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Boro-norleucine as a P1 residue for the design of selective and potent DPP7 inhibitors
- Source :
- Bioorganicmedicinal chemistry letters. 15(19)
- Publication Year :
- 2005
-
Abstract
- 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.
- Subjects :
- Stereochemistry
Clinical Biochemistry
Norleucine
Pharmaceutical Science
Biochemistry
Chemical synthesis
Substrate Specificity
Residue (chemistry)
chemistry.chemical_compound
Inhibitory Concentration 50
Structure-Activity Relationship
Drug Discovery
Structure–activity relationship
Humans
Dipeptidyl-Peptidases and Tripeptidyl-Peptidases
Molecular Biology
Alkyl
chemistry.chemical_classification
Dipeptide
biology
Organic Chemistry
Dipeptides
Boronic Acids
Enzyme
chemistry
Enzyme inhibitor
Drug Design
biology.protein
Molecular Medicine
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 15
- Issue :
- 19
- Database :
- OpenAIRE
- Journal :
- Bioorganicmedicinal chemistry letters
- Accession number :
- edsair.doi.dedup.....aea2d11dfa8f1be80ee25e269573224e