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Compound class:
Peptide or derivative
Comment: A side chain modified dipeptide inhibitor of PepT1 (Peptide transporter 1 / SLC15A1) [2].
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
| References |
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1. Biegel A, Knütter I, Hartrodt B, Gebauer S, Theis S, Luckner P, Kottra G, Rastetter M, Zebisch K, Thondorf I et al.. (2006)
The renal type H+/peptide symporter PEPT2: structure-affinity relationships. Amino Acids, 31 (2): 137-56. [PMID:16868651] |
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2. Knütter I, Hartrodt B, Theis S, Foltz M, Rastetter M, Daniel H, Neubert K, Brandsch M. (2004)
Analysis of the transport properties of side chain modified dipeptides at the mammalian peptide transporter PEPT1. Eur J Pharm Sci, 21 (1): 61-7. [PMID:14706812] |
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3. Stauffer M, Jeckelmann JM, Ilgü H, Ucurum Z, Boggavarapu R, Fotiadis D. (2022)
Peptide transporter structure reveals binding and action mechanism of a potent PEPT1 and PEPT2 inhibitor. Commun Chem, 5 (1): 23. [PMID:36697632] |
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4. Theis S, Knutter I, Hartrodt B, Brandsch M, Kottra G, Neubert K, Daniel H. (2002)
Synthesis and characterization of high affinity inhibitors of the H+/peptide transporter PEPT2. J Biol Chem, 277 (9): 7287-92. [PMID:11751927] |
