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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 
 
 
 
 
 

Synthesis and structure-activity relationship of N-alkyl Gly-boro-Pro inhibitors of DPP4, FAP, and DPP7.

The structure-activity relationship of various N-alkyl Gly-boro-Pro derivatives against three dipeptidyl peptidases (DPPs) was studied. In a series of N-cycloalkyl analogs, DPP4 and fibroblast activation protein-alpha (FAP) optimally preferred N-cycloheptyl whereas DPP7 tolerated even larger cycloalkyl rings. Gly alpha-carbon derivatization of N-cyclohexyl or N-(2-adamantyl) Gly-boro-Pro resulted in a significant decrease in potency against all the three DPPs.[1]

References

  1. Synthesis and structure-activity relationship of N-alkyl Gly-boro-Pro inhibitors of DPP4, FAP, and DPP7. Hu, Y., Ma, L., Wu, M., Wong, M.S., Li, B., Corral, S., Yu, Z., Nomanbhoy, T., Alemayehu, S., Fuller, S.R., Rosenblum, J.S., Rozenkrants, N., Minimo, L.C., Ripka, W.C., Szardenings, A.K., Kozarich, J.W., Shreder, K.R. Bioorg. Med. Chem. Lett. (2005) [Pubmed]
 
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