, Issue:2, 2007
SAR, species specificity, and cellular activity of cyclopentene dicarboxylic acid amides as DHODH inhibitors.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 15, Issue:21, 2005
New dermatological agents for the treatment of psoriasis.Journal of medicinal chemistry, , Feb-01, Volume: 44, Issue:3, 2001
Enables
This protein enables 4 target(s):
| Target | Category | Definition |
|---|
| dihydroorotase activity | molecular function | Catalysis of the reaction: (S)-dihydroorotate + H2O = N-carbamoyl-L-aspartate + H+. [EC:3.5.2.3, RHEA:24296] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| dihydroorotate dehydrogenase (quinone) activity | molecular function | (S)-dihydroorotate + a quinone = orotate + a quinol. [RHEA:30187] |
| dihydroorotate dehydrogenase activity | molecular function | Catalysis of the reaction: (S)-dihydroorotate + A = AH(2) + orotate. [RHEA:18073] |
Located In
This protein is located in 4 target(s):
| Target | Category | Definition |
|---|
| nucleoplasm | cellular component | That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653] |
| mitochondrion | cellular component | A semiautonomous, self replicating organelle that occurs in varying numbers, shapes, and sizes in the cytoplasm of virtually all eukaryotic cells. It is notably the site of tissue respiration. [GOC:giardia, ISBN:0198506732] |
| mitochondrial inner membrane | cellular component | The inner, i.e. lumen-facing, lipid bilayer of the mitochondrial envelope. It is highly folded to form cristae. [GOC:ai] |
| cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|
| mitochondrial inner membrane | cellular component | The inner, i.e. lumen-facing, lipid bilayer of the mitochondrial envelope. It is highly folded to form cristae. [GOC:ai] |
Involved In
This protein is involved in 4 target(s):
| Target | Category | Definition |
|---|
| UDP biosynthetic process | biological process | The chemical reactions and pathways resulting in the formation of UDP, uridine (5'-)diphosphate. [ISBN:0198506732] |
| 'de novo' UMP biosynthetic process | biological process | The chemical reactions and pathways resulting in the formation of UMP, uridine monophosphate, starting with the synthesis of (S)-dihydroorotate from bicarbonate; UMP biosynthesis may either occur via reduction by quinone, NAD+ or oxygen. [GOC:ecd, GOC:jl] |
| pyrimidine ribonucleotide biosynthetic process | biological process | The chemical reactions and pathways resulting in the formation of a pyrimidine ribonucleotide, a compound consisting of nucleoside (a pyrimidine base linked to a ribose sugar) esterified with a phosphate group at either the 3' or 5'-hydroxyl group of the sugar. [GOC:go_curators, ISBN:0198506732] |
| 'de novo' pyrimidine nucleobase biosynthetic process | biological process | The chemical reactions and pathways resulting in the formation of pyrimidine nucleobases, 1,3-diazine, organic nitrogenous bases, beginning with the synthesis of a pyrimidine ring from simpler precursors. [GOC:mah, ISBN:0716720094] |