5717-81-7Relevant academic research and scientific papers
Design of potent inhibitors for Schistosoma japonica glutathione S-transferase
Jao, Shu-Chuan,Chen, Jessica,Yang, Kelvin,Li, Wen-Shan
, p. 304 - 318 (2007/10/03)
We implemented both structure-based drug design and the concept of polyvalency to discover a series of potent and unsymmetrical Schistosoma japonicum glutathione S-transferase (SjGST) inhibitors 10-12. This strategy achieved not only an excellent enhancement (10- to 490-fold) in the inhibitory potency, compared to the monofunctional analogues 1-5, but was also an effective modification by selecting a hydrophobic moiety with a flexible linker. The designed compounds with a low micromolar hit demonstrate special values in refining the new generation of SjGST inhibitors. The stoichiometry of the binding is one inhibitor molecule per SjGST monomer via isothermal titration calorimetric measurement.
Lithocholic acid analogues, new and potent α-2,3-sialyltransferase inhibitors
Chang, Kai-Hsuan,Lee, Lenselot,Chen, Jessica,Li, Wen-Shan
, p. 629 - 631 (2008/02/10)
A new type of noncompetitive α-2,3-sialyltransferase inhibitor has been synthesized; we report the discovery, preparation and inhibitory activity of sixteen lithocholic acid analogues. The Royal Society of Chemistry 2006.
