fucosyltransferase

SGN-2FF is an oral fucosylation inhibitor and inhibits fucosyltransferase activity, and has antitumor activity.

2F-Peracetyl-Fucose (1,3,4-Tri-O-acetyl-2-deoxy-2-fluoro-L-fucopyranos) is a potent fucosyltransferase (FUT) inhibitor that suppresses salivary acidification and fucosylation in an in vitro inflammatory model.

Alpha-1,3/4-Fucosyltransferase (α1,3/4FucT) (Hp3/4FT) is found in Helicobacter pylori and catalyzes the transfer of fucose from donor GDP-beta-l-fucose to the GlcNAc [1].

Fucosyltransferase 2 (EC:2.4.1.69; FUT2) attaches fucose to the terminal galactose of a type I chain via an α1-2 linkage.

Fucosyltransferase 8 (EC:2.4.1.68; FUT8; α1-6FucT) is a glycosyltransferase that catalyzes the transfer of fucose residues from GDP-fucose to the innermost N-acetylglucosamine residue of N-glycans.

Fucosyltransferase 9 (EC:2.4.1.152, FUT9) catalyzes the final step in the biosynthesis of Lewis antigens by adding fucose to precursor polysaccharides. FUT9 synthesizes the LeX oligosaccharide (CD15).

Protein O-Fucosyltransferase 1 (EC:2.4.1.221; POFUT1) is a glycosyltransferase characterized by cysteine-rich motifs serving as receptor sugars and GDP as the donor.

Fucosyltransferase 3 (EC:2.4.1.65, FUT3, FT3B) exhibits potent α 1-3 and α 1-4 fucosyltransferase activity.

Fucosyltransferase 5 (EC:2.4.1.65, Fucosyltransferase 5, Fucosyltransferase V) is responsible for the final step in the synthesis of Lex, sialy-Lex, and Lea antigens.

Focusyltransferase 7 (FUT7) is a Golgi stack membrane protein. It catalyzes the final fucosylation step in the synthesis of Lewis antigens, resulting in the production of the specific glycosylated product sialyl Lewis X (sLeX). FUT7 is involved in catalyzing the α-1,3 glycosidic bond, which is crucial for sialyl Lewis X antigen expression.

Fucosyltransferase 11 (EC:2.4.1.-, FUT11) attaches α-L-fucose to glycoprotein substrates, specifically on asialoglycoprotein glycans and biantennary N-glycan acceptors. This enzyme is significant in the field of oncology.

FUT8-IN-1 (Compound 37) is an inhibitor of α-1,6-fucosyltransferase (FUT8), with a dissociation constant (KD) of 49 nM and an IC50 around 50 µM. In the presence of FUT8, FUT8-IN-1 forms a highly active naphthoquinone imine intermediate, thereby inhibiting FUT8's enzymatic activity.

Mer-NF5003F (Stachybotrydial; F 1839M) is a sesquiterpene isolated from Stachybotrys, effective in inhibiting avian myeloblastosis virus (AMV) protease with an IC50 of 7.8 μM. It also inhibits sialyltransferases ST6N, ST3O, and ST3N with IC50 values of 0.61, 6.7, and 10 μg/mL, respectively, and fucosyltransferase with an IC50 of 11.3 μg/mL. Additionally, Mer-NF5003F exhibits in vitro activity against herpes simplex virus HSV-1 (IC50=4.32 μg/mL) and multi-drug-resistant Plasmodium falciparum K1 strain (IC50=0.85 μg/mL).

Lacto-N-biose I, also known as Galβ1-3GlcNAc, is a naturally occurring metabolite that serves as a substrate for the α1,2-fucosyltransferase enzyme derived from Helicobacter pylori[1].

FDW028 is a selective and potent fucosyltransferase 8 (FUT8) inhibitor with anti-tumor activity that drives B7-H3 lysosomal degradation via defucosylation and CMA pathways. FUT8 can be used to study metastatic colorectal cancer (mCRC).

Inebilizumab(FUT8-KO) is a modified version of inebilizumab that features a knocked-out fucosyltransferase 8 gene (FUT8). This anti-CD19 monoclonal antibody (mAb) exhibits enhanced antibody-dependent cell-mediated cytotoxicity against B cells, making it suitable for research into multiple sclerosis and neuromyelitis optica.

Petosemtamab (FUT8-KO) is a variant of Petosemtamab with the fucosyltransferase 8 gene (FUT8) knocked out. Petosemtamab is a monoclonal antibody (mAb) targeting EGFR (with a Kd of 0.22 nM) and LGR5 (with a Kd of 0.86 nM). This antibody disrupts EGFR signaling and causes receptor degradation in LGR5+ cancer cells. It is applicable in research on solid tumors such as head and neck squamous cell carcinoma (HNSCC) and metastatic colorectal cancer (CRC).

Osemitamab (FUT8-KO) is a monoclonal antibody targeting claudin-18.2, expressed in CHO cells with a knockout of the fucosyltransferase 8 gene (FUT8). The absence of fucose heightens the antibody's ADCC effect. When combined with Capecitabine and Oxaliplatin, it can be used for G/GEJ cancer research.