garft

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.

Pemetrexed (LY-231514 Disodium Hydrate), a guanine-derived antineoplastic agent, binds to and inhibits the enzyme thymidylate synthase (TS).

Pemetrexed disodium (LY-231514) is a parenterally administered folate antagonist and antineoplastic agent, used in the treatment of non-small cell lung cancer and malignant mesothelioma. Pemetrexed disodium therapy has been associated with moderate rates of serum enzyme elevations during therapy, but has not been convincingly linked to instances of acute, clinically apparent liver injury.

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.

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

Pemetrexed disodium hemipenta hydrate (LY-231514 Disodium Hydrate) is a new-type antifolate and antimetabolite for TS, DHFR, and GARFT. The Ki of Pemetrexed Disodium Hydrate for TS, DHFR and GARFT is 1.3 nM, 7.2 nM and 65 nM, respectively.

Pemetrexed disodium heptahydrate (LY231514) is an antifolate that inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinyl-adenosine 5'-monophosphate (GARMT) with K_i values of 1.3 nM, 7.2 nM, and 65 nM respectively. This inhibits the formation of precursor purine and pyrimidine nucleotides and cancer cell proliferation, making it suitable for research into pleural mesothelioma and non-small cell lung cancer (NSCLC).

LY 254155, an antifolate,binds to mFBP and inhibits hGARFT with Kis of 1.7±0.1 and 2.1±0.2 nM, respectively.

AG2034 is an inhibitor of the glycinamide ribonucleotide formyltransferase (GARFT).

Lometrexol hydrate (DDATHF hydrate) is an antipurine antifolate compound that inhibits glycinamide ribonucleotide formyltransferase (GARFT) activity without inducing detectable DNA strand breaks. It further disrupts de novo purine synthesis, leading to abnormal cell proliferation, apoptosis, and cell cycle arrest, exhibiting anticancer activity [1] [2]. Additionally, it acts as a potent inhibitor of human Serine hydroxymethyltransferase1/2 (h SHMT1/2) [3].

Lometrexol (DDATHF) disodium is a potent inhibitor of human serine hydroxymethyltransferase 1/2 (hSHMT1/2) and antifolate, which reduces the activity of glycinamide ribonucleotide formyltransferase (GARFT) without causing detectable levels of DNA strand breaks. Lometrexol disodium exhibits anticancer effects by inhibiting the de novo synthesis of purines, causing abnormal cell proliferation, apoptosis and cell cycle arrest.