VNLG-152

VNLG-152 is a novel small molecule retinamide designed as a first-in-class dual degrader of MAP kinase-interacting serine/threonine-protein kinases MNK1 and MNK2. By promoting proteasomal degradation of these kinases (via upregulation of E3 ligase Synoviolin 1/SYVN1), it inhibits the phosphorylation of eIF4E, a key step in oncogenic mRNA translation initiation. This results in potent inhibition of both Mnk-eIF4E and mTORC1 signaling pathways, leading to suppression of tumor growth, metastasis, cell cycle progression, epithelial-mesenchymal transition (EMT), and pro-inflammatory cytokine/chemokine secretion. Preclinical studies have demonstrated efficacy against triple-negative breast cancer (TNBC), prostate cancer (including castration-resistant forms), acne vulgaris, psoriasis, ulcerative colitis, Crohn disease, inflammatory bowel diseases and other neoplasms[1][2][6][8]. The drug was developed by researchers at the University of Maryland School of Medicine with further development by Isoprene Pharmaceuticals.

Other names

retinamide VNLG-152