garft

Pelitrexol (AG 2037) is a glycinamide ribonucleotide formyltransferase (GARFT) inhibitor.

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 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.

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

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.

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

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

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].

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

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.