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Literature summary for 3.4.14.5 extracted from

  • Longenecker, K.L.; Stewart, K.D.; Madar, D.J.; Jakob, C.G.; Fry, E.H.; Wilk, S.; Lin, C.W.; Ballaron, S.J.; Stashko, M.A.; Lubben, T.H.; Yong, H.; Pireh, D.; Pei, Z.; Basha, F.; Wiedeman, P.E.; von Geldern, T.W.; Trevillyan, J.M.; Stoll, V.S.
    Crystal structures of DPP-IV (CD26) from rat kidney exhibit flexible accommodation of peptidase-selective inhibitors (2006), Biochemistry, 45, 7474-7482.
    View publication on PubMed

Crystallization (Commentary)

Crystallization (Comment) Organism
vapor diffusion method, 2.8 A resolution Rattus norvegicus

Inhibitors

Inhibitors Comment Organism Structure
(1R,3S)-2-[(2S)-2-amino-2-cyclopentylacetyl]-3-ethynylcyclopentanecarbonitrile
-
Homo sapiens
(1R,3S)-2-[(2S)-2-amino-2-cyclopentylacetyl]-3-ethynylcyclopentanecarbonitrile
-
Rattus norvegicus
(2S)-1-[(2S)-2-amino-2-cyclopentylacetyl]pyrrolidine-2-carbonitrile
-
Homo sapiens
(2S)-1-[(2S)-2-amino-2-cyclopentylacetyl]pyrrolidine-2-carbonitrile
-
Rattus norvegicus
(2S,5R)-1-[(2S)-2-amino-2-cyclopentylacetyl]-5-prop-1-yn-1-ylpyrrolidine-2-carbonitrile
-
Homo sapiens
(2S,5R)-1-[(2S)-2-amino-2-cyclopentylacetyl]-5-prop-1-yn-1-ylpyrrolidine-2-carbonitrile
-
Rattus norvegicus
2-([8-(3-aminopiperidin-1-yl)-1,3-dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl]methyl)benzonitrile
-
Homo sapiens
2-([8-(3-aminopiperidin-1-yl)-1,3-dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl]methyl)benzonitrile
-
Rattus norvegicus
additional information conformational flexibility of tyr548 is unique among protein family members and may be utilized in drug design to achieve peptidase selectivity Homo sapiens
additional information conformational flexibility of tyr548 is unique among protein family members and may be utilized in drug design to achieve peptidase selectivity Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Rattus norvegicus P14740
-
-

Source Tissue

Source Tissue Comment Organism Textmining
kidney
-
Rattus norvegicus
-

Synonyms

Synonyms Comment Organism
CD26
-
Rattus norvegicus

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000001
-
(2S)-1-[(2S)-2-amino-2-cyclopentylacetyl]pyrrolidine-2-carbonitrile
-
Rattus norvegicus
0.000001
-
2-([8-(3-aminopiperidin-1-yl)-1,3-dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl]methyl)benzonitrile
-
Homo sapiens
0.000002
-
(2S)-1-[(2S)-2-amino-2-cyclopentylacetyl]pyrrolidine-2-carbonitrile
-
Homo sapiens
0.000003
-
2-([8-(3-aminopiperidin-1-yl)-1,3-dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl]methyl)benzonitrile
-
Rattus norvegicus
0.000008
-
(1R,3S)-2-[(2S)-2-amino-2-cyclopentylacetyl]-3-ethynylcyclopentanecarbonitrile
-
Homo sapiens
0.000012
-
(1R,3S)-2-[(2S)-2-amino-2-cyclopentylacetyl]-3-ethynylcyclopentanecarbonitrile
-
Rattus norvegicus
0.00003
-
(2S,5R)-1-[(2S)-2-amino-2-cyclopentylacetyl]-5-prop-1-yn-1-ylpyrrolidine-2-carbonitrile
-
Homo sapiens
0.000056
-
(2S,5R)-1-[(2S)-2-amino-2-cyclopentylacetyl]-5-prop-1-yn-1-ylpyrrolidine-2-carbonitrile
-
Rattus norvegicus