Bioorganic & medicinal chemistry letters

An enthalpic basis of additivity in biphenyl hydroxamic acid ligands for stromelysin-1

EM Wilfong, Y Du, EJ Toone

Index: Wilfong, Erin M.; Du, Yu; Toone, Eric J. Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 20 p. 6521 - 6524

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Citation Number: 4

Abstract

Fragment based drug discovery remains a successful tool for pharmaceutical lead discovery. Although based upon the principle of thermodynamic additivity, the underlying thermodynamic basis is poorly understood. A thermodynamic additivity analysis was performed using stromelysin-1 and a series of biphenyl hydroxamate ligands identified through fragment additivity. Our studies suggest that, in this instance, additivity arises from ...