Drug intelligence / Profile preview

3Fax-Neu5Ac

Development stage
Preclinical
Lead developer
Dana-Farber Cancer Institute
Modality
Small Molecules
Administration
Intratumoral, Intravenous, Parenteral
01

Overview

3Fax-Neu5Ac (3-fluorinated N-acetylneuraminic acid) is a cell-permeable small molecule that acts as a global inhibitor of sialyltransferases. It is a fluorinated analog of sialic acid that, upon entry into the cell, is metabolically activated to CMP-3F-Neu5Ac. This metabolite acts as a potent competitive inhibitor of various sialyltransferases in the Golgi apparatus, effectively blocking the sialylation of glycoproteins and glycolipids on the cell surface. In oncology research, particularly in multiple myeloma, 3Fax-Neu5Ac is utilized to reduce hypersialylation, thereby disrupting the interaction between sialic acids and inhibitory Siglec receptors (such as Siglec-6) on immune cells. This blockade helps to reverse immune dysfunction, activate plasmacytoid dendritic cells (pDCs), and enhance T-cell-mediated anti-tumor activity.

Other names
3-fluorinated N-acetylneuraminic acid3-fluoro-N-acetylneuraminic acid3-fluoro-sialic acidsialyltransferase inhibitor
02

Targets

ST (ST8 alpha-N-acetyl-neuraminide alpha-2,8-sialyltransferase 4)

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