5L8A

Targeting the PEX14-PEX5 interaction by small molecules provides novel therapeutic routes to treat trypanosomiases.

Summary for 5L8A

• Entry DOI: 10.2210/pdb5l8a/pdb
• Related: 2W84
• Descriptor: Peroxin 14, 1-(2-hydroxyethyl)-5-[(4-methoxynaphthalen-1-yl)methyl]-~{N}-(phenylmethyl)-6,7-dihydro-4~{H}-pyrazolo[4,3-c]pyridine-3-carboxamide, GLYCINE, ... (6 entities in total)
• Functional Keywords: trypanosomiasis, glycosome, protein-protein interaction inhibitor, structure-based drug discovery, inhibitor, signaling protein
• Biological source: Trypanosoma brucei brucei
• Total number of polymer chains: 4
• Total formula weight: 33574.68

Authors

Dawidowski, M.,Emmanouilidis, L.,Sattler, M.,Popowicz, G.M. (deposition date: 2016-06-07, release date: 2017-03-08, Last modification date: 2024-01-10)

• Primary citation: Dawidowski, M.,Emmanouilidis, L.,Kalel, V.C.,Tripsianes, K.,Schorpp, K.,Hadian, K.,Kaiser, M.,Maser, P.,Kolonko, M.,Tanghe, S.,Rodriguez, A.,Schliebs, W.,Erdmann, R.,Sattler, M.,Popowicz, G.M.; Inhibitors of PEX14 disrupt protein import into glycosomes and kill Trypanosoma parasites.; Science, 355:1416-1420, 2017; PubMed: 28360328; DOI: 10.1126/science.aal1807

Experimental method

X-RAY DIFFRACTION (1.57 Å)