target/transferase/1

Target 1 在生命科学相关研究中具有广泛的应用。

Gamma-Glutamyl Transferase-IN-1 (compound 4de) 是一种 β-羰基酰肼类抑制剂，靶向谷氨酰转移酶，具有抗真菌和抗菌活性。它通过促进活性氧积累、破坏细胞膜和失调组蛋白乙酰化来发挥作用。

Tunicamycin 15:1 is a mixture of tunicamycin structural isomers that contain a 15-carbon N-acyl chain with variable branching patterns. The N-acyl chain incorporated into tunicamycins, like tunicamycin 15:1, is derived from the same pool of cellular branched-chain fatty acids (BCFAs) inStreptomycesand directly impacts the biological activity of each individual tunicamycin variant.1,2,3Purified tunicamycin 15:1 withiso,anteiso, or a mixture ofisoandanteisobranching configurations inhibit bacterial phospho-MurNAc-pentapeptide transferase (MraY) with IC50values of 0.05, 0.36, and 0.09 μM, respectively.2 1.Price, N.P.J., Jackson, M.A., Hartman, T.M., et al.Branched chain lipid metabolism as a determinant of the N-Acyl variation of Streptomyces natural productsACS Chem. Biol.16(1)116-124(2021) 2.Hering, J., Dunevall, E., Snijder, A., et al.Exploring the active site of the antibacterial target MraY by modified tunicamycinsACS Chem Biol.15(11)2885-2895(2020) 3.Duksin, D., and Mahoney, W.C.Relationship of the structure and biological activity of the natural homologues of tunicamycinJ. Biol. Chem.257(6)3105-3109(1982)

Keap1-Nrf2-IN-9（compound 11）是一种有效Keap1-Nrf2PPI抑制剂，IC50为0.575 µM。该化合物能够提升Nrf2靶基因表达，涉及血红素加氧酶1 (Hmox1)、谷胱甘肽S转移酶P (GstP) 以及谷氨酸-半胱氨酸连接酶的催化(Gclc)与调节(Gclm)亚基。在ARPE19细胞中，Keap1-Nrf2-IN-9展现出无细胞毒活性。

Tunicamycin 17:1 is a mixture of tunicamycin structural isomers that contain a 17-carbon N-acyl chain with variable branching patterns. The N-acyl chain incorporated into tunicamycins, like tunicamycin 17:1, is derived from the same pool of cellular branched-chain fatty acids (BCFAs) inStreptomycesand directly impacts the biological activity of each individual tunicamycin variant.1,2,3Purified tunicamycin 17:1 withisooranteisobranching configurations inhibits bacterial phospho-MurNAc-pentapeptide transferase (MraY) with IC50values of 0.12 and 0.9 μM, respectively.2 1.Price, N.P.J., Jackson, M.A., Hartman, T.M., et al.Branched chain lipid metabolism as a determinant of the N-Acyl variation of Streptomyces natural productsACS Chem. Biol.16(1)116-124(2021) 2.Hering, J., Dunevall, E., Snijder, A., et al.Exploring the active site of the antibacterial target MraY by modified tunicamycinsACS Chem Biol.15(11)2885-2895(2020) 3.Duksin, D., and Mahoney, W.C.Relationship of the structure and biological activity of the natural homologues of tunicamycinJ. Biol. Chem.257(6)3105-3109(1982)