901037-01-2Relevant academic research and scientific papers
Discovery of a novel noniminosugar acid α glucosidase chaperone series
Xiao, Jingbo,Motabar, Omid,Lea, Wendy A.,Hu, Xin,Zheng, Wei,Southall, Noel,Liu, Ke,Simeonov, Anton,Ferrer, Marc,Marugan, Juan J.,Westbroek, Wendy,Velayati, Arash,Gustafson, Ann Marie,Goldin, Ehud,Sidransky, Ellen,Tamargo, Rafael J.,Ribes, Antonia,Matalonga, Leslie
, p. 7546 - 7559,14 (2020/08/24)
Pompe disease is an autosomal recessive lysosomal storage disorder (LSD) caused by deficiency of the lysosomal enzyme acid α-glucosidase (GAA). Many disease-causing mutated GAA retain enzymatic activity but are not translocated from endoplasmic reticulum
Identification of inhibitors of NOD1-induced nuclear factor-κB activation
Khan, Pasha M.,Correa, Ricardo G.,Divlianska, Daniela B.,Peddibhotla, Satyamaheshwar,Sessions, E. Hampton,Magnuson, Gavin,Brown, Brock,Suyama, Eigo,Yuan, Hongbin,Mangravita-Novo, Arianna,Vicchiarelli, Michael,Su, Ying,Vasile, Stefan,Smith, Layton H.,Diaz, Paul W.,Reed, John C.,Roth, Gregory P.
, p. 780 - 785 (2011/12/02)
NOD1 (nucleotide-binding oligomerization domain 1) protein is a member of the NLR (NACHT and leucine rich repeat domain containing proteins) protein family, which plays a key role in innate immunity as a sensor of specific microbial components derived from bacterial peptidoglycans and induction of inflammatory responses. Mutations in NOD proteins have been associated with various inflammatory diseases that affect NF-κB (nuclear factor κB) activity, a major signaling pathway involved in apoptosis, inflammation, and immune response. A luciferase-based reporter gene assay was utilized in a high-throughput screening program conducted under the NIH-sponsored Molecular Libraries Probe Production Center Network program to identify the active scaffolds. Herein, we report the chemical synthesis, structure-activity relationship studies, downstream counterscreens, secondary assay data, and pharmacological profiling of the 2-aminobenzimidazole lead (compound 1c, ML130) as a potent and selective inhibitor of NOD1-induced NF-κB activation.
