A double‐blind, randomized, placebo‐controlled phase 2 trial evaluating the selective dihydroorotate dehydrogenase inhibitor vidofludimus calcium in relapsing‐remitting multiple sclerosis
Sign Up to like & getrecommendations! Published in 2022 at "Annals of Clinical and Translational Neurology"
DOI: 10.1002/acn3.51574
Abstract: Inhibition of dihydroorotate dehydrogenase suppresses magnetic resonance imaging brain lesions and disease activity in multiple sclerosis but has limiting tolerability. We assessed the safety and efficacy of vidofludimus calcium, a novel, selective dihydroorotate dehydrogenase inhibitor,… read more here.
Keywords: vidofludimus calcium; multiple sclerosis; dihydroorotate dehydrogenase;
Synthesis and biological evaluation of new quinoline‐4‐carboxylic acid‐chalcone hybrids as dihydroorotate dehydrogenase inhibitors
Sign Up to like & getrecommendations! Published in 2022 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.202200374
Abstract: Fourteen novel quinoline‐4‐carboxylic acid‐chalcone hybrids were obtained via Claisen–Schmidt condensation and evaluated as potential human dihydroorotate dehydrogenase (hDHODH) inhibitors. The ketone precursor 2 was synthesized by the Pfitzinger reaction and used for further derivatization at… read more here.
Keywords: carboxylic acid; acid chalcone; chalcone hybrids; dihydroorotate dehydrogenase ... See more keywords
Tetrahydro-1H,5H-pyrazolo[1,2-a]pyrazole-1-carboxylates as inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase.
Sign Up to like & getrecommendations! Published in 2019 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2019.102982
Abstract: The reactions between 5-substituted pyrazolidine-3-ones, aldehydes, and methyl methacrylate provided tetrahydropyrazolo[1,2-a]pyrazole-1-carboxylates as mixtures of syn- and anti-diastereomers. Testing for inhibition of dihydroorotate dehydrogenase of Plasmodium falciparum (PfDHODH) revealed high activity of some anti-isomers of the… read more here.
Keywords: pyrazolo pyrazole; pyrazole; pyrazole carboxylates; plasmodium falciparum ... See more keywords
Dihydroorotate dehydrogenase: A drug target for the development of antimalarials.
Sign Up to like & getrecommendations! Published in 2017 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2016.09.085
Abstract: Malaria is a critical human disease with extensive exploration yet unestablished due to occurrence of frequent drug resistance. This aspect of malaria pharmacology calls for the introduction of new antimalarial. The drugs reported till date… read more here.
Keywords: drug; drug target; dhodh; development ... See more keywords
Horizontal transfer of mitochondria and dihydroorotate dehydrogenase function in respiration recovery of mtDNA deficient cancer cells
Sign Up to like & getrecommendations! Published in 2018 at "Free Radical Biology and Medicine"
DOI: 10.1016/j.freeradbiomed.2018.04.177
Abstract: Recently, we showed that ρ0 cancer cells devoid of mitochondrial DNA (mtDNA) recover tumour formation ability only after acquisition of host mtDNA. In order to restore respiration, mtDNA moves between cells in whole mitochondria. While… read more here.
Keywords: recovery; mtdna; respiration; cancer cells ... See more keywords
Discovery of Antimalarial Azetidine-2-carbonitriles That Inhibit P. falciparum Dihydroorotate Dehydrogenase
Sign Up to like & getrecommendations! Published in 2017 at "ACS Medicinal Chemistry Letters"
DOI: 10.1021/acsmedchemlett.7b00030
Abstract: Dihydroorotate dehydrogenase (DHODH) is an enzyme necessary for pyrimidine biosynthesis in protozoan parasites of the genus Plasmodium, the causative agents of malaria. We recently reported the identification of novel compounds derived from diversity-oriented synthesis with… read more here.
Keywords: discovery antimalarial; antimalarial azetidine; azetidine carbonitriles; dihydroorotate dehydrogenase ... See more keywords
Inhibition of mitochondrial complex III or dihydroorotate dehydrogenase (DHODH) triggers formation of poly(A)+ RNA foci adjacent to nuclear speckles following activation of ATM (ataxia telangiectasia mutated)
Sign Up to like & getrecommendations! Published in 2022 at "RNA Biology"
DOI: 10.1080/15476286.2022.2146919
Abstract: ABSTRACT Intracellular and intercellular signalling networks play an essential role in optimizing cellular homoeostasis and are thought to be partly reflected in nuclear mRNA dynamics. However, the regulation of nuclear mRNA dynamics by intracellular and… read more here.
Keywords: rna; nuclear speckles; poly rna; complex iii ... See more keywords
Dihydroorotate dehydrogenase inhibitors in SARS‐CoV‐2 infection
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DOI: 10.1111/eci.13366
Abstract: Since late 2019, a severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) viral outbreak has spread all over the world. The disease caused by SARS-CoV-2, named COVID-19, has caused over 550,000 deaths and infected close to… read more here.
Keywords: dehydrogenase inhibitors; inhibitors sars; sars cov; cov infection ... See more keywords
Dihydroorotate dehydrogenase inhibitor olorofim has potent in vitro activity against Microascus/Scopulariopsis, Rasamsonia, Penicillium and Talaromyces species
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DOI: 10.1111/myc.13548
Abstract: Treatment options against infections caused by rare but emerging moulds may be limited by their reduced susceptibility or resistance to clinically available antifungals. The investigational antifungal olorofim, which targets the biosynthesis of pyrimidines within fungi,… read more here.
Keywords: dehydrogenase inhibitor; potent vitro; activity; olorofim potent ... See more keywords
Abstract C042: Inhibition of Dihydroorotate Dehydrogenase (DHODH) by RP7214 attenuates growth and promotes differentiation of AML cell lines
Sign Up to like & getrecommendations! Published in 2019 at "Molecular Cancer Therapeutics"
DOI: 10.1158/1535-7163.targ-19-c042
Abstract: Background: Dihydroorotate dehydrogenase (DHODH), a rate limiting enzyme in pyrimidine synthesis, is overexpressed in certain cancers; blockade of which impedes tumor cell proliferation via cell cycle arrest. RP7214 is a novel and potent DHODH inhibitor… read more here.
Keywords: aml cell; dihydroorotate dehydrogenase; cell; rp7214 ... See more keywords
Abstract 234: A novel, small molecule inhibitor of dihydroorotate dehydrogenase (DHODH), RP7214, potentiates activity of chemotherapeutics in breast and colorectal cancers
Sign Up to like & getrecommendations! Published in 2020 at "Cancer Research"
DOI: 10.1158/1538-7445.am2020-234
Abstract: Background: Dihydroorotate dehydrogenase (DHODH) is an enzyme which is critically involved in process of de novo pyrimidine biosynthesis. Therefore, it plays important roles in cell proliferation, mitosis and cellular metabolism. Importantly, overexpression of DHODH has… read more here.
Keywords: inhibitor; breast colorectal; rp7214; dhodh ... See more keywords