ribonucleotide

Caracemide (NSC-253272) inhibits the enzyme ribonucleotide reductase of Escherichia coli and can be utilized in anticancer studies.

COH29 (RNR Inhibitor COH29) is an orally available, aromatically substituted thiazole and human ribonucleotide reductase (RNR) inhibitor with potential antineoplastic activity. COH29 binds to the ligand-binding pocket of the RNR M2 subunit (hRRM2) near the C-terminal tail, decreasing the pool of deoxyribonucleotide triphosphates needed for DNA synthesis, leading to cell cycle arrest and growth inhibition. It may also inhibit the nuclear enzyme poly (ADP-ribose) polymerase (PARP) 1, preventing DNA repair, causing accumulation of DNA breaks, and inducing apoptosis.

5-Aminoimidazole ribonucleotide sodium (AIR) is an intermediate in purine biosynthesis. It undergoes further enzymatic modification to eventually form inosine monophosphate (IMP), which can then be converted into the purine bases adenine (A) and guanine (G). 5-Aminoimidazole ribonucleotide sodium is considered an endogenous metabolite (endogenous metabolite).

5-Aminoimidazole ribonucleotide (AIR) serves as an intermediate in purine biosynthesis, undergoing enzymatic modifications to form inosine monophosphate (IMP), which is subsequently converted into the purine bases adenine (A) and guanine (G) [1].

Polydeoxyribonucleotide can improve secretion of various growth factors, promote collagen synthesis, and restore tensile strength of the Achilles tendon in a rat model with Achilles tendon injury.

LSN 3213128, anti-tumor activity. is a selective, nonclassical, orally bioavailable antifolate with potent and specific inhibitory activity for aminoimidazole-4-carboxamide ribonucleotide formyltransferase (AICARFT), with IC50 of 16 nM for AICARFT enzyme inhibiton and 19 nM in cells.

Lometrexol (LY 264618), an antipurine Antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol can further inhibit de novo purine synthesis, causing abnormal cell proliferation and Apoptosis, even cell cycle arrest. Lometrexol has anticancer activity. Lometrexol also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor.

AICAR monophosphate (Aica ribonucleotide) is a purine precursor with antineoplastic activity and can be used in studies about type 2 diabetes.

Clofarabine (Clofarex)m, a second generation purine nucleoside analog with antineoplastic activity, inhibits the enzymatic activities of ribonucleotide reductase (IC50 = 65 nM) and DNA polymerase.

Osalmid (Oxaphenamide) is a choleretic drug, inhibits ribonucleotide reductase activity by targeting ribonucleotide reductase small subunit M2 (RRM2).

5-Amino-3H-imidazole-4-Carboxamide (AICA) is an imidazole derivative and a metabolite of the antineoplastic agents BIC and DIC. It serves as a condensation agent in the preparation of nucleosides and nucleotides, and when compounded with orotic acid, it is used to treat liver diseases.

Cytidine 5'-diphosphate disodium (CDP sodium salt) produces CTP to support DNA and RNA biosynthesis and ribonucleotide reductase to produce dCMP.

Pyrimidine (Metadiazine)s are heterocyclic, six-membered, nitrogen-containing carbon ring structures, with uracil, cytosine and thymine being the basal structures of ribose-containing nucleosides (uridine, cytidine, and thymidine respectively), or deoxyribose-containing deoxynucleosides, and their corresponding ribonucleotides or deoxyribonucleotides. Pyrimidines serve essential functions in human metabolism as ribonucleotide bases in RNA (uracil and cytosine), and as deoxyribonucleotide bases in DNA (cytosine and thymine), and are linked by phosphodiester bridges to purine nucleotides in double-stranded DNA, in both the nucleus and the mitochondria. Pyrimidine activated sugars are also involved in polysaccharide and phospholipid synthesis, glucuronidation in detoxification processes, glycosylation of proteins and lipids and in the recently identified novel endothelium-derived vasoactive dinucleotides.

Histidine (abbreviated as His or H) is an alpha-amino acid. The L-isomer is one of the 22 proteinogenic amino acids, i.e., the building blocks of proteins. It is classified as a charged, polar because of the hydrophilic nature of the imidazole side chain.

Inosine 5'-monophosphate disodium salt hydrate (Inosine 5'-monophosphate disodium salt), or inosinic acid, is the ribonucleotide of hypoxanthine and the first nucleotide formed during purine synthesis.

Fludarabine Phosphate (NSC 312887 Phosphate) is the phosphate salt of a fluorinated nucleotide antimetabolite analog of the antiviral agent vidarabine (ara-A) with antineoplastic activity. Fludarabine phosphate is rapidly dephosphorylated to 2-fluoro-ara-A and then phosphorylated intracellularly by deoxycytidine kinase to the active triphosphate, 2-fluoro-ara-ATP. This metabolite may inhibit DNA polymerase alpha, ribonucleotide reductase, and DNA primase, thereby interrupting DNA synthesis and inhibiting tumor cell growth.

2'-Azido-2'-deoxyuridine (N3dUrd) is a ribonucleotide reductase inhibitor exhibiting anti-cancer activity.

LY 222306, a glycinamide ribonucleotide formyltransferase (GARFT) inhibitor, has a Ki of 0.77 nM.

Pelitrexol (AG2037) is a GARFT inhibitor, which can inhibit the activity of mTORC1, reduce intracellular guanine nucleotides and block the cell cycle in the s-phase, with antiproliferative activity, and can be used in non-small cell lung cancer.

Gemcitabine elaidate (CP-4126), is a lipophilic, unsaturated fatty acid ester derivative of gemcitabine (dFdC), an antimetabolite deoxynucleoside analogue, with potential antineoplastic activity. Upon hydrolysis intracellularly by esterases, the prodrug gemcitabine is converted into the active metabolites difluorodeoxycytidine di- and tri-phosphate (dFdCDP and dFdCTP) by deoxycytidine kinase. dFdCDP inhibits ribonucleotide reductase, thereby decreasing the deoxynucleotide pool available for DNA synthesis; dFdCTP is incorporated into DNA, resulting in DNA strand termination and apoptosis.

LY309887 is a potent inhibitor of glycinamide ribonucleotide formyltransferase (Ki: 6.5 nM) with antitumor activity.

3-AP (Triapine) is a novel inhibitor of the M2 subunit of ribonucleotide reductase (RR).

Guanazole, a triazole-derived antimetabolite, functions as an RNR inhibitor. This compound suppresses mammalian ribonucleotide reductase activity and DNA synthesis by eliminating tyrosyl radicals, thereby exhibiting cytostatic properties.

3-AP-Me is the dimethyl derivative of the ribonucleotide reductase inhibitor 3-AP (SML0568). It activates the endoplasmic reticulum (ER) stress pathway by promoting eIF2α phosphorylation and upregulating gene expression of transcription factors ATF4 and ATF6, thereby inducing apoptosis. Additionally, 3-AP-Me activates cellular stress kinases c-Jun N-terminal kinase (JNK) and p38 mitogen-activated protein kinase, leading to the upregulation of spliced mRNA variant XBP1. It is applicable in cancer research.