Crystal structure of a glutaminyl cyclase in complex with NHV-1009

Discovery of highly potent human glutaminyl cyclase (QC) inhibitors as anti-Alzheimer's agents by the combination of pharmacophore-based and structure-based design.

Glutaminyl cyclase,sQC,Glutaminyl-tRNA cyclotransferase,Glutamyl cyclase,EC

AWPEEKNYHQPAILNSSALRQIAEGTSISEMWQNDLQPLLIERYPGSPGSYAARQHIMQRIQRLQADWVLEIDTFLSQTP
YGYRSFSNIISTLNPTAKRHLVLACHYDSKYFSHWNNRVFVGATDSAVPCAMMLELARALDKKLLSLKTVSDSKPDLSLQ
LIFFDGEEAFLHWSPQDSLYGSRHLAAKMASTPHPPGARGTSQLHGMDLLVLLDLIGAPNPTFPNFFPNSARWFERLQAI
EHELHELGLLKDHSLEGRYFQNYSYGGVIQDDHIPFLRRGVPVLHLIPSPFPEVWHTMDDNEENLDESTIDNLNKILQVF
VLEYLHL

4M Ammonium acetate, pH 7.0, 0.1M Bis-Tris propane

glutaminyl cyclases (QCs), Alzheimer disease, TRANSFERASE