Bisnorcymserine, an Alzheimer's disease therapeutic currently in clinical studies, acts as inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), two enzymes involved in the development and progression of the disease. To elucidate structural determinants contributing to the BChE versus AChE selectivity shown by this compound and to clarify the clearance mechanism, we undertook kinetic studies and, based on the results, crystallized and analyzed the x ray structure of the complex between AChE and bisnorcymserine.
Structural and Kinetic Studies of the Experimental Alzheimer's Disease Therapeutic Bisnorcymserine
C Bartolucci;D Lamba
2012
Abstract
Bisnorcymserine, an Alzheimer's disease therapeutic currently in clinical studies, acts as inhibitor of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), two enzymes involved in the development and progression of the disease. To elucidate structural determinants contributing to the BChE versus AChE selectivity shown by this compound and to clarify the clearance mechanism, we undertook kinetic studies and, based on the results, crystallized and analyzed the x ray structure of the complex between AChE and bisnorcymserine.File in questo prodotto:
Non ci sono file associati a questo prodotto.
I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
