transferase

OSMI-1 is an O-GlcNAc transferase (OGT) inhibitor (IC50=2.7 μM) that is orally active and cell-permeable. OSMI-1 inhibits protein O-GlcNA acetylation without qualitatively altering cell-surface N- or O- linked glycans.

FGTI-2734 is a dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT-1) inhibitor, exhibiting IC50 values of 250 nM and 520 nM for FT and GGT-1, respectively. It effectively prevents the membrane localization of KRAS, addressing the issue of KRAS resistance and inhibiting the growth of mutant KRAS patient-derived pancreatic tumors.

Cycloleucine is an antagonist of NMDA receptor associated glycine receptor with a Ki of 600 μM. Cycloleucine is also a competitive inhibitor of S-adenosyl-methionine mediated methylation with anxiolytic and cytostatic effects.

PD 128042 (CI 976) is a potent, orally active, and selective ACAT inhibitor (IC50: 73 nM) as well as a lysophospholipid acyltransferase (LPAT) inhibitor. CI 976 inhibits Golgi-associated LPAT activity (IC50: 15 μM) and multiple membrane trafficking steps.

Gamma-Glutamyl Transferase-IN-2 (compound 4dq), a β-carboline 1-hydrazide inhibitor, exhibits antifungal and antibacterial properties by targeting glutamyltransferase, inducing reactive oxygen species accumulation, compromising cell membranes, and disrupting histone acetylation processes [1].

Gamma-Glutamyl Transferase-IN-1 (compound 4de), a β-carboline 1-hydrazide inhibitor, exhibits antifungal and antibacterial properties by targeting glutamyltransferase, inducing reactive oxygen species accumulation, disrupting cell membranes, and dysregulating histone acetylation [1].

Phenylethanolamine N-methyl transferase, bovine, is a biocatalyst and a pivotal enzyme in emerging biocatalyst technology. Enzyme engineering focuses on improving reaction kinetics, substrate selectivity, and activity in extreme conditions (e.g., low or high pH). Modifying these enzymes to introduce stimulus responsiveness also enables dynamic control of their activity.

Glucosaminyl (N-acetyl) transferase 4 (GCNT4) is an enzyme significantly downregulated in gastric cancer and associated with poor prognosis. Overexpression of Glucosaminyl (N-acetyl) transferase 4 can inhibit cell proliferation and alter the cell cycle.

Glucosaminyl (N-acetyl) Transferase 1 (EC:2.4.1.102, GCNT1) is crucial for the formation of the Gal beta 1-3(GlcNAc beta 1-6)GalNAc structure and core 2 O-glycan branching and plays a significant role in cancer.

Glucosaminyl (N-acetyl) Transferase 2 (EC:2.4.1.150, GCNT2, GCNT5, NACGT1, N-acetyllactosaminide beta-1,6-N-acetylglucosaminyl-transferase, N-acetylglucosaminyltransferase, IGNT) is responsible for the formation of the I antigen in blood type and also plays a significant role in cancer.

Glycosyltransferase-IN-1 is a glycosyltransferase inhibitor with bacteriostatic activity, inhibiting MSSA, MRSA, Bacillus subtilis, and Enterobacteriaceae.

α-2,3-sialyltransferase-IN-1 (Lith-O-Asp analog) is an α-2,3-sialyltransferase inhibitor with anticancer activity. Vapendavir diphosphate inhibits EV71 replication.

Beta-1, 3-N-Acetylhexaminyltransferase (LgtA), a glycosyltransferase, plays a critical role in biochemical studies by catalyzing the transfer of N-acetylglucosamine from UDP-GlcNAc to substrates including N-acetyllactosamine and lactose [1].

Alpha-1,4-Galactosyltransferase (LgtC) (A4GALT), a glycosphingolipid-specific glycosyltransferase, catalyzes the transfer of a galactose molecule to the alpha-1,4 position on lactosylceramide, resulting in the formation of globotriaosylceramide. This enzyme plays a crucial role in the synthesis of P1 blood group antigens [1] [2].

Alpha-2,6-Sialyltransferase (Pd26ST) efficiently catalyzes the sialylation of both terminal and internal galactose and N-acetylgalactosamine residues, resulting in the production of terminal α2,6-sialosides [1].

ST6Sialyltransferase5 (EC:2.4.3.3, ST6GALNAC5, SIAT7E, ST6 N-acetylgalactosaminide alpha-2,6-sialyltransferase 5) transfers sialic acid to N-acetylgalactosamine (GalNAc) residues. It may serve as a biomarker in cervical screening samples.

Histone acetyltransferase p300 Inhibitor 4c is a 2-aminothiazole derivative. Histone acetyltransferase p300 Inhibitor 4c inhibited hCA I, hCA II, AChE and BChE with Ki values of 0.008 ± 0.001, 0.124 ± 0.017, 0.129 ± 0.030 and 0.083 ± 0.041 µM. 0.017, 0.129 ± 0.030 and 0.083 ± 0.041 μM.

Alpha-1,3-N-Acetylgalactosaminyltransferase (Pm1138) (EC 2.4.1.40(Pm1138)), also known as the ABO system transferase, exhibits glycosyl transferase activity [1].

Phosphate acetyltransferase, a transferase enzyme utilized in biochemical research, catalyzes the reversible acetylation of CoA from acetyl-P, yielding acetyl-CoA and inorganic phosphate. This process is integral to acetate assimilation dissimilation reactions [1].

Galactose-1-phosphate uridyl transferase catalyzes the second step of the Leloir pathway in galactose metabolism, facilitating the conversion of galactose into glucose. A deficiency in galactose-1-phosphate uridyl transferase results in classic galactosemia in humans, making it significant for research into metabolic diseases.

Diacylglycerol Acyltransferase Inhibitor-1, a diacylglycerol acyltransferase (DGAT1) inhibitor, effectively suppresses the activity of DGAT1.

Histone Acetyltransferase Inhibitor II is a selective and cell permeable inhibitor of p300 histone acetyltransferase(IC50 : 5 μM).with anti-acetylase activity in mammalian cells.

Purinephosphoribosyltransferase-IN-1 (Compound (S,R)-48) is a potent inhibitor of Plasmodium falciparum (Pf), Plasmodium vivax (Pv), and Trypanosoma brucei (Tbr) 6-oxopurine phosphate ribosyltransferase (PRT), with Ki values of 50 nM, 20 nM, and 2 nM, respectively.

Purine phosphoribosyltransferase-IN-2 is a potent inhibitor of Plasmodium falciparum (Pf), Plasmodium vivax (Pv), and Trypanosoma brucei (Tbr) 6-oxopurine phosphoribosyltransferase (PRT) with Ki values of 30, 20, and 2 nM, respectively.