Tandem synthesis, cytotoxicity, and in silico study of new 1,3,4‐oxadiazoles as potential thymidylate synthase inhibitors
Sign Up to like & getrecommendations! Published in 2022 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.202200170
Abstract: A new series of pyrrole‐linked mono‐ and bis(1,3,4‐oxadiazole) hybrids, attached to various arene units, was prepared using a two‐step tandem protocol. Therefore, a benzohydrazide derivative was condensed with the appropriate aldehydes in ethanol at 80°C… read more here.
Keywords: inhibition percentages; thymidylate synthase; tandem synthesis; cytotoxicity ... See more keywords
Gastric cancer with microsatellite instability displays increased thymidylate synthase expression
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Surgical Oncology"
DOI: 10.1002/jso.26822
Abstract: Gastric cancer (GC) with microsatellite instability (MSI) is a less aggressive disease and associated with resistance to 5‐fluorouracil (5‐FU)‐based chemotherapy (CMT). Thymidylate synthase (TS) is inhibited by 5‐FU, and another potential mediator of therapeutic resistance… read more here.
Keywords: cancer microsatellite; microsatellite instability; thymidylate synthase; gastric cancer ... See more keywords
Molecular docking to Toxoplasma gondii thymidylate synthase-dihydrofolate reductase and efficacy of raltitrexed in infected mice
Sign Up to like & getrecommendations! Published in 2018 at "Parasitology Research"
DOI: 10.1007/s00436-018-5835-5
Abstract: Toxoplasmosis is a zoonosis of worldwide distribution. Currently, two drugs, pyrimethamine and sulfadiazine, are used as a reference in the treatment of toxoplasmosis, but the resistance of Toxoplasma gondii appears as a relevant public health… read more here.
Keywords: gondii thymidylate; gondii; thymidylate synthase; infected mice ... See more keywords
Synthesis, characterization and molecular docking studies of thiouracil derivatives as potent thymidylate synthase inhibitors and potential anticancer agents
Sign Up to like & getrecommendations! Published in 2017 at "Molecular Diversity"
DOI: 10.1007/s11030-017-9776-1
Abstract: Thymidylate synthase (TS), one of folate-dependent enzymes, is a key and well-recognized target for anticancer agents. In this study, a series of 6-aryl-5-cyano thiouracil derivatives were designed and synthesized in accordance with essential pharmacophoric features… read more here.
Keywords: anti proliferative; anticancer agents; thymidylate synthase; thiouracil derivatives ... See more keywords
Thymidylate synthase-catalyzed, tetrahydrofolate-dependent self-inactivation by 5-FdUMP.
Sign Up to like & getrecommendations! Published in 2019 at "Archives of biochemistry and biophysics"
DOI: 10.1016/j.abb.2019.108106
Abstract: In view of previous crystallographic studies, N4-hydroxy-dCMP, a slow-binding thymidylate synthase inhibitor apparently caused "uncoupling" of the two thymidylate synthase-catalyzed reactions, including the N5,10-methylenetetrahydrofolate one-carbon group transfer and reduction, suggesting the enzyme's capacity to use… read more here.
Keywords: synthase; hydroxy dcmp; synthase catalyzed; thymidylate synthase ... See more keywords
Mechanism of naphthoquinone selectivity of thymidylate synthase ThyX.
Sign Up to like & getrecommendations! Published in 2020 at "Biophysical journal"
DOI: 10.1016/j.bpj.2020.10.042
Abstract: Naphthoquinones (NQs) are natural and synthetic compounds with a wide range of biological activities commonly attributed to their redox activity and/or chemical reactivity. However, genetic and biochemical experiments have recently demonstrated that 2-hydroxy-NQs (2-OH-NQs) act… read more here.
Keywords: thymidylate synthase; thyx; mechanism; synthase thyx ... See more keywords
Characterization of Plasmodium knowlesi dihydrofolate reductase-thymidylate synthase and sensitivity to antifolates.
Sign Up to like & getrecommendations! Published in 2018 at "Parasitology international"
DOI: 10.1016/j.parint.2018.08.004
Abstract: Malaria caused by an infection of Plasmodium knowlesi can result in high parasitemia and deaths. Therefore, effective and prompt treatment is necessary to reduce morbidity and mortality. The study aims to characterize P. knowlesi dihydrofolate… read more here.
Keywords: sensitivity antifolates; reductase thymidylate; dihydrofolate reductase; knowlesi dihydrofolate ... See more keywords
Caught in Action: X-ray Structure of Thymidylate Synthase with Noncovalent Intermediate Analog.
Sign Up to like & getrecommendations! Published in 2021 at "Biochemistry"
DOI: 10.1021/acs.biochem.1c00063
Abstract: Methylation of 2-deoxyuridine-5'-monophosphate (dUMP) at the C5 position by the obligate dimeric thymidylate synthase (TSase) in the sole de novo biosynthetic pathway to thymidine 5'-monophosphate (dTMP) proceeds by forming a covalent ternary complex with dUMP… read more here.
Keywords: analog; dump; thymidylate synthase; structure ... See more keywords
The Oxidase Reaction of Flavin-Dependent Thymidylate Synthase Reveals the Nature of Inhibitor Binding.
Sign Up to like & getrecommendations! Published in 2025 at "Biochemistry"
DOI: 10.1021/acs.biochem.5c00510
Abstract: Escalating antimicrobial resistance presents an urgent need for novel antibiotics, particularly against Mycobacterium tuberculosis (M. tb), which claims 1.5 million lives annually. A promising avenue for antibiotic development is inhibiting DNA biosynthesis by targeting Thymidylate… read more here.
Keywords: reaction; flavin dependent; oxidase reaction; inhibitor ... See more keywords
Conformational Propensity and Biological Studies of Proline Mutated LR Peptides Inhibiting Human Thymidylate Synthase and Ovarian Cancer Cell Growth.
Sign Up to like & getrecommendations! Published in 2018 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.7b01699
Abstract: LR and [d-Gln4]LR peptides bind the monomer-monomer interface of human thymidylate synthase and inhibit cancer cell growth. Here, proline-mutated LR peptides were synthesized. Molecular dynamics calculations and circular dichroism spectra have provided a consistent picture… read more here.
Keywords: cell growth; thymidylate synthase; human thymidylate; cancer cell ... See more keywords
Structural Insight into Effective Inhibitors' Binding to Toxoplasma gondii Dihydrofolate Reductase Thymidylate Synthase.
Sign Up to like & getrecommendations! Published in 2022 at "ACS chemical biology"
DOI: 10.1021/acschembio.1c00627
Abstract: Pyrimethamine (Pyr), a known dihydrofolate reductase (DHFR) inhibitor, has long been used to treat toxoplasmosis caused by Toxoplasma gondii (Tg) infection. However, Pyr is effective only at high doses with associated toxicity to patients, calling… read more here.
Keywords: thymidylate synthase; gondii; toxoplasma gondii; dhfr ... See more keywords