Cation-pi interactions at the active site of factor Xa: dramatic enhancement upon stepwise N-alkylation of ammonium ions.

Abstract

Efficient ligands of factor Xa usually feature a more or less preorganized central scaffold which orients two approximately orthogonal vectors to fill the S1 and S4 pockets at the enzyme active site. In earlier work, the S1 pocket was mainly occupied by an aromatic ring bearing a basic residue, such as a phenylamidinium substituent, which in the protonated… (More)
DOI: 10.1002/anie.200804695

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