34020-33-2

Usage

Uses

Used in Pharmaceutical Industry:
5-Guanylic acid, 6-S-methyl-6-thiois used as a pharmaceutical compound for its immunosuppressant activity. It is particularly relevant for biological studies focusing on the development of new treatments for conditions involving immune system dysregulation.
Used in Research and Development:
In the field of research and development, 5-Guanylic acid, 6-S-methyl-6-thioserves as a valuable tool for scientists to study the mechanisms of immune response and the potential for modulating these responses. This can lead to the discovery of new therapeutic strategies and the development of novel drugs targeting specific immune-related conditions.
Used in Diagnostic Applications:
5-Guanylic acid, 6-S-methyl-6-thiomay also find use in the development of diagnostic tools and tests, particularly those related to immune system function. Its unique properties could be harnessed to create sensitive and specific assays for detecting immune-related biomarkers or for monitoring the effectiveness of immunosuppressive therapies.

Upstream product

• 15867-02-4 6-thioguanosine-5'-monophosphate 

Relevant academic research and scientific papers

Methylation of mercaptopurine, thioguanine, and their nucleotide metabolites by heterologously expressed human thiopurine S-methyltransferase

Thiopurine S-methyltransferase (TPMT), a cytosolic enzyme that exhibits genetic polymorphism, catalyzes S-methylation of mercaptopurine (MP) and thioguanine (TG), yielding S-methylated nucleobases that are inactive, whereas S-methylated nucleotides of these thiopurines are cytotoxic. A yeast- based heterologous expression system was therefore used to characterize human TPMT-catalyzed methylation of MP, TG, and their principal nucleotide metabolites [thioinosine monophosphate (TIMP) and thioguanosine monophosphate (TGMP), respectively]. MP, TG, TIMP, and TGMP were all substrates for human TPMT, exhibiting similar Michaelis-Menten kinetic parameters (K(m), 10.6- 27.1 μM; V(max), 31-59 nmol/min/mg of TPMT). Consistent with these kinetic parameters, human leukemia cells (CEM) incubated for 24 hr with 10 μM MP or TG accumulated significantly higher (2.3-fold, p = 0.01) concentrations of methyl-TIMP after MP incubation than methyl-TGMP after TG incubation, due to the 2.7-fold higher concentration of TIMP after MP incubation, compared with TG nucleotides (TGN) after TG incubation. Moreover, intracellular accumulation of TGN was 2.5-fold greater after TG incubation than after MP incubation (p = 0.01). These data establish that MP, TG, and their principal nucleotide metabolites are comparable substrates for polymorphic TPMT, and they demonstrate significant differences in the accumulation of active TGN and methylated nucleotides when leukemia cells are treated with MP versus TG.