908567-47-5Relevant academic research and scientific papers
Phenotypic Discovery of SB1501, an Anti-obesity Agent, through Modulating Mitochondrial Activity
Jo, Ala,Kim, Mingi,Kim, Jong In,Ha, Jaeyoung,Hwang, Yoon Soo,Nam, Hyunsung,Hwang, Injae,Kim, Jae Bum,Park, Seung Bum
supporting information, p. 1104 - 1115 (2021/03/16)
Obesity has become a pandemic that threatens the quality of life and discovering novel therapeutic agents that can reverse obesity and obesity-related metabolic disorders are necessary. Here, we aimed to identify new anti-obesity agents using a phenotype-based approach. We performed image-based high-content screening with a fluorogenic bioprobe (SF44), which visualizes cellular lipid droplets (LDs), to identify initial hit compounds. A structure-activity relationship study led us to yield a bioactive compound SB1501, which reduces cellular LDs in 3T3-L1 adipocytes without cytotoxicity. SB1501 induced the expression of gene products that regulate mitochondrial biogenesis and fatty acid oxidation in 3T3-L1 adipocytes. Daily treatment with SB1501 improved the metabolic states of db/db mice by reducing body fat mass, adipose tissue mass, food intake, and increasing glucose tolerance. The anti-obesity effect of SB1501 may result from perturbation of the PGC-1α–UCP1 regulatory axis in inguinal white adipose tissue and brown adipose tissue. These data suggest the therapeutic potential of SB1501 as an anti-obesity agent via modulating mitochondrial activities.
Concise and diversity-oriented synthesis of novel scaffolds embedded with privileged benzopyran motif
Ko, Sung Kon,Jang, Hwan Jong,Kim, Eunha,Park, Seung Bum
, p. 2962 - 2964 (2008/09/19)
A branching DOS strategy for an unbiased natural product-like library with embedded privileged benzopyran motif was established to provide complexity and diversity of resulting heterocycles with desired drug-likeness. The importance of skeletal diversity
