7ZYF

Insulin regulated aminopeptidase (IRAP) in complex with a nanomolar alpha hydroxy beta amino acid based inhibitor.

Summary for 7ZYF

• Entry DOI: 10.2210/pdb7zyf/pdb
• Descriptor: Leucyl-cystinyl aminopeptidase, pregnancy serum form, DI(HYDROXYETHYL)ETHER, 2-AMINO-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, ... (12 entities in total)
• Functional Keywords: insulin regulated aminopeptidase, irap, hsplap, bestatin analogues, alpla hydroxy beta amino acid based inhibitor, hydrolase
• Biological source: Homo sapiens (human)
• Total number of polymer chains: 2
• Total formula weight: 210241.13

Authors

Mpakali, A.,Stratikos, E.,Giastas, P.,Papakyriakou, A. (deposition date: 2022-05-24, release date: 2022-07-20, Last modification date: 2024-01-31)

• Primary citation: Vourloumis, D.,Mavridis, I.,Athanasoulis, A.,Temponeras, I.,Koumantou, D.,Giastas, P.,Mpakali, A.,Magrioti, V.,Leib, J.,van Endert, P.,Stratikos, E.,Papakyriakou, A.; Discovery of Selective Nanomolar Inhibitors for Insulin-Regulated Aminopeptidase Based on alpha-Hydroxy-beta-amino Acid Derivatives of Bestatin.; J.Med.Chem., 65:10098-10117, 2022; PubMed: 35833347; DOI: 10.1021/acs.jmedchem.2c00904

Experimental method

X-RAY DIFFRACTION (2.81 Å)