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

Boro-norleucine as a P1 residue for the design of selective and potent DPP7 inhibitors.

Dipeptide-based inhibitors with C-substituted (alkyl or aminoalkyl) alpha-amino acids in the P2 position and boro-norleucine (boro-Nle) in the P1 position were synthesized. Relative to boro-proline, boro-Nle as a P1 residue was shown able to significantly dial out DPP4, FAP, DPP8, and DPP9 activity. Dab-boro-Nle (4g) proved to be the most selective and potent DPP7 inhibitor with a DPP7 IC50 value of 480 pM.[1]

References

  1. Boro-norleucine as a P1 residue for the design of selective and potent DPP7 inhibitors. Shreder, K.R., Wong, M.S., Corral, S., Yu, Z., Winn, D.T., Wu, M., Hu, Y., Nomanbhoy, T., Alemayehu, S., Fuller, S.R., Rosenblum, J.S., Kozarich, J.W. Bioorg. Med. Chem. Lett. (2005) [Pubmed]
 
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