Crystal Structure of an Acylation Transition-State Analog of the TEM-1 β-Lactamase. Mechanistic Implications for Class A β-Lactamases†

Biochemistry ◽  
1998 ◽  
Vol 37 (8) ◽  
pp. 2622-2628 ◽  
Author(s):  
Laurent Maveyraud ◽  
R. F. Pratt ◽  
Jean-Pierre Samama
Keyword(s):  
Crystal Structure ◽  
Transition State ◽  
Transition State Analog ◽  
Class A

Cytidine Deaminase. The 2·3 Å Crystal Structure of an Enzyme: Transition-state Analog Complex

1994 ◽  
Vol 235 (2) ◽  
pp. 635-656 ◽  
Author(s):  
Laurie Betts ◽  
Shibin Xiang ◽  
Steven A. Short ◽  
Richard Wolfenden ◽  
Charles W. Carter
Keyword(s):  
Crystal Structure ◽  
Transition State ◽  
Cytidine Deaminase ◽  
Transition State Analog

Memapsin 2, a drug target for Alzheimer's disease

2003 ◽  
Vol 70 ◽  
pp. 213-220 ◽  
Author(s):  
Gerald Koelsch ◽  
Robert T. Turner ◽  
Lin Hong ◽  
Arun K. Ghosh ◽  
Jordan Tang
Keyword(s):  
Crystal Structure ◽  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Transition State ◽  
Amyloid Precursor Protein ◽  
Therapeutic Target ◽  
Drug Target ◽  
Aspartic Protease ◽  
Precursor Protein ◽  
Memapsin 2

Mempasin 2, a ϐ-secretase, is the membrane-anchored aspartic protease that initiates the cleavage of amyloid precursor protein leading to the production of ϐ-amyloid and the onset of Alzheimer's disease. Thus memapsin 2 is a major therapeutic target for the development of inhibitor drugs for the disease. Many biochemical tools, such as the specificity and crystal structure, have been established and have led to the design of potent and relatively small transition-state inhibitors. Although developing a clinically viable mempasin 2 inhibitor remains challenging, progress to date renders hope that memapsin 2 inhibitors may ultimately be useful for therapeutic reduction of ϐ-amyloid.

Crystal structure of cobra-venom phospholipase A2 in a complex with a transition-state analogue

Science ◽  
1990 ◽  
Vol 250 (4987) ◽  
pp. 1560-1563 ◽  
Author(s):  
S. White ◽  
D. Scott ◽  
Z. Otwinowski ◽  
M. Gelb ◽  
P. Sigler
Keyword(s):  
Crystal Structure ◽  
Transition State ◽  
Phospholipase A2 ◽  
Cobra Venom ◽  
Transition State Analogue
Sign in / Sign up

Export Citation Format

Share Document