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A Single Second Shell Amino Acid Determines Affinity and Kinetics of Linagliptin Binding to Type 4 Dipeptidyl Peptidase and Fibroblast Activation Protein

Drugs targeting type 4 dipeptidyl peptidase (DPP‐4) are beneficial for glycemic control, whereas fibroblast activation protein alpha (FAP‐α) is a potential target for cancer therapies. Unlike other gliptins, linagliptin displays FAP inhibition. We compared biophysical and structural characteristics...

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Detalles Bibliográficos
Autores principales: Schnapp, Gisela, Hoevels, Yvette, Bakker, Remko A., Schreiner, Patrick, Klein, Thomas, Nar, Herbert
Formato: Online Artículo Texto
Lenguaje:English
Publicado: John Wiley and Sons Inc. 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7984154/
https://www.ncbi.nlm.nih.gov/pubmed/33030297
http://dx.doi.org/10.1002/cmdc.202000591