mura-in-1

MurA-IN-1 (compound 1a) is a PTPRR inhibitor, with IC50 values of 0.23 μM, 0.8 μM, 0.75 μM and 0.09 μM for PTP1B, PTPN5, PTPN7 and PTPRR, respectively[1]. (A family of human MAPK-specific protein tyrosine phosphatases) [1]. Jeyanthy Eswaran, et al. Crystal structures and inhibitor identification for PTPN5, PTPRR and PTPN7: a family of human MAPK-specific protein tyrosine phosphatases. Biochem J. 2006 May 1;395(3):483-91.

Feglymycin is a 13-amino acid peptide originally isolated from Streptomyces that has antibacterial and antiviral activities. It is active against Gram-positive bacteria (MICs = 32-64 μg/ml) and inhibits HIV viral replication in H9 cells (IC50 = ~5 μM). Feglymycin is also active against clinical isolates of HIV-1 from clades A-D, A/E, and G (EC50s = 0.5-6.7 μM). It interacts with gp120 and inhibits HIV-1 NL4.3 binding to human soluble CD4 (EC50 = 4.4 μM) and to CD4+ SupT1 T cells by 74.5% when used at a concentration of 10.5 μM. Feglymycin inhibits the E. coli peptidoglycan biosynthesis enzymes MurA and MurC (Kis = 3.4 and 0.3 μM, respectively) in a noncompetitive manner.

MurA-IN-2 (compound 37) 是一种含有伯胺的氯乙酰胺片段，它是一种有效的 MurA 抑制剂，其 IC50值为 39 μM。MurA-IN-2 具有抗菌活性，抑制细菌细胞壁合成。

MurA-IN-3为基于吡咯烷二酮的MurA可逆抑制剂，对MurA展现出抑制活性，IC50为4.5 μM，并具备抗菌活性。

MurA-IN-4是一种具有抗细菌活性的MurA抑制剂，能够抑制细菌细胞壁的合成。