Targeted Protein Degradation of NUDT5 Dissociates Catalytic Inhibition from Protein Loss in 6-Thioguanine Response [PDF]
6-Thioguanine (6-TG) is an FDA-approved antimetabolite drug that is widely used clinically, including for the treatment of leukemia. Its cellular effects require metabolic activation and are regulated through interactions with various proteins such as ...
Anne-Sophie M. C. Marques +13 more
doaj +2 more sources
6-Thioguanine in Children With Acute Lymphoblastic Leukaemia: Influence of Food on Parent Drug Pharmacokinetics and 6-Thioguanine Nucleotide Concentrations [PDF]
Aims Since relatively little is known about the pharmacokinetics of 6‐thioguanine (6TG) in children receiving 6‐thioguanine for maintenance therapy of acute lymphoblastic leukaemia (ALL), we studied plasma drug concentrations under standardized conditions and investigated the effect of food on parent drug pharmacokinetics and the accumulation of the ...
Lynne Lennard, J S Lilleyman
exaly +3 more sources
Nudix hydrolase 15 deficiency and azathioprine toxicity in a liver transplant recipient: A case report [PDF]
Abstract Thiopurines, such as azathioprine (AZA), are among the immunosuppressants used to prevent allograft rejection. Thiopurines are metabolized by thiopurine S‐methyltransferase (TPMT) and nudix hydrolase 15 (NUDT15) enzymes, and their functions are highly influenced by genetic variation. We present a 6‐year‐old female with recurrent acute cellular
Nguyen J +4 more
europepmc +2 more sources
Measurements of 6-thioguanine nucleotide levels with TPMT and NUDT15 genotyping in patients with Crohn's disease. [PDF]
The association between the 6-thioguanine nucleotide (6-TGN) level and clinical remission in Crohn's disease (CD) remains controversial. Thiopurine-induced leukopenia is a life-threatening complication of CD in Asians that was recently shown to strongly ...
Ji Hyeon Lee +8 more
doaj +2 more sources
6-thioguanine: a drug with unrealized potential for cancer therapy. [PDF]
AbstractSixty years ago, 6-thioguanine (6-TG) was introduced into the clinic. We suggest its full potential in therapy may not have been reached. In this paper, we contrast 6-TG and the more widely used 6-mercaptopurine; discuss 6-TG metabolism, pharmacokinetics, dosage and schedule; and summarize many of the early studies that have shown infrequent ...
Munshi PN, Lubin M, Bertino JR.
europepmc +4 more sources
Purine and pyrimidine analogs differentially regulate cell wall precursor biosynthesis to control β-lactam susceptibility in methicillin-resistant Staphylococcus aureus [PDF]
Maintaining the efficacy of β-lactam antibiotics against Staphylococcus aureus is a clinical priority given the prevalence of methicillin-resistant S. aureus (MRSA).
Aaron C. Nolan +3 more
doaj +2 more sources
Maintenance therapy containing methotrexate and 6-mercapto - purine is essential to cure acute lymphoblastic leukemia (ALL). Cytotoxicity is elicited by incorporation of thioguanine nucleotides into DNA (DNA-TG), and higher leukocyte DNA-TG is ...
Rikke Hebo Larsen +17 more
doaj +1 more source
Au Nanoparticle Loaded with 6-Thioguanine Anticancer Drug as a New Strategy for Drug Delivery [PDF]
In this study we suggested a new strategy for drug delivery of 6-thioguanine (6-TG) as a cancer drug by loading of this thiolic drug at a surface of Au nanoparticles. For this goal, we synthesized Au nanoparticle (Au/NPs) by reduction of tetrachloroauric
Hassan Karimi-Maleh +4 more
doaj +1 more source
Excited State Dynamics of 6-Thioguanine [PDF]
Here we present the excited state dynamics of jet-cooled 6-thioguanine (6-TG), using resonance-enhanced multiphoton ionization (REMPI), IR-UV double resonance spectroscopy, and pump-probe spectroscopy in the nanosecond and picosecond time domains. We report data on two thiol tautomers, which appear to have different excited state dynamics.
Siouri, Faady M +3 more
openaire +4 more sources
A sensitive electrochemical sensor was developed using reduced graphene oxide RGO-Cu2O/Fe2O3 nanocomposite for 6-mercaptopurine detection based on a facile fabrication method.
Fatemeh Irannezhad +2 more
doaj +1 more source

