Potential transition-state inhibitors of glyoxalase. I

Richard B. Brandt; Mark E. Brandt; Michael E. April; Colin Thomson

doi:10.1002/qua.560220731

Potential transition-state inhibitors of glyoxalase. I

International Journal of Quantum Chemistry ◽

10.1002/qua.560220731 ◽

2009 ◽

Vol 22 (S9) ◽

pp. 335-343

Author(s):

Richard B. Brandt ◽

Mark E. Brandt ◽

Michael E. April ◽

Colin Thomson

Keyword(s):

Transition State ◽

Glyoxalase I

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A metabolically stable tight-binding transition-state inhibitor of glyoxalase-I

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2006.08.121 ◽

2006 ◽

Vol 16 (23) ◽

pp. 6039-6042 ◽

Cited By ~ 14

Author(s):

Swati S. More ◽

Robert Vince

Keyword(s):

Transition State ◽

Tight Binding ◽

Glyoxalase I

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Bivalent Transition-State Analogue Inhibitors of Human Glyoxalase I

Organic Letters ◽

10.1021/ol035917s ◽

2003 ◽

Vol 5 (25) ◽

pp. 4855-4858 ◽

Cited By ~ 8

Author(s):

Zhe-Bin Zheng ◽

Donald J. Creighton

Keyword(s):

Transition State ◽

Glyoxalase I ◽

Transition State Analogue ◽

Transition State Analogue Inhibitors

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Reaction Mechanism of Glyoxalase I Explored by an X-ray Crystallographic Analysis of the Human Enzyme in Complex with a Transition State Analogue†

Biochemistry ◽

10.1021/bi990696c ◽

1999 ◽

Vol 38 (41) ◽

pp. 13480-13490 ◽

Cited By ~ 92

Author(s):

Alexander D. Cameron ◽

Marianne Ridderström ◽

Birgit Olin ◽

Malcolm J. Kavarana ◽

Donald J. Creighton ◽

...

Keyword(s):

Reaction Mechanism ◽

Transition State ◽

Crystallographic Analysis ◽

Glyoxalase I ◽

X Ray ◽

Human Enzyme ◽

Transition State Analogue

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Inhibition of glyoxalase I: a possible transition-state analogue inhibitor approach to potential antineoplastic agents?

FEBS Letters ◽

10.1016/0014-5793(79)80539-6 ◽

1979 ◽

Vol 106 (2) ◽

pp. 393-396 ◽

Cited By ~ 36

Author(s):

Kenneth T. Douglas ◽

Iffat N. Nadvi

Keyword(s):

Transition State ◽

Antineoplastic Agents ◽

Glyoxalase I ◽

Transition State Analogue

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Partial transition-state inhibitors of glyoxalase I from human erythrocytes, yeast and rat liver

Biochimica et Biophysica Acta (BBA) - Protein Structure and Molecular Enzymology ◽

10.1016/0167-4838(85)90074-3 ◽

1985 ◽

Vol 829 (1) ◽

pp. 109-118 ◽

Cited By ~ 13

Author(s):

Kenneth T. Douglas ◽

Dhanesh I. Gohel ◽

Iffat N. Nadvi ◽

A.Joy Quilter ◽

Andrew P. Seddon

Keyword(s):

Transition State ◽

Rat Liver ◽

Human Erythrocytes ◽

Glyoxalase I

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Memapsin 2, a drug target for Alzheimer's disease

Biochemical Society Symposium ◽

10.1042/bss0700213 ◽

2003 ◽

Vol 70 ◽

pp. 213-220 ◽

Cited By ~ 1

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.

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