189250-15-5Relevant articles and documents
Design, Synthesis, and Characterization of Ogerin-Based Positive Allosteric Modulators for G Protein-Coupled Receptor 68 (GPR68)
Yu, Xufen,Huang, Xi-Ping,Kenakin, Terry P.,Slocum, Samuel T.,Chen, Xin,Martini, Michael L.,Liu, Jing,Jin, Jian
, p. 7557 - 7574 (2019/09/09)
G protein-coupled receptor 68 (GPR68) is an understudied orphan G protein-coupled receptor (GPCR). It is expressed most abundantly in the brain, potentially playing important roles in learning and memory. Pharmacological studies with GPR68 have been hinde
Screening for novel antimicrobials from encoded combinatorial libraries by using a two-dimensional agar format
Silen, Joy L.,Lu, Amy T.,Solas, Dennis W.,Gore, Medini A.,Maclean, Derek,Shah, Nikil H.,Coffin, Jill M.,Bhinderwala, Naseema S.,Wang, Yongwen,Tsutsui, Ken T.,Look, Gary C.,Campbell, David A.,Hale, Ron L.,Navre, Marc,Deluca-Flaherty, Camille R.
, p. 1447 - 1453 (2007/10/03)
A sensitive lawn-based format has been developed to screen bead-tethered combinatorial chemical libraries for antimicrobial activity. This method has been validated with beads linked to penicillin V via a photocleavable chemical linker in several analyses including a spike-and-recover experiment. The lawn-based screen sensitivity was modified to detect antibacterial compounds of modest potency, and a demonstration experiment with a naive combinatorial library of over 46,000 individual triazines was evaluated for antibacterial activity. Numerous hits were identified, and both active and inactive compounds were resynthesized and confirmed in traditional broth assays. This demonstration experiment suggests that novel antimicrobial compounds can be easily identified from very large combinatorial libraries of small, nonpeptidic compounds.
