Chapter Nine

I J. Ellis Bell

I Department of Chemistry

I Gottwald Science Center

I University of Richmond

I Richmond, Virginia f James C. Burnett

(■ School of Pharmacy and Department of Medicinal Chemistry I Institute for Structural Biology and Drug Discovery Virginia Commonwealth University Richmond, Virginia

Jessica K. Bell

Department of Pharmaceutical Chemistry University of California at San Francisco San Francisco, California

Peter S. Galatin : Donald J. Abraham

School of Pharmacy and Department of Medicinal Chemistry Institute for Structural Biology and Drug Discovery Virginia Commonwealth University Richmond, Virginia

Contents l Introduction, 296

2 Allosteric Theory and Models, 296

2.l The Monod-Wyman-Changeux

2.l.l Monod-Wyman-Changeaux: The

Concerted Model, 300

gel: The Sequential Model, 301

2.2 Hemoglobin: Classic Example of Allostery,

2.3 Common Features of Allosteric Proteins, 304

Burger's Medicinal Chemistry and Drug Discovery Sixth Edition, Volume 2: Drug Development Edited by Donald J. Abraham ISBN 0-471-37028-2 © 2003John Wiley & Sons, Inc.

2.4 Understanding Allosteric Transitions at the Molecular Level, 3G5

2.5 The Molecular Mechanisms of Allosteric Changes, 306

2.6 The Basis for Allosteric Effectors as Potential Therapeutic Agents, 312

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