Literature summary for 5.2.1.8 extracted from

Demange, L.; Moutiez, M.; Dugave, C.
Synthesis and evaluation of Glypsi(PO2R-N)Pro-containing pseudopeptides as novel inhibitors of the human cyclophilin hCyp-18 (2002), J. Med. Chem., 45, 3928-3933.

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Inhibitors

Inhibitors	Comment	Organism	Structure
Ac-Ala-GlyPSI(PO2Et-N)Pro-Phe-4-nitroanilide	transition-state analogue of peptidylprolyl isomerase activity of cyclophilin Cyp-18, Kd value 0.127 mM	Homo sapiens
Suc-Ala-Ala-Pro-Phe-4-nitroanilide	transition-state analogue of peptidylprolyl isomerase activity of cyclophilin Cyp-18, Kd value 0.138 mM	Homo sapiens
Suc-Ala-GlyPSI(PO2Et-N)Pro-Phe-4-nitroanilide	transition-state analogue of peptidylprolyl isomerase activity of cyclophilin Cyp-18, Kd value 0.02 mM. Selectively inhibits Cyp-18, but not enzyme isoform FKBP12	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	isoform cyclophilin Cyp-18	-

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.015	-	10°C	Homo sapiens	Suc-Ala-GlyPSI(PO2Et-N)Pro-Phe-4-nitroanilide
0.215	-	10°C	Homo sapiens	Ac-Ala-GlyPSI(PO2Et-N)Pro-Phe-4-nitroanilide
0.54	-	10°C	Homo sapiens	Suc-Ala-Ala-Pro-Phe-4-nitroanilide

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Release 2023.1 (January 2023)